Search Result
Results for "
receptor
" in MedChemExpress (MCE) Product Catalog:
9927
Inhibitors & Agonists
75
Biochemical Assay Reagents
703
Isotope-Labeled Compounds
| Cat. No. |
Product Name |
Target |
Research Areas |
Chemical Structure |
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- HY-14234
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Glucocorticoid Receptor
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Metabolic Disease
Inflammation/Immunology
Endocrinology
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Glucocorticoid receptor agonist is a Glucocorticoid receptor agonist that acts on Glucocorticoid receptor (GR), progesterone receptor (PR) and mineralocorticoid receptor (MR) with the IC50 values of 2.1 , 1200 and 210 nM, respectively. Glucocorticoid receptor agonist has steroid-like anti-inflammatory properties and may be used to improve metabolism and reduce increased levels of body fat and serum insulin .
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- HY-148435
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Glucocorticoid Receptor
ADC Cytotoxin
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Inflammation/Immunology
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Glucocorticoid receptor agonist-2 (compound 21) is an glucocorticoid receptor agonist with an IC50 value of 6.6 nM. Glucocorticoid receptor agonist-2 can be used to synthesize anti-inflammatory ADC molecules. Glucocorticoid receptor agonist-2 is an active reference of ABBV-3373 .
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- HY-10861
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5-HT Receptor
Dopamine Receptor
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Neurological Disease
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D3/5-HT receptor modulator-1 (compound 5i) is a selective dopamine D3 receptor and 5-HT2A receptor antagonist and a partial 5-HT1A receptor agonist. D3/5-HT receptor modulator-1 shows Ki values of 4.5 nM, 11.9 nM, and 15.3 nM for dopamine D3, 5-HT2A, and 5-HT2A receptors. D3/5-HT receptor modulator-1 has a low affinity for dopamine D2 receptors, 5-HT2C receptors, and hERG channels. D3/5-HT receptor modulator-1 has an atypical antipsychotic profile .
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- HY-144419
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Adenosine Receptor
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Cancer
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Adenosine receptor antagonist 3 is a potent antagonist of adenosine receptor. Adenosine receptor antagonist 3 has the potential for the research of cancer disease (extracted from patent WO2019233994A1, compound 1) .
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- HY-161090
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iGluR
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Neurological Disease
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AMPA receptor modulator-7 (compound 36) is a modulator of AMPA receptor. AMPA receptor modulator-7 has oral activity and can penetrate the blood-brain barrier .
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- HY-147560
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Sigma Receptor
Opioid Receptor
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Neurological Disease
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σ1 Receptor/μ Opioid receptor modulator 1 (Compound 44) is a potent σ1 receptor antagonist and μ opioid receptor agonist with Kis of 1.86 nM and 2.1 nM, respectively.σ1 Receptor/μ Opioid receptor modulator 1 exhibits potent analgesic activity. σ1 Receptor/μ Opioid receptor modulator 1 can be used for the research of neuropathic pain .
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- HY-160173
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LPL Receptor
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Others
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LPA receptor antagonist-1 (example 52) is an antagonist of lysophosphatidic acid (LPA) receptor. LPA receptor antagonist-1 can be used for kinds of studies .
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- HY-109572
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GABA Receptor
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Neurological Disease
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GABAA receptor modulator-1 (9eey) is a GABAA receptor modulator that can be used in the study of central nervous system diseases .
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- HY-145458
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GCGR
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Metabolic Disease
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GLP-1 receptor agonist 9 is a GLP-1 receptor agonist, example 7, extracted from WO2020234726 A1 .
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- HY-151515
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Dopamine Receptor
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Neurological Disease
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Dopamine D2 receptor agonist-2 (compound 36) is a potent dopamine D2 receptor biased agonism ligand with an Ki value of 11.2 nM. Dopamine D2 receptor agonist-2 can be used to research antipsychosis .
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- HY-153816
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GLP Receptor
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Metabolic Disease
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GLP-1 receptor agonist 12 (compound 20A) is an agonist of GLP Receptor. GLP-1 receptor agonist 12 can be used in the study of diseases such as diabetes .
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- HY-160615
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- HY-P2518
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Protease Activated Receptor (PAR)
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Inflammation/Immunology
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Protease-Activated Receptor-1, PAR-1 Agonist is a selective proteinase-activated receptor1 (PAR-1) agonist peptide. Protease-Activated Receptor-1, PAR-1 Agonist corresponds to PAR1 tethered ligand and which can selectively mimic theactions of thrombin via this receptor .
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- HY-115953
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Dopamine Receptor
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Neurological Disease
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Dopamine D3 receptor ligand is a potent, selective and high affinity ligand for Dopamine D3 receptor with 89-fold selective for D3 over D2 (D3 Ki= 8 nM, D2 Ki= 715 nM) .
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- HY-144204
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Estrogen Receptor/ERR
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Endocrinology
Cancer
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Estrogen receptor antagonist 5 is a potent antagonist of Estrogen receptor. The estrogen receptor is a ligand-activated transcriptional regulatory protein that mediates induction of a variety of biological effects through its interaction with endogenous estrogens. Estrogen receptor antagonist 5 has the potential for the research of metastatic disease (extracted from patent WO2017174757A1, compound 165) .
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- HY-144206
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Estrogen Receptor/ERR
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Endocrinology
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Estrogen receptor antagonist 6 is a potent antagonist of Estrogen receptor. The estrogen receptor is a ligand-activated transcriptional regulatory protein that mediates induction of a variety of biological effects through its interaction with endogenous estrogens. Estrogen receptor antagonist 6 has the potential for the research of metastatic disease (extracted from patent WO2017174757A1, compound 166) .
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- HY-150059
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- HY-P2519
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- HY-108513
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Sigma Receptor
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Neurological Disease
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σ1 Receptor antagonist 4 (compound TC1) is a selective sigma1 (σ1) receptor antagonist with a Ki of 10 nM. σ1 Receptor antagonist 4 is weakly active at σ2 receptor (Ki of 370 nM) and has no activity at dopamine (DAT), serotonin (SERT), and norepinephrine (NET) transporters .
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- HY-162851
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Adenosine Receptor
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Others
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Adenosine receptor agonist 1 (compound 6m) is an A3 adenosine receptor (AR) partial agonist with Ki value of 6.7 nM .
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- HY-153798
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GLP Receptor
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Metabolic Disease
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GLP-1 receptor agonist 10 (compound 42) is an agonist of GLP Receptor. GLP-1 receptor agonist 10 inhibits food intake and reduces glucose excursion in mice. GLP-1 receptor agonist 10 can be used in the study of type 2 diabetes (T2DM) and obesity .
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- HY-147542
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- HY-169752
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Apelin Receptor (APJ)
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Cardiovascular Disease
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APJ receptor agonist 11 (Ex 174) is a APJ receptor agonist with IC50 values ranging from 0.01 nM to 10 nM. APJ receptor agonist 11 can be used in the study of cardiovascular diseases .
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- HY-144138
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Estrogen Receptor/ERR
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Cancer
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Estrogen receptor antagonist 2 is a selective estrogen receptor downregulator. Estrogen (E2) and estrogen alpha receptor (ERα) are important drivers of breast cancer development. Estrogen receptor antagonist 2 has the potential for the research of breast cancer diseases (extracted from patent WO2021228210A1, compound 3) .
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- HY-144137
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Estrogen Receptor/ERR
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Cancer
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Estrogen receptor antagonist 1 is a selective estrogen receptor antagonist. Estrogen (E2) and estrogen alpha receptor (ERα) are important drivers of breast cancer development. Estrogen receptor antagonist 1 has the potential for the research of breast cancer diseases (extracted from patent WO2021249533A1, compound 4) .
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- HY-120273
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Glucocorticoid Receptor
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Metabolic Disease
Inflammation/Immunology
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Glucocorticoids receptor agonist 3 is a potent agonist of glucocorticoids receptor. Glucocorticoids receptor agonist 3 is useful to research diseases, such as obesity, diabetes, and inflammation (extracted from patent WO2000066522A1, compound 345) .
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- HY-P2519A
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- HY-139314
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Adenosine Receptor
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Metabolic Disease
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A2B receptor antagonist 2 (compound 18) is an adenosine receptor A2B antagonist, with Ki values of 2.30 μM, 6.8 μM and 3.44 μM for rA1, rA2A and hA2B, respectively .
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- HY-145250
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- HY-145775
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Fc Receptor (FcR)
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Inflammation/Immunology
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hIgG–hFc receptor-IN-1 (comp 66) is a human immunoglobulin G–human neonatal Fc receptor (hIgG–hFcRn) protein-protein interaction inhibitor, with an IC50 of 2 μM .
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- HY-144064
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Adenosine Receptor
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Cancer
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Adenosine receptor antagonist 2 is an orally active A2a/A2b adenosine receptor antagonist with IC50s of 1 nM and 3 nM, respectively. Adenosine receptor antagonist 2 has anti-tumor activity .
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- HY-156968
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GLP Receptor
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Metabolic Disease
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GLP-1 receptor agonist 14 (compound 73) is a potent agonist of glucagon-like peptide-1 (GLP-1). GLP-1 receptor agonist 14 plays an important role in diabetes or other metabolic disorders .
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- HY-153477
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- HY-113591
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Cannabinoid Receptor
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Others
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CB2 receptor agonist 10 is a CB2 receptor agonist with a Ki of 3.7 nM for hCB2, a Ki of 110 nM for hCB1, and an EC50 of 0.52 nM for hCB2 .
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- HY-107580
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GPR109A
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Cardiovascular Disease
Metabolic Disease
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GPR109 receptor agonist-1 (Compound 3a) is a highly selective agonist of the human orphan G-protein-coupled receptor GPR109b, with the pEC50 of 6.4. GPR109 receptor agonist-1 can be used for the research of cardio-metabolic diseases .
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- HY-160076
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Apelin Receptor (APJ)
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Cardiovascular Disease
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APJ receptor agonist 8 (compound 99) is an agonist of APJ receptor. APJ receptor agonist 8 increases the load independent cardiac contractility of isolated perfused rat hearts .
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- HY-400878
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Glucocorticoid Receptor
Drug-Linker Conjugates for ADC
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Cancer
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Glucocorticoid receptor agonist-1 phosphate Gly-Glu-Mal, a glucocorticoid receptor agonist, is a drug-linker conjugate for ADC. Glucocorticoid receptor agonist-1 phosphate Gly-Glu-Mal can be used to synthesize the anti-CD40 antibody agent conjugates (WO2019106608A1; example 9) .
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- HY-145284
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Apelin Receptor (APJ)
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Cardiovascular Disease
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APJ receptor agonist 4 is a potent and orally active agonist of apelin receptor (APJ) with EC50 and Ki of 0.06 nM and 0.07 nM respectively. APJ receptor agonist 4 displays excellent pharmacokinetic profiles in the rodent heart failure (HF) model. APJ receptor agonist 4 also shows an acceptable safety profile in preclinical toxicology studies. APJ receptor agonist 4 leads to improved cardiac function and can be used for researching the HF disease .
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- HY-147398
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Dopamine Receptor
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Neurological Disease
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Dopamine D4 receptor antagonist-1 is a selective DRD4 antagonists, with a Ki of 9.0 nM for Hd4.2. Dopamine D4 receptor antagonist-1 can be used in study of schizophrenia .
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- HY-144139
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Estrogen Receptor/ERR
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Cancer
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Estrogen receptor antagonist 3 is a potent antagonist of estrogen receptor (ER). The estrogen signaling system plays an important role in regulating cell growth, differentiation and apoptosis. Estrogen receptor antagonist 3 has the potential for the research of cancer diseases (extracted from patent WO2021213358A1, compound 7) .
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- HY-144202
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Estrogen Receptor/ERR
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Cancer
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Estrogen receptor antagonist 4 is a potent antagonist of estrogen receptor (ER). The estrogen signaling system plays an important role in regulating cell growth, differentiation and apoptosis. Estrogen receptor antagonist 4 has the potential for the research of cancer diseases (extracted from patent WO2021213358A1, compound 1) .
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- HY-W071581
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Glucocorticoid Receptor
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Inflammation/Immunology
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Glucocorticoid receptor activator 1 (compound A) is a phenyl aziridine precursor and an activator of the glucocorticoid receptor (GR). Glucocorticoid receptor activator 1 down-modulates TNF-induced pro-inflammatory gene expression by activating GR and can be utilized in inflammation research .
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- HY-172099
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- HY-145285
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Apelin Receptor (APJ)
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Cardiovascular Disease
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APJ receptor agonist 5 (compound 3) is a potent and orally active agonist of apelin receptor (APJ) with an EC50 of 0.4 nM. APJ receptor agonist 5 displays excellent pharmacokinetic profiles in the rodent heart failure (HF) model. APJ receptor agonist 5 also shows an acceptable safety profile in preclinical toxicology studies. APJ receptor agonist 5 leads to improved cardiac function and can be used for researching the HF disease .
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- HY-143313
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Protease Activated Receptor (PAR)
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Cardiovascular Disease
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Protease-Activated Receptor-1 antagonist 1 (Compound 13) is a protease-activated receptor-1 (PAR-1) antagonist with the IC50 of 3 nM by FLIPR technology. Protease-Activated Receptor-1 antagonist 1 can be used for the research of thrombotic cardiovascular, myocardial infarction, and peripheral arterial disease .
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- HY-144609
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Opioid Receptor
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Neurological Disease
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Mu opioid receptor antagonist 4 (compound 31) is a potent and selective μ opioid receptor (MOR) antagonist with a Ki of 0.38 nM and an EC50 of 1.07 nM. Mu opioid receptor antagonist 4 has remarkable CNS antagonism against morphine, and precipitated fewer withdrawal symptoms than Naloxone. Mu opioid receptor antagonist 4 Mu opioid receptor antagonist 4 can be used for researching opioid use disorders (OUD) .
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- HY-163895
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Fluorescent Dye
Opioid Receptor
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Neurological Disease
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δ opioid receptor antagonist 1 (compound 6-Cy3) is a fluorescent antagonist probe with high selectivity for δ opioid receptor (DOR) (Ki=1.7 nM). δ opioid receptor antagonist 1 can be used to study the mechanism of pain perception .
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- HY-155319
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Opioid Receptor
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Neurological Disease
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μ opioid receptor agonist 3 (compound 20) is a potent μ opioid receptor (µOR) agonist with an EC50 of 0.87 nM. μ opioid receptor agonist 3 has the potential for pain and neuropsychiatric indications research .
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- HY-147751
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Arrestin
Apelin Receptor (APJ)
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Cardiovascular Disease
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APJ receptor agonist 6 (compound 9) is a potent APJ (apelin receptor) agonist, with Ki of 1.3 μM. APJ receptor agonist 6 has EC50 values of 0.070 , 0.097, and 0.063 μM for calcium, cAMP, and β-arrestin, respectively .
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- HY-162125
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Angiotensin Receptor
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Cardiovascular Disease
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AT2 receptor ligand-1(compound 14) is a potent angiotensin AT2 receptor ligand with the Ki 4.9 nM. AT2 receptor ligand-1 shows high stability in microsomes of the sulfonamide ligands .
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- HY-144608
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Opioid Receptor
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Neurological Disease
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Mu opioid receptor antagonist 3 (compound 26) is a potent and selective μ opioid receptor (MOR) antagonist with a Ki of 0.24 nM and an EC50 of 0.54 nM. Mu opioid receptor antagonist 3 has remarkable CNS antagonism against morphine, and precipitated fewer withdrawal symptoms than Naloxone. Mu opioid receptor antagonist 3 can be used for researching opioid use disorders (OUD) .
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- HY-152121
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- HY-144610
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Opioid Receptor
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Neurological Disease
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Mu opioid receptor antagonist 5 (compound NAP) is a selective and blood-brain barrier (BBB) penetrant μ opioid receptor (MOR) antagonist with an EC50 value of 1.14 nM and a Ki value of 0.37 nM. Mu opioid receptor antagonist 5 can be used for researching opioid use disorders (OUD) .
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- HY-155737
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Estrogen Receptor/ERR
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Cardiovascular Disease
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ET receptor antagonist 1 (compound 16h) is an orally active ET receptor antagonist (IC50=0.18 nM), which can be used for research in pulmonary arterial hypertension (PAH). ET receptor antagonist 1 attenuates monocrotaline (HY-N0750) induced PAH in rat model .
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- HY-155739
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Estrogen Receptor/ERR
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Cardiovascular Disease
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ET receptor antagonist 3 (compound 17d) is an orally active ET receptor antagonist (IC50=0.26 nM), which can be used for research in pulmonary arterial hypertension (PAH). ET receptor antagonist 3 attenuates monocrotaline (HY-N0750) induced PAH in rat model .
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- HY-155738
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Estrogen Receptor/ERR
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Cardiovascular Disease
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ET receptor antagonist 2 (compound 16j) is an orally active ET receptor antagonist (IC50=0.22 nM), which can be used for research in pulmonary arterial hypertension (PAH). ET receptor antagonist 2 attenuates monocrotaline (HY-N0750) induced PAH in rat model .
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- HY-149975
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iGluR
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Neurological Disease
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AMPA receptor modulator-4, a 3,4-dihydro-2H-1,2,4-benzothiadiazine 1,1-dioxide (BTD), is an orally active positive allosteric modulator of the AMPA receptors (AMPAR PAMs). AMPA receptor modulator-4 can cross the blood-brain barrier. AMPA receptor modulator-4 increases the cognition performance and improves working memory performance in mice .
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- HY-144698
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mGluR
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Neurological Disease
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mGlu4 receptor agonist 1 (compound 62) is a potent mGlu4 receptor positive allosteric modulator, with an EC50 of 308 nM. mGlu4 receptor agonist 1 shows significant anxiolytic- and antipsychotic-like effect .
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- HY-153458
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- HY-168562
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Sigma Receptor
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Neurological Disease
Cancer
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σ1 Receptor ligand 1 (compound 5I) is a σ1 receptor ligand with a Ki of 3.9 nM. σ1 Receptor ligand 1 has a high plasma protein binding (89%) and promising metabolic stability in the presence of mouse liver microsomes and NADPH. σ1 Receptor ligand 1 can be utilized in neurological and cancer research .
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- HY-147908
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Adenosine Receptor
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Inflammation/Immunology
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Adenosine receptor inhibitor 2 (compound 14b) is a potent AR (adenosine receptor) inhibitor. Adenosine receptor inhibitor 2 shows dual affinity toward A1/A2A ARs with higher affinity for the A1- than the A2AAR. Adenosine receptor inhibitor 2 has Ki values of 52.2 nM for the A1AR and 167 nM for the A2AAR .
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- HY-144607
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Opioid Receptor
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Neurological Disease
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Mu opioid receptor antagonist 2 (compound 25) is a potent, selective and blood-brain barrier (BBB) penetrant μ opioid receptor (MOR) antagonist with a Ki of 0.37 nM and an EC50 of 0.44 nM. Mu opioid receptor antagonist 2 has remarkable CNS antagonism against morphine, and precipitated fewer withdrawal symptoms than Naloxone. Mu opioid receptor antagonist 2 can be used for researching opioid use disorders (OUD) .
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- HY-P0078
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TRAP-6
4 Publications Verification
PAR-1 agonist peptide; Thrombin receptor Activator Peptide 6
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Protease Activated Receptor (PAR)
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Inflammation/Immunology
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TRAP-6 (PAR-1 agonist peptide), a peptide fragment, is a selective protease activating receptor 1 (PAR1) agonist. TRAP-6 activates human platelets via the thrombin receptor. TRAP-6 shows no activity at PAR4 .
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- HY-142919
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Opioid Receptor
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Neurological Disease
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μ opioid receptor agonist 2 （Compound H-3）is an optically pure oxaspiro ring substituted pyrrolopyrazole derivative, acts as a MOR receptor agonist and can be used for the research of pain and pain related diseases .
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- HY-142918
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Opioid Receptor
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Neurological Disease
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μ opioid receptor agonist 1 （Compound H-1a）is an optically pure oxaspiro ring substituted pyrrolopyrazole derivative, acts as a MOR receptor agonist and can be used for the research of pain and pain related diseases .
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- HY-159492
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5-HT Receptor
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Neurological Disease
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5-HT7 receptor ligand 2 (compound 32) is an arylpiperazinehydrazine ligand for 5-HT7R (Ki=178 nM). 5-HT7 receptor ligand 2 has good membrane permeability, low hepatotoxicity and cardiotoxicity, and high plasma protein binding. 5-HT7 receptor ligand 2 shows neuroprotective effects in SH-SY5Y cells and can be used for the study of central nervous system related diseases .
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- HY-P0297
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- HY-145258
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GABA Receptor
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Neurological Disease
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GABAA receptor agent 6 (compound 2027) is a potent γ-GABAAR antagonist with an Ki of 0.56 µM. GABAA receptor agent 6 shows γ-GABAAR antagonist activity with low cellular membrane permeability .
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- HY-162977
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- HY-164817
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Cannabinoid Receptor
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Cancer
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CB1/2 receptor-1 (compound 5.3) is a CB1/2 receptor agonist. CB1/2 receptor-1 can be used in angiogenesis research .
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- HY-154798
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iGluR
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Neurological Disease
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AMPA receptor modulator-5 (Example 217) is an AMPA receptor modulator. AMPA receptor modulator-5 can be used for research of neurological disease .
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- HY-10036
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- HY-50159
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- HY-50158
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- HY-155628
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iGluR
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Others
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AMPA receptor modulator-6 is an AMPA receptor positive allosteric modulator (PAM). AMPA receptor modulator-6 can be used in the study of neurological diseases .
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- HY-P0283
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- HY-164860
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Glucocorticoid Receptor
ADC Cytotoxin
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Inflammation/Immunology
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Glucocorticoid receptor agonist-5 (compound 4), a glucocorticoid molecule, is a potent glucocorticoid receptor agonist. Glucocorticoid receptor agonist-5 shows anti-inflammatory and immunosuppressive activity. Glucocorticoid receptor agonist-5 is used as an ADC Cytotoxin for antibody-drug conjugate .
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- HY-160177
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- HY-153535
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- HY-136905
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iGluR
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Others
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AMPA receptor antagonist-2 (example 23) is an AMPA receptor antagonist .
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- HY-160664
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Prostaglandin Receptor
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Cardiovascular Disease
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TP receptor antagonist-2 (example 7n) is a thromboxane A2 receptor (TP receptor) antagonist, with IC50 values of 5.64 and 5.27 μM for TPα and TPβ, respectively. TP receptor antagonist-2 inhibits platelet aggregation .
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- HY-170902
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GABA Receptor
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Neurological Disease
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GABAA receptor modulator-4 (Compound 4) is the negative allosteric modulator for GABAA receptor. GABAA receptor modulator-4 inhibits α1β3γ2 GABAA receptor-mediated peak and steady currents with IC50 of 10 μM and 10 μM .
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- HY-P0317
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- HY-131953
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Androgen Receptor
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Cancer
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Androgen receptor-IN-3 (Compound 22) is an androgen receptor inhibitor. Androgen receptor-IN-3 inhibits AR-driven transcriptional activity in LNCaP cells, with an IC50 of 5.04 μM .
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- HY-139627
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- HY-118914
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GCGR
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Glucagon receptor antagonist inactive control (Compound 2) is a compound structurally similar to the glucagon receptor (GCGR) antagonist Glucagon receptor antagonist (Compound 1) but lacks antagonistic activity against glucagon receptor (GCGR). Glucagon receptor antagonist inactive control can be used as a negative control to study mechanisms related to glucagon receptor-mediated signaling pathways .
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- HY-136275
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iGluR
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Others
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AMPA receptor modulator-2 (Example 134) is a AMPA receptor modulator, with a pIC50 of 10.1 for TARPγ8 dependent AMPA receptor . pIC50 = -lgIC50.
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- HY-P5889
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Thrombin
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Cardiovascular Disease
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Thrombin receptor peptide ligand is a thrombin receptor antagonist peptide that can be used as an antithrombotic agent .
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- HY-145959
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iGluR
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Neurological Disease
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AMPA receptor antagonist-3 is an AMPA receptor antagonist extracted from patent US20070027143A1. AMPA receptor antagonist-3 can be used for the research of central nervous system disorders .
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- HY-122150
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iGluR
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Neurological Disease
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AMPA receptor modulator-3 is an allosteric AMPA receptor modulator (EC50: 4.4 μM). AMPA receptor modulator-3 can be used in the research of mammalian nervous system, such as learning and memory .
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- HY-151220
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Androgen Receptor
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Others
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Androgen receptor-IN-4 (Compound 206) is an androgen receptor inhibitor, and can be used for research of Kennedy's disease .
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- HY-153129
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Prostaglandin Receptor
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Endocrinology
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EP2 receptor antagonist-2 (CID891729) is an antagonist of EP2 receptor. EP2 receptor antagonist-2 inhibits the EP2 receptor activation induced by PGE2. EP2 receptor antagonist-2 also suppresses lactate dehydrogenase (LDH) release induced by N-methyl-D-aspartate (NMDA) .
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- HY-155478
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|
|
Androgen Receptor
|
Cancer
|
|
Androgen receptor-IN-6 (compound 16) is an orally available androgen receptor (Androgen Receptor) potent inhibitor (IC50=0.12 μM in vitro), targeting the disordered N-terminal domain (NTD). Androgen receptor-IN-6 has good Caco2 cell membrane permeability and has an oral activity (F/%) of 16% in male CD-1 mice .
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-
- HY-161784
-
|
|
GABA Receptor
|
Neurological Disease
|
|
GABAA receptor modulator-5 (Compound S28) is a modulator for (γ-aminobutyric acid)A receptor (GABAA receptor), with EC50 of 56 nM and 10 nM, for α1β2γ2 and α4β3δ subtype. GABAA receptor modulator-5 exhibits good pharmacokinetic characteristics in rats. GABAA receptor modulator-5 is slightly toxic toxicity in rats with a loss of rollover reflex (LORR) threshold dose of 23.3 μmol/kg, and exhibits potential ameliorating the postpartum depression .
|
-
- HY-W1006471
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-
- HY-P1840
-
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|
Neuropeptide Y Receptor
|
Neurological Disease
Endocrinology
|
|
Galanin Receptor Ligand M35 is a high-affinity ligand and antagonist of galanin receptor (Kd=0.1 nM). Galanin Receptor Ligand M35 exerts a Ki values of 0.11 and 2.0 nM for human galanin receptor type 1 and 2, respectively .
|
-
- HY-U00339
-
-
- HY-128781
-
|
|
GCGR
|
Metabolic Disease
|
|
Glucagon receptor antagonist-5 (compound 13K) is a potent and orally bioavailable indazole-based glucagon receptor antagonist (Ki=32 nM). Glucagon receptor antagonist-5 has potential for the treatment of type 2 diabetes mellitus (T2DM) .
|
-
- HY-W681071
-
-
- HY-128103
-
|
|
GCGR
Adenylate Cyclase
|
Metabolic Disease
|
|
Glucagon receptor antagonist-7 (Compound 1) is an antagonist for hGCGR, that inhibits the binding of 125I-labeled glucagon to the human glucagon receptor (hGCGR) with IC50 of 181 nM. Glucagon receptor antagonist-7 activates glucagon-stimulated adenylyl cyclase with a KDB of 81 nM in CHO cell. Glucagon receptor antagonist-7 inhibits glucagon-mediated glycogenolysis in human hepatocytes, and lowers blood glucose levels .
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-
- HY-153276
-
|
|
Androgen Receptor
|
Cancer
|
|
Androgen receptor-IN-5 is an androgen receptor inhibitor with potent anticancer effects. Androgen receptor-IN-5 also inhibits the production of IL-17A, IL- 17F and INF-γ (WO2023281097A1,Example 1/1) .
|
-
- HY-170498
-
|
|
GABA Receptor
|
Neurological Disease
|
|
GABA-A Receptor Ligand-1 (Compound 4) is a ligand for GABA-A receptor with a pKi of 7.27. GABA-A Receptor Ligand-1 reduces mitochondrial dysfunction, promotes neurite outgrowth and neuronal regeneration. GABA-A Receptor Ligand-1 exhibits neuroprotective efficacy in rats ischemic stroke models .
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-
- HY-112189
-
|
|
IFNAR
|
Inflammation/Immunology
|
|
Interferon receptor inducer-1 (compound 6) is an interferon (IFN) receptor inducer. Used accordingly in the treatment of a disorder in which the induction of interferon is involved .
|
-
- HY-162764
-
|
|
Androgen Receptor
|
Cancer
|
|
Androgen receptor degrader-5 (compound 14k) exhibits promising properties, including superior androgen receptor degradation activity and antiproliferative activity .
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-
- HY-163065
-
|
|
Opioid Receptor
Sigma Receptor
|
Neurological Disease
|
|
σ1 Receptor/μ Opioid receptor modulator 2 (compound 4x) is a dual μOR agonist/σ1R antagonist, and displays picomolar μOR agonism activity (EC50: 0.6 ± 0.2 nM) and good σ1R inhibitory activity (Ki: 363.7 ± 5.6 nM). σ1 Receptor/μ Opioid receptor modulator 2 exhibits robust analgesic effects in various pain models .
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-
- HY-156522
-
|
|
CFTR
|
Endocrinology
|
|
CRF1 receptor antagonist-1 (Compound 2) is a CRF1 receptor antagonist. CRF1 receptor antagonist-1 can be used for research of congenital adrenal hyperplasia (CAH) .
|
-
- HY-170033
-
|
|
Opioid Receptor
|
Neurological Disease
|
|
3-Carboxamidonaltrexone (example 32) is a opioid receptor binding compound with Ki values of 1.9 nM, 110 nM, and 22 nM for μ-opioid receptor, δ-opioid receptor, and K-opioid receptor, respectively .
|
-
- HY-153478
-
|
|
Estrogen Receptor/ERR
|
Cancer
|
|
Estrogen receptor modulator 7 is a potent estrogen receptor modulator. Estrogen receptor modulator 7 can be used in research of cancer .
|
-
- HY-W063197
-
|
|
Adenosine Receptor
|
Cancer
|
|
Adenosine receptor antagonist 4 (compound 2) is an adenosine A1 receptor antagonist with a Ki of 101 nM for human A1 receptor .
|
-
- HY-147736
-
|
|
GABA Receptor
|
Neurological Disease
|
|
GABAA receptor agonist 2 (compound 4c) is a potent GABAA receptor agonist. GABAA receptor agonist 2 shows anti-depression activities in classical mouse models of depression of FST and TST. GABAA receptor agonist 2 binds at the GABA binding site of GABAA receptor in order to produce GABAergic effects. GABAA receptor agonist 2 has the potential for the research of depression .
|
-
- HY-147735
-
|
|
GABA Receptor
|
Neurological Disease
|
|
GABAA receptor agonist 1 (compound 3e) is a potent GABAA receptor agonist. GABAA receptor agonist 1 shows anti-depression activities in classical mouse models of depression of FST and TST. GABAA receptor agonist 1 binds at the GABA binding site of GABAA receptor in order to produce GABAergic effects. GABAA receptor agonist 1 has the potential for the research of depression .
|
-
- HY-160179
-
-
- HY-131974
-
-
- HY-160931
-
|
|
iGluR
|
Neurological Disease
|
|
NMDA receptor modulator 8 (Compound 3-6) is a modulator for NMDA receptor, with 50%-100% potentiation of NMDA receptor at 10 μM .
|
-
- HY-121488
-
|
|
Interleukin Related
|
Neurological Disease
|
|
GP130 receptor agonist-1 is a potent, brain-penetrant and orally active GP130 receptor agonist. GP130 receptor agonist-1 has a neuroprotective effect on NMDA-induced neurotoxicity .
|
-
- HY-165155
-
|
|
Leukotriene Receptor
|
Inflammation/Immunology
|
|
CysLT1 receptor antagonist-1 (Compound 4) is an antagonist for cysteinyl leukotriene receptor 1 (CysLT1R) with an IC50 of 3.9 μM. CysLT1 receptor antagonist-1 exhibits weak agonist activity against G-protein-coupled bile acid receptor 1 (GPBAR1) with an efficact of 23% at 10 μM. CysLT1 receptor antagonist-1 can be used for asthma and allergic diseases researchs .
|
-
- HY-142941
-
|
|
Glucocorticoid Receptor
MMP
|
Inflammation/Immunology
|
|
Glucocorticoid receptor-IN-1 (Compound WX002) is a selective glucocorticoid receptor (GR) modulator with anti-inflammatory effect. Glucocorticoid receptor-IN-1 exhibits very good transcriptional repressive activity with an IC50 of 2.11 nM against hMMP1, and transcriptional activation activity with an EC50 of 5.59 nM against MMTV .
|
-
- HY-142942
-
|
|
Glucocorticoid Receptor
MMP
|
Inflammation/Immunology
|
|
Glucocorticoid receptor-IN-2 (Compound WX019) is a selective glucocorticoid receptor (GR) modulator with anti-inflammatory effect. Glucocorticoid receptor-IN-2 exhibits very good transcriptional repressive activity with an IC50 of 0.171 nM against hMMP1, and comparable transcriptional activation activity with an EC50 of 0.94 nM against MMTV .
|
-
- HY-P5914
-
|
WaTx
|
TRP Channel
|
Neurological Disease
|
|
Wasabi Receptor Toxin is a cell-penetrating scorpion toxin. Wasabi Receptor Toxin is the activator for TRPA1 ion channel with EC50 in nanomolar level, and prolongs the channel open time, but reduces Ca 2+ permeability. Wasabi Receptor Toxin causes thermal hypersensitivity and mechanical allodynia in rats, without triggering neurogenic inflammation .
|
-
- HY-145684
-
|
|
Prostaglandin Receptor
|
Inflammation/Immunology
|
|
EP2 receptor antagonist-1 (compound 1) is a potent, reversible, and agonist dependent allosteric prostaglandin EP2 receptor antagonist. EP2 receptor antagonist-1 shows anti-inflammatory effects .
|
-
- HY-145364
-
|
|
GHSR
|
Metabolic Disease
|
|
Ghrelin receptor full agonist-2 (compound 12j) is a highly potent Ghrelin receptor full agonist.
|
-
- HY-150601
-
-
- HY-143390
-
|
|
iGluR
|
Neurological Disease
|
|
NMDA receptor modulator 2 (Compound 1) is a potent NMDA receptor modulator. NMDA receptor modulator 2 can be used for neurological disorder research .
|
-
- HY-143396
-
|
|
iGluR
|
Neurological Disease
|
|
NMDA receptor modulator 5 (Compound 195) is a potent NMDA receptor modulator. NMDA receptor modulator 5 can be used for neurological disorder research .
|
-
- HY-143393
-
|
|
iGluR
|
Neurological Disease
|
|
NMDA receptor modulator 4 (Compound 169) is a potent NMDA receptor modulator. NMDA receptor modulator 4 can be used for neurological disorder research .
|
-
- HY-143391
-
|
|
iGluR
|
Neurological Disease
|
|
NMDA receptor modulator 3 (Compound 99) is a potent NMDA receptor modulator. NMDA receptor modulator 3 can be used for neurological disorder research .
|
-
- HY-143397
-
|
|
iGluR
|
Neurological Disease
|
|
NMDA receptor modulator 6 (Compound 183) is a potent NMDA receptor modulator. NMDA receptor modulator 6 can be used for neurological disorder research .
|
-
- HY-123301
-
-
- HY-146099
-
|
|
GABA Receptor
|
Neurological Disease
|
|
GABAA receptor agent 7 (compoud 5c) is a potent GABAA receptor positive modulator. GABAA receptor agent 7 shows anticonvulsant activity in vitro and in vivo with low neurotoxicity. GABAA receptor agent 7 has the potential for the research of epilepsy .
|
-
- HY-146100
-
|
|
GABA Receptor
|
Neurological Disease
|
|
GABAA receptor agent 8 (compoud 5e) is a potent GABAA receptor positive modulator. GABAA receptor agent 8 shows anticonvulsant activity in vitro and in vivo with low neurotoxicity. GABAA receptor agent 8 has the potential for the research of epilepsy .
|
-
- HY-153772
-
|
|
Androgen Receptor
|
Cancer
|
|
Androgen receptor antagonist 8 (Example 13) is an androgen receptor antagonist. Androgen receptor antagonist 8 inhibits prostate specific antigen secretion in LNcap cell (IC50: 88 nM). Androgen receptor antagonist 8 can be used for prostate cancer research .
|
-
- HY-149105
-
|
|
Estrogen Receptor/ERR
|
Endocrinology
|
|
FSH receptor antagonist 1 (compound 10) is a potent antagonist of the G(s)-protein-coupled human follicle-stimulating hormone (FSH) receptor. FSH receptor antagonist 1 exhibits an IC50 of 28 nM on a cell line expressing the human FSH receptor. FSH receptor antagonist 1 significantly inhibits follicle growth and ovulation in an ex vivo mouse model .
|
-
- HY-160105
-
-
- HY-112689
-
-
- HY-160659
-
|
|
Androgen Receptor
|
Endocrinology
|
|
Androgen receptor antagonist 10 (compound 6h) is a androgen receptor antagonist. Androgen receptor antagonist 10 reduces the wax esters in the golden syrian hamster model .
|
-
- HY-156541
-
-
- HY-156538
-
|
|
RXFP Receptor
|
Inflammation/Immunology
|
|
RXFP1 receptor agonist-3 (Example 223) is a RXFP1 receptor agonist. RXFP1 receptor agonist-3 stimulates cAMP production in HEK293 cells stably expressing human RXFP1, with an EC50 value of 2 nM .
|
-
- HY-156537
-
-
- HY-146026
-
|
|
Androgen Receptor
|
Cancer
|
|
Androgen receptor antagonist 3 (Compound C18) is an androgen receptor (AR) antagonist with an IC50 of 2.4 μM. Androgen receptor antagonist 3 shows anticancer activities .
|
-
- HY-133036
-
|
|
Apelin Receptor (APJ)
|
Cardiovascular Disease
|
|
APJ receptor agonist 1, a biphenyl acid derivative, is a potent APJ receptor (APJ-R) agonist (EC50s 0.093 and 0.12 nM for human and rat APJ-R, respectively). APJ receptor agonist 1 displays in vitro potency to apelin-13, the endogenous peptidic ligand for the APJ receptor. APJ receptor agonist 1 has the potential for the research of heart failure .
|
-
- HY-156543
-
-
- HY-156539
-
-
- HY-156540
-
|
|
RXFP Receptor
|
Inflammation/Immunology
|
|
RXFP1 receptor agonist-5 (Example 98) is a RXFP1 receptor agonist. RXFP1 receptor agonist-5 stimulates cAMP production in HEK293 cells stably expressing human RXFP1, with an EC50 value of 1.3 nM .
|
-
- HY-156922
-
-
- HY-156542
-
-
- HY-136922
-
-
- HY-18076
-
-
- HY-P1840A
-
|
|
Neuropeptide Y Receptor
|
Neurological Disease
Endocrinology
|
|
Galanin Receptor Ligand M35 TFA is a high-affinity ligand and antagonist of galanin receptor (Kd=0.1 nM). Galanin Receptor Ligand M35 TFA exerts a Ki values of 0.11 and 2.0 nM for human galanin receptor type 1 and 2, respectively .
|
-
- HY-150205
-
|
|
Succinate Receptor 1
|
Inflammation/Immunology
|
|
Succinate/succinate receptor antagonist 1 (compound 7a) is a succinate/succinate receptor antagonist. Succinate/succinate receptor antagonist 1 blocks succinate signaling in gingival tissue. Succinate/succinate receptor antagonist 1 inhibits the activation of succinate receptor 1 (SucnRl) with an IC50 value of 20 μΜ. Succinate/succinate receptor antagonist 1 can be used for the research of periodontal disease .
|
-
- HY-156536
-
-
- HY-136582
-
|
Androgen receptor-IN-2
|
Androgen Receptor
|
Cancer
|
|
Masofaniten (Androgen receptor-IN-2) is a potent and orally active androgen receptor inhibitor. Masofaniten has antitumor activity against prostate cancer .
|
-
- HY-149165
-
|
|
Glucocorticoid Receptor
|
Inflammation/Immunology
|
|
Glucocorticoid receptor modulator 2 (Example 1) is a glucocorticoid receptor modulator, with an IC50 value less than 100 nM. Glucocorticoid receptor modulator 2 can be used for research of inflammatory and immune diseases .
|
-
- HY-146101
-
|
|
iGluR
|
Neurological Disease
|
|
NMDA receptor antagonist 5 (Compound 10e) is a potent, brain permeable and non-toxic NMDA receptor antagonist. NMDA receptor antagonist 5 can be used for neurological disorder research .
|
-
- HY-100113
-
-
- HY-171049
-
-
- HY-133486
-
-
- HY-143315
-
|
|
Protease Activated Receptor (PAR)
|
Cardiovascular Disease
|
|
Protease-Activated Receptor-1 antagonist 3 is a potent protease-activated receptor-1 antagonist with an IC50 value of 7 nM. Protease-Activated Receptor-1 antagonist 3 shows binding affinity for hERG K + channel with an IC50 value of 9 µM .
|
-
- HY-164726
-
|
|
Estrogen Receptor/ERR
|
Others
|
|
Estrogen receptor modulator 11 (Compound 27) is a tetrahydroisoquinoline derivative. Estrogen receptor modulator 11 has a certain affinity for estrogen receptors (ER), with IC50 values of 285 nM and 421 nM for ERα and ERβ, respectively. Estrogen receptor modulator 11 lacks antagonist activity in the MCF-7 cellular assay .
|
-
- HY-160761
-
|
|
Opioid Receptor
|
Inflammation/Immunology
|
|
K-Opioid receptor agonist-1 (Compound 5a) is an agonist for κ-Opioid receptor with Ki of 0.25 nM and EC50 of 2 nM. K-Opioid receptor agonist-1 is blood brain barrier (BBB) penetrate (brain/plasma ratios of 0.50 to 0.65). K-Opioid receptor agonist-1 exhibits anti-inflammatory activity in dermatitis models induced by Arachidonic acid (HY-109590) or oxazolidinone .
|
-
- HY-147352
-
|
|
iGluR
|
Neurological Disease
|
|
NMDA receptor potentiator-1 (Compound 1368) is a subunit selective NMDA receptor potentiator with IC50s of 4 μM and 5 μM against NR2C and NR2D expression, respectively .
|
-
- HY-170654
-
|
|
Opioid Receptor
|
Neurological Disease
|
|
Opioid receptor antagonist 1 (Compound 10) is an Orvinol (HY-D0168)-based opioid receptor antagonist. Opioid receptor antagonist 1 has antagonistic activity to the analgesic properties of Morphine .
|
-
- HY-169349
-
|
|
Androgen Receptor
|
Cancer
|
|
Androgen receptor antagonist 12 (Compound EF2) is an orally active Androgen receptor (AR) antagonist (IC50: 0.30 μM). Androgen receptor antagonist 12 inhibits transcriptional activity of variant AR mutants and and the proliferation of AR-positive PCa cell lines. Androgen receptor antagonist 12 blocks AR nuclear translocation. Androgen receptor antagonist 12 inhibits tumor growth in a C4-2B xenograft mouse model. Androgen receptor antagonist 12 can be used for prostate cancer (PCa) research .
|
-
- HY-139876
-
-
- HY-103418
-
|
|
Dopamine Receptor
|
Neurological Disease
|
|
Dopamine D2 receptor agonist-3 (compound 3) is a selective D2 receptor
partial agonist and Dopamine D3 receptor antagonist (with pEC50 of 8.3 and <5.5 respectively) .
|
-
- HY-143253
-
|
|
Estrogen Receptor/ERR
|
Cancer
|
|
Estrogen receptor antagonist 7 (compound 13) is a potent estrogen receptors (ER) antagonist. Estrogen receptor antagonist 7 has antiproliferative activity against breast and ovarian cancer cells. Anticancer and anti-uterotrophic activities .
|
-
- HY-146027
-
|
|
Androgen Receptor
|
Cancer
|
|
Androgen receptor antagonist 4 (Compound AT2) is an androgen receptor (AR) antagonist with an IC50 of 0.15 μM. Androgen receptor antagonist 4 efficiently antagonizes AR transcriptional activity, suppresses downstream target gene of AR, and blocks the DHT-induced AR nuclear translocation. Androgen receptor antagonist 4 shows anticancer activities .
|
-
- HY-127024
-
|
|
Thyroid Hormone Receptor
|
Metabolic Disease
|
|
Thyroid hormone receptor antagonist (1-850) is a competitive, selective and high-affinity thyroid hormone receptor (TR) antagonist with an IC50 of 1.5 μM for antagonizing the effect of T3 on TR. Thyroid hormone receptor antagonist (1-850) blocks T3-mediated interaction of TRα and TRβ with nuclear receptor coactivator. Thyroid hormone receptor antagonist (1-850) has no effect on the activity of RARα .
|
-
- HY-P5914A
-
|
WaTx TFA
|
TRP Channel
|
Neurological Disease
|
|
Wasabi Receptor Toxin TFA (WaTx TFA) is the TFA salt form of Wasabi Receptor Toxin (HY-P5914). Wasabi Receptor Toxin TFA is a cell-penetrating scorpion toxin. Wasabi Receptor Toxin TFA is the activator for TRPA1 ion channel with EC50 in nanomolar level, and prolongs the channel open time, but reduces Ca 2+ permeability. Wasabi Receptor Toxin TFA causes thermal hypersensitivity and mechanical allodynia in rats, without triggering neurogenic inflammation .
|
-
- HY-75502
-
|
N-0923; (-)-N 0437
|
Dopamine Receptor
Adrenergic Receptor
5-HT Receptor
|
Neurological Disease
Endocrinology
|
|
Rotigotine is a potent dopamine receptor agonist with Ki values of 0.71?nM, 4-15?nM, and 83?nM for the dopamine D3 receptor and D2, D5, D4 receptors and dopamine D1 receptor. Rotigotine a partial agonist of the 5-HT1A receptor, and an antagonist of the α2B-adrenergic receptor. Rotigotine can be used for parkinson's disease (PD) research .
|
-
- HY-106617A
-
|
|
5-HT Receptor
Adrenergic Receptor
|
Neurological Disease
|
|
Etoperidone hydrochloride, an antidepressant agent, is an orally active serotonin and nor-adrenaline re-uptake antagonist. Etoperidone hydrochloride shows Kd values of 36 nM, 38 nM, 85 nM, and 570 nM for 5-HT2 receptor, α1-adrenergic receptor, 5-HT1A receptor, and α2-adrenergic receptor, respectively .
|
-
- HY-106617
-
|
|
5-HT Receptor
Adrenergic Receptor
|
Neurological Disease
|
|
Etoperidone, an antidepressant agent, is an orally active serotonin and nor-adrenaline re-uptake antagonist. Etoperidone shows Kd values of 36 nM, 38 nM, 85 nM, and 570 nM for 5-HT2 receptor, α1-adrenergic receptor, 5-HT1A receptor, and α2-adrenergic receptor, respectively .
|
-
- HY-139708
-
|
|
iGluR
|
Neurological Disease
|
|
NMDA receptor antagonist-3, a NMDA receptor antagonist, stands out with a remarkable percentage of recovery (40.0%, at 100 μM) and safe toxicological profile in SH-SY5Y and human adipose mesenchymal stem cells.
|
-
- HY-143314
-
|
|
Protease Activated Receptor (PAR)
|
Cardiovascular Disease
|
|
Protease-Activated Receptor-1 antagonist 2 is an orally active protease-activated receptor-1 (PAR-1) antagonist, with an IC50 value of 7 nM. Protease-Activated Receptor-1 antagonist 2 has favorable pharmacokinetic properties which is useful in the research of cardiovascular disease (CVD), such as atherosclerosis and restenosis .
|
-
- HY-150692
-
|
|
Estrogen Receptor/ERR
|
Cancer
|
|
Estrogen receptor α antagonist 1 (compound 35) is a highly selective antagonist of estrogen receptor α, with IC50s of 0.02, 6.55 and 7.73 μM for estrogen receptor α, estrogen receptor β and MCF-7 cells, respectively. Estrogen receptor α antagonist 1 can be used for the research of cancer .
|
-
- HY-162466
-
|
|
Proton Pump
|
Others
|
|
ABA receptor agonist 1 (compound 4c) is a receptor agonist for abscisic acid (ABA). ABA receptor agonist 1 can inhibit seed germination and seedling growth of Arabidopsis and rice, stomatal closure and drought resistance of wheat and soybean .
|
-
- HY-155185A
-
|
|
iGluR
|
Neurological Disease
|
|
NMDA receptor antagonist 8 (Compound (R)-10a) is GluN2B subunit-selective NMDA Receptor antagonist, with an Ki of 265 nM and an IC50 of 62 nM. NMDA receptor antagonist 8 can be used for research of neurodegenerative diseases .
|
-
- HY-155185
-
|
|
iGluR
|
Neurological Disease
|
|
NMDA receptor antagonist 7 (Compound (S)-10a) is GluN2B subunit-selective NMDA Receptor antagonist, with an Ki of 93 nM and an IC50 of 72 nM. NMDA receptor antagonist 7 can be used for research of neurodegenerative diseases .
|
-
- HY-75502R
-
|
|
Dopamine Receptor
Adrenergic Receptor
5-HT Receptor
|
Neurological Disease
Endocrinology
|
|
Rotigotine (Standard) is the analytical standard of Rotigotine. This product is intended for research and analytical applications. Rotigotine is a potent dopamine receptor agonist with Ki values of 0.71 nM, 4-15 nM, and 83 nM for the dopamine D3 receptor and D2, D5, D4 receptors and dopamine D1 receptor. Rotigotine a partial agonist of the 5-HT1A receptor, and an antagonist of the α2B-adrenergic receptor. Rotigotine can be used for parkinson's disease (PD) research .
|
-
- HY-161520
-
|
|
Glucocorticoid Receptor
NF-κB
|
Inflammation/Immunology
|
|
Glucocorticoid receptor/NF-κB modulator-1 (Compound 20) is a derivative of ocotillol. Glucocorticoid receptor/NF-κB modulator-1 suppresses the degradation of glucocorticoid receptor (GR) mRNA and GR protein, inhibits the activation of NF-κB signaling pathway. Glucocorticoid receptor/NF-κB modulator-1 downregulates levels of NO, interleukin-6 and tumor necrosis factor-alpha (TNF-α). Glucocorticoid receptor/NF-κB modulator-1 ameliorates sepsis in mouse model .
|
-
- HY-146494
-
|
|
Androgen Receptor
|
Cancer
|
|
Androgen receptor antagonist 5 (compound 42f) is a potent androgen receptor (AR) antagonist with an IC50 value of 6.17 μM. Androgen receptor antagonist 5 can effectively impair AR nuclear translocation, reducing the levels of nuclear AR, and disrupts AR-mediated gene regulation. Androgen receptor antagonist 5 has antiproliferative activity against LNCaP and exhibits antitumor activity in LNCaP xenograft tumor mice model. Androgen receptor antagonist 5 can be used for researching prostate cancer .
|
-
- HY-15618
-
|
M1 receptor modulator
|
mAChR
|
Neurological Disease
|
|
MK-7622 (M1 receptor modulator) is a muscarinic M1 receptor positive allosteric modulator .
|
-
- HY-139709
-
-
- HY-139710
-
-
- HY-P5431
-
|
|
Insulin Receptor
|
Others
|
|
Insulin receptor (1142-1153), pTyr1150 is a biological active peptide. (Peptide used as insulin receptor tyrosine kinase substrate.)
|
-
- HY-110201
-
|
|
Estrogen Receptor/ERR
|
Cancer
|
|
Estrogen receptor modulator 1 (compound 18) is an orally active and selective estrogen receptor modulator (SERM), with a pIC50 of 0.46. Estrogen receptor modulator 1 induces regression of Tamoxifen-resistant, hormone independent xenograft tumors .
|
-
- HY-110161
-
|
|
Somatostatin Receptor
|
Cardiovascular Disease
Endocrinology
|
|
sst2 Receptor agonist-1 is a potent somatostatin receptor subtype 2 (sst2) agonist with a Ki value of 0.025 nM and a cAMP IC50 value of 4.8 nM. sst2 Receptor agonist-1 can inhibit rat growth hormone (GH) secretion and ocular neovascular lesion formation. Antiangiogenic effect .
|
-
- HY-163672
-
|
|
Glucocorticoid Receptor
|
Metabolic Disease
Inflammation/Immunology
|
|
Glucocorticoid receptor modulator 3 (Payload 6) is a thioester-containing glucocorticoid receptor modulator (IC50=0.6 nM). Glucocorticoid receptor modulator 3 is designed to inactivate unconjugated payloads rapidly through liver metabolism, thereby minimizing systemic exposure. Glucocorticoid receptor modulator 3 can be utilized in the development of antibody-drug conjugates (ADCs) targeting autoimmune diseases .
|
-
- HY-10672
-
|
|
Urotensin Receptor
Cytochrome P450
Sodium Channel
Opioid Receptor
|
Cardiovascular Disease
|
|
Urotensin-II receptor antagonist-1 (compound 1) is a low oral bioavailability (F=0-3%, rat) selective human Urotensin II receptor antagonist, Ki=16 nM (test on HEK293 cells expressing recombinant human UT receptor). Urotensin-II receptor antagonist-1 inhibits cytochrome P450 (IC50=0.75 μM, CYP2D6; 1.4 μM, CYP3A4), inhibits κ-opioid receptor (EC50=3.2 μM), targets cardiac sodium channels (Ki=2.5 μM) .
|
-
- HY-P2518A
-
|
|
Protease Activated Receptor (PAR)
|
Cancer
|
|
Protease-Activated Receptor-1, PAR-1 Agonist TFA is a selective proteinase-activated receptor1 (PAR-1) agonist peptide. Protease-Activated Receptor-1, PAR-1 Agonist TFA corresponds to PAR1 tethered ligand and which can selectively mimic theactions of thrombin via this receptor .
|
-
- HY-155049
-
|
|
iGluR
|
Neurological Disease
|
|
NMDA receptor antagonist 6 (compound 13b) is an antagonist of NMDA receptor, targeting to the glycine binding site. NMDA receptor antagonist 6 shows cytoneuroprotective potency, and protects PC12 cells against NMDA-induced injury and cell apoptosis .
|
-
- HY-170419
-
|
|
Apelin Receptor (APJ)
|
Cardiovascular Disease
|
|
APJ receptor agonist 10 (Compound I choline salt) modulates the activity of APJ receptor and can be used in research about pulmonary arterial hypertension. APJ receptor agonist 10 exhibits good bioavailability other than its free base form .
|
-
- HY-162771
-
|
|
Opioid Receptor
|
Neurological Disease
|
|
Mu opioid receptor agonist 1 (compound 12) is a Mu opioid receptor agonist. Mu opioid receptor agonist 1 can be used in nervous system related research .
|
-
- HY-137093
-
-
- HY-U00387
-
-
- HY-163673
-
|
|
Glucocorticoid Receptor
Drug-Linker Conjugates for ADC
|
Inflammation/Immunology
|
|
Glucocorticoid receptor modulator 4 (Compound DL5) is a conjugate of a linker and a glucocorticoid receptor modulator. Glucocorticoid receptor modulator 4 exhibits GRE Reporter activity in mTNF expressing K562 cell with an EC50 of 40 μM. Glucocorticoid receptor modulator 4 binds with an anti-tumor necrosis factor (TNF) antibody, and exhibits anti-inflammtory activity against arthritis in mouse models .
|
-
- HY-145256
-
|
|
GABA Receptor
|
Neurological Disease
|
|
GABAA receptor agent 4 (compound 1e) is a potent γ-GABAAR antagonist with an Ki of 0.18 µM. GABAA receptor agent 4 efficiently rescues inhibition of T cell proliferation. GABAA receptor agent 4 has the immunomodulatory potential .
|
-
- HY-155406
-
|
|
Estrogen Receptor/ERR
Caspase
Bcl-2 Family
|
Cancer
|
|
Estrogen receptor modulator 10 (compound G-5b) is an estrogen receptor (ER) antagonist (IC50=6.7 nM) and degrader (DC50=0.4 nM). Estrogen receptor modulator 10 is developed based on the Fulvestrant (HY-13636) molecule and can rapidly degrade ER receptors through the proteasome pathway. Estrogen receptor modulator 10 can induce cell apoptosis and block cells in the G1/G0 phase and can be used in cancer research .
|
-
- HY-14229
-
|
CCDC
|
G protein-coupled Bile Acid Receptor 1
Calcium Channel
|
Metabolic Disease
|
|
TGR5 Receptor Agonist (CCDC), a potent Takeda G protein-coupled receptor 5 (TGR5; GPCR19) agonist, shows improved potency in the U2-OS cells and melanophore cells with pEC50s of 6.8 and 7.5, respectively. TGR5 Receptor Agonist can induce peripheral and central hypersensitivity to bladder distension in mice, and increase intracellular Ca 2+ concentration. TGR5 Receptor Agonist can also reduces food intake and improves insulin responsiveness, in diet-induced obese mice. TGR5 Receptor Agonist can be used to research diabetes, bladder hypersensitivity and anti-obesity .
|
-
- HY-U00420
-
-
- HY-133123
-
|
|
Prostaglandin Receptor
|
Inflammation/Immunology
Cancer
|
|
EP4 receptor antagonist 1 is a highly potent and selective competitive prostanoid EP4 receptor antagonist for cancer immunotherapy. EP4 receptor antagonist 1 inhibits human and mouse EP4 receptor with IC50s of 6.1 nM and 16.2 nM, respectively. IC50s >10 μM for human EP1, EP2,and EP3 receptors .
|
-
- HY-136645
-
|
|
Prostaglandin Receptor
|
Cancer
|
|
EP4 receptor antagonist 2 (compound 2-13) is a potent EP4 receptor antagonist with an IC50 of 7.8 nM. EP4 receptor antagonist 2 shows antitumor activity .
|
-
- HY-138501
-
|
|
ERK
|
Inflammation/Immunology
|
|
GPR34 receptor antagonist 2 (Compound D2) is a GPR34 receptor antagonist. GPR34 receptor antagonist 2 can be used for immune diseases, inflammatory diseases research .
|
-
- HY-147657
-
|
|
GABA Receptor
|
Neurological Disease
|
|
GABAA receptor modulator-2 (Compound 20) is selective, orally active α5-GABAAR negative allosteric modulator (NAM) with a Ki of 4.1 nM. GABAA receptor modulator-2 shows high-metabolic stability and good CNS safety .
|
-
- HY-115955
-
|
|
Dopamine Receptor
|
Neurological Disease
|
|
Dopamine D3 receptor ligand-3 (compound 12C) is a potent D3 receptor ligand with a Ki of 3.6 nM. Dopamine D3 receptor ligand-3 have high selectivity for D3 over D2 (Ki=353 nM).
|
-
- HY-115954
-
|
|
Dopamine Receptor
|
Neurological Disease
|
|
Dopamine D3 receptor ligand-2 (compound 8) is a potent D3 receptor ligand with a Ki of 11.4 nM. Dopamine D3 receptor ligand-2 have high selectivity for D3 over D2 (Ki=1228 nM) .
|
-
- HY-138690
-
|
|
Estrogen Receptor/ERR
|
Endocrinology
|
|
Estrogen receptor modulator 6 (compound 3a) is a selective estrogen receptor (ER) β agonist (Ki=0.44 nM). Estrogen receptor modulator 6 displays 19-fold selectivity for ERβ over ERα(Ki=8.4 nM) .
|
-
- HY-162669
-
|
|
Opioid Receptor
|
Neurological Disease
|
|
Mu opioid receptor antagonist 8 (368) is a μ-opioid receptor antagonist. Mu opioid receptor antagonist 8 (368) significantly inhibits met-enkephalin-induced µOR activation of Gi .
|
-
- HY-147907
-
|
|
Adenosine Receptor
|
Neurological Disease
Inflammation/Immunology
Cancer
|
|
Adenosine receptor inhibitor 1 is a potent and selective adenosine receptor (AR) inhibitor with Ki values of >1000, 68.5, >1000, >1000 nM for A1AR, A2AAR, A2BAR, A3AR, respectively. Adenosine receptor inhibitor 1 shows antinociceptive activity, anti-inflammatory effect and peripheral analgesic effect. Adenosine receptor inhibitor 1 has the potential for the research of cancer or neurodegenerative diseases .
|
-
- HY-121091
-
-
- HY-P1308
-
-
- HY-152524
-
|
|
Androgen Receptor
|
Cancer
|
|
Androgen receptor antagonist 7 is an effective androgen receptor (AR) antagonist with an IC50 value of 1.18 µM. Androgen receptor antagonist 7 has biological activity in vitro and inhibits the expression of AR target in a time and dose dependent manner with an GI50 value of 7.9 µM .
|
-
- HY-153700
-
|
|
Estrogen Receptor/ERR
|
Endocrinology
|
|
Estrogen receptor modulator 8 (compound 4) is an orally active inhibitor of Estrogen Receptor/ERR α (IC50=0.437 nM, MCF-7 cells). Estrogen receptor modulator 8 inhibits MCF-7 cells proliferation with an IC50 value of 0.1 nM .
|
-
- HY-170903
-
|
|
GABA Receptor
|
Neurological Disease
|
|
GABAA receptor modulator-3 (compound 3b) is a positive allosteric modulator (PAM). GABAA receptor modulator-3 inhibits α1β3γ2 GABAAR at peak and steady state currents with IC50s of 671 and 64 μM, respectively .
|
-
- HY-116380
-
-
- HY-132217
-
|
|
Cannabinoid Receptor
|
Neurological Disease
|
|
CB2 receptor agonist 2 is a potent and selective agonist for the CB2 (cannabinoid type 2) receptor with a Ki of 8.5 nM. CB2 receptor agonist 2 has high affinity and selectivity for CB2 .
|
-
- HY-153815
-
|
|
GLP Receptor
|
Metabolic Disease
|
|
GLP-1 receptor agonist 11 (compound 3) is an agonist of GLP Receptor. GLP-1 receptor agonist 11 can be used in the study of diseases such as diabetes and non-alc. fatty liver disease .
|
-
- HY-129946
-
-
- HY-114017
-
-
- HY-148179
-
-
- HY-145106
-
-
- HY-U00429
-
-
- HY-162787
-
|
|
Adenosine Receptor
|
Cancer
|
|
Adenosine receptor antagonist 5 (Compound 39) is a selective antagonist for human adenosine A3 receptor (hA3R) with Ki of 12 nM. Adenosine receptor antagonist 5 inhibits IB-MECA (HY-13591)-induced cAMP accumulation in NCI-H1792 cell, inhibits the proliferation of cancer cell LK-2 and NCI-H1792. Adenosine receptor antagonist 5 exhibits a fast metabolic rate in human liver microsomes .
|
-
- HY-115968
-
|
|
Dopamine Receptor
|
Neurological Disease
|
|
Dopamine D3 receptor ligand-4 (compound 6) is a potent and selective dopamine D3 receptor ligand, with a Ki of 0.5 nM. Dopamine D3 receptor ligand-4 shows high level of selectivity for D3 over D2 (Ki=7.43 nM) .
|
-
- HY-146517
-
|
|
Orexin Receptor (OX Receptor)
|
Neurological Disease
|
|
Orexin receptor antagonist 4 is potent and selective orexin 2 receptor (OX2R) antagonist with an IC50 of 4.27 nM. Orexin receptor antagonist 4 is 61-fold selective for the OX2R over the OX1R (IC50 of 295 nM) (WO2018206959A1; example 1) .
|
-
- HY-173030
-
|
|
Opioid Receptor
|
Neurological Disease
|
|
Opioid receptor agonist 1 (Compound 2638-28) is the orally active agonist for opioid receptor that exhibits good affinity to MOR, DOR and KOR with Ki of 5, 24 and 212 nM, respectively. Opioid receptor agonist 1 exhibits analgesic activity in mouse warm water tail flick models and acetic acid writhing models .
|
-
- HY-114025
-
-
- HY-156830
-
-
- HY-W823500
-
|
|
GLP Receptor
|
Metabolic Disease
|
|
GLP-1 Receptor modulator 1 (Compound 7) is a potent GLP-1 receptor positive allosteric modulator. GLP-1 Receptor modulator 1 can be used for the research of obesity and type 2 diabetes .
|
-
- HY-130992
-
|
|
Androgen Receptor
Ligands for Target Protein for PROTAC
|
Cancer
|
|
Androgen receptor antagonist 1 is an orally available full androgen receptor (AR) antagonist with an IC50 of 59 nM . Androgen receptor antagonist 1 (Compound 6) can be used in the synthesis of PROTAC AR degraders, which results 24% and 47 % AR protein degradation in LNCaP cells at 1 μM and 10 μM, respectively .
|
-
- HY-154980
-
|
|
GPR52
|
Neurological Disease
|
|
GPR52 receptor modulator 1 (Procedure 1) is a GPR52 receptor modulator with the potential to study neuropsychiatric diseases .
|
-
- HY-112451
-
-
- HY-112455
-
-
- HY-148076
-
|
|
Adenosine Receptor
|
Cancer
|
|
A2A receptor antagonist 3 (Example 92) is an adenosine A2a receptor antagonist with a Ki of 0.4 nM. A2A receptor antagonist 3 also binds to A2b, A1 and A3 receptor with Kis of 37, 107 and 1467 nM, respectively .
|
-
- HY-139680
-
|
|
Dopamine Receptor
|
Neurological Disease
|
|
Dopamine D3 receptor antagonist-1 is a dopamine D3 receptor-selective or multitarget bitopic ligand (Ki = 1.58 nM) potentially useful for central nervous system disorders.
|
-
- HY-139681
-
|
|
Dopamine Receptor
|
Neurological Disease
|
|
Dopamine D3 receptor antagonist-2 is a dopamine D3 receptor-selective (Ki = 2.16 nM) or multitarget bitopic ligand potentially useful for central nervous system disorders.
|
-
- HY-128132
-
|
|
Complement System
|
Inflammation/Immunology
|
|
C3a receptor agonist 1 (compound benzeneacetamide) is a potent C3a receptor agonist. C3a receptor agonist 1 has the potential for the research of acute inflammation .
|
-
- HY-119733
-
|
|
Opioid Receptor
|
Neurological Disease
|
|
BU09059 is a potent and selective Kappa-opioid receptor antagonist with a pA2 of 8.62. BU09059 has nanomolar affinity for the κ-receptor, with 15-fold and 616-fold selectivity over μ- and δ-receptors, respectively. BU09059 significantly blocks U50488 (HY-15997B)-induced antinociception .
|
-
- HY-119010
-
-
- HY-119088
-
|
|
Estrogen Receptor/ERR
|
Others
|
|
Estrogen receptor modulator 12 (compound 1a-(R)) is a selective estrogen receptor modulator with estrogen agonist and antagonist activities in in vivo models. Estrogen receptor modulator 12 exhibits antagonist effects on the uterus and estrogen agonist activities on bone, plasma lipids, hot flashes, and vagina in in vivo models, and is a potential compound for suppressing postmenopausal symptoms.
|
-
- HY-137882
-
-
- HY-155320
-
|
|
Opioid Receptor
|
Neurological Disease
|
|
Mu opioid receptor antagonist 7 (compound 24) is a potent and CNS permeable antagonist of µOR (µ-opioid receptor), with an IC50 of 29 ± 3.0 nM. Mu opioid receptor antagonist 7 can be used for the research of pain and opioid use disorder .
|
-
- HY-144606
-
|
|
Opioid Receptor
|
Neurological Disease
|
|
Mu opioid receptor antagonist 1 (compound 19) is a selective and orally active μ opioid receptor (MOR) ligand with an Ki value of 0.58 nM and an EC50 of 1.15 nM. Orally administrating with Mu opioid receptor antagonist 1 increases intestinal motility during morphine-induced constipation. Mu opioid receptor antagonist 1 can be used for researching opioid-induced constipation (OIC) .
|
-
- HY-170511
-
|
|
GLP Receptor
Potassium Channel
|
Metabolic Disease
|
|
GLP-1 receptor agonist 15 (Example 4) is a GLP receptor agonist with an EC50 of 0.74 nM. The IC50 for the hERG potassium ion channel is 10.1 μM. GLP-1 receptor agonist 15 can be used for research in the field of diabetes .
|
-
- HY-P4190
-
|
|
GnRH Receptor
|
Endocrinology
|
|
FSH receptor-binding inhibitor fragment(bi-10) is a potent FSH antagonist. FSH receptor-binding inhibitor fragment(bi-10) blocks the binding of FSH to FSHR, and alteres FSH action at the receptor level. FSH receptor-binding inhibitor fragment(bi-10) results in the suppression of ovulation and causes follicular atresia of mice. FSH receptor-binding inhibitor fragment(bi-10) has the potential for utilizing to restrain the carcinogenesis of ovarian cancer by down-regulating overexpression of FSHR and ERβ in the ovaries .
|
-
- HY-168338
-
|
|
Cannabinoid Receptor
Caspase
|
Cancer
|
|
CB2 receptor agonist 8 (Compound 17) is an agonist for cannabinoid receptor 2 (CB2 receptor). CB2 receptor agonist 8 exhibits cytotoxicity in cells U87, RPMI 8226, HL-60, and L929 with IC50s of 91.03, 16.29, 23.51 and 564.6 μM, respectively. CB2 receptor agonist 8 activates caspase 3/7, increases the expressions of pro-apoptotic genes BAX, BAD, BIM and tumor suppressor genes p53, and induces apoptosis in U87. CB2 receptor agonist 8 inhibits the migration of U87 .
|
-
- HY-103513
-
|
|
GABA Receptor
|
Others
|
|
GABAA receptor agent 2 (compound 13) is a compound used to study the structure and orthosteric ligand binding of GABA(A) receptors. The relevant model of GABAA receptor agent 2 can be used to understand the details of orthosteric ligand binding, and a detailed binding mode hypothesis was created through structure-activity relationships with two homologous series of orthosteric GABA(A)R antagonists.
|
-
- HY-150068
-
-
- HY-112679
-
|
|
GCGR
|
Others
|
|
GLP-1 receptor agonist 2 is a glucagon-like peptide-1 receptor (GLP-1R) agonist.
|
-
- HY-W009456
-
-
- HY-155481
-
|
|
Cannabinoid Receptor
|
Neurological Disease
|
|
CB2 receptor antagonist 3 (compound (S)-1) is an inverse agonist of the cannabinoid receptor CB2R with Kd=39 nM. CB2 receptor antagonist 3 can be used as a tool to synthesize a variety of CB2R probes .
|
-
- HY-168734
-
|
|
Cannabinoid Receptor
|
Inflammation/Immunology
|
|
CB2 receptor agonist 9 (Compound 33) is an orally active agonist for cannabinoid receptor 2 (CB2 receptor) with an EC50 of 16.2 nM. CB2 receptor agonist 9 inhibits the expression of TNF-α, IL-1β and IL-6, exhibits anti-inflammatory efficacy in DDS (HY-116282)-induced mouse acute colitis model .
|
-
- HY-148526
-
|
|
Adrenergic Receptor
mAChR
|
Metabolic Disease
|
|
β2AR/M3-receptor agonist-1 (example 9) is a potent β2AR and M3 receptor agonist. β2AR/M3-receptor agonist-1 shows M3 receptor affinity with a pIC50 value of 9.3. β2AR/M3-receptor agonist-1 has the potential for the research of respiratory tract disorders .
|
-
- HY-118259
-
-
- HY-14160
-
-
- HY-155147
-
-
- HY-160180
-
-
- HY-160178
-
-
- HY-106199
-
|
|
Adenosine Receptor
|
Neurological Disease
Inflammation/Immunology
|
|
Adenosine A1 receptor activator T62 is an allosteric enhancer of adenosine A1 receptor. Adenosine A1 receptor activator T62 produces antinociception in animal models of acute pain and also reduces hypersensitivity in models of inflammatory and nerve-injury pain .
|
-
- HY-145393
-
|
|
5-HT Receptor
|
Neurological Disease
|
|
5-HT2A receptor agonist-1 is a 5-HT2A receptor agonist with the EC50 of 5.54 nM. 5-HT2A receptor agonist-1 can be used for the research of mood disorders .
|
-
- HY-P5506
-
|
|
Complement System
|
Others
|
|
C5a Receptor agonist, W5Cha (Peptide 1) is a selective complement C5a receptor (C5aR) agonist (EC50=0.2 μM), a hexapeptide derived from the C-terminus of C5a with specific amino acid modifications. C5a Receptor agonist, W5Cha is able to interact with the Arg-206 site of the C5a receptor through its C-terminal arginine, thereby activating the receptor .
|
-
- HY-135482
-
|
|
GABA Receptor
|
Neurological Disease
|
|
GABAA receptor agent 2 TFA is a potent and high-affinity GABAA receptor antagonist with an IC50 of 24 nM (human α1β2γ2 GABAA-expressing tsA201 cells) and a Ki of 28 nM (rat GABAA receptors). GABAA receptor agent 2 TFA is inactive against four human GABA transporters (hGAT-1, hBGT-1, hGAT-2, and hGAT-3) .
|
-
- HY-10815
-
|
|
Sigma Receptor
Apoptosis
|
Neurological Disease
Cancer
|
|
σ1 Receptor antagonist-1 is a highly potent and selective sigma 1 receptor antagonist (pKi=10.28). σ1 Receptor antagonist-1 inhibits cell growth, arrests cell cycle at G0/G1 phase and induces apoptosis of MCF-7/ADR cells .
|
-
- HY-121094
-
|
|
Estrogen Receptor/ERR
|
Cancer
|
|
Androgen receptor allosteric antagonist 1(compound D36)is a a llosteric, competitive androgen receptor (AR) antagonist with the Ki of 9 μM. Androgen receptor allosteric antagonist 1 inhibits R1881-mediated transcription and proliferation and can be used for study of prostate cancer .
|
-
- HY-P1085
-
|
|
EGFR
|
Cancer
|
|
Epidermal Growth Factor Receptor Peptide (985-996) is an amino acid peptide fragment derived from positions 985-996 in epidermal growth factor receptor (EGFR) .
|
-
- HY-163091
-
-
- HY-W141876
-
|
|
Bacterial
|
Others
|
|
DL-2-Aminopimelic Acid is a weak agonist of glutamate receptors and also reduces the sensitivity of leech glutamate receptors to glutamate .
|
-
- HY-151876
-
|
|
Glucocorticoid Receptor
NF-κB
AP-1
|
Inflammation/Immunology
|
|
Glucocorticoid receptor modulator 1 is a highly potent and orally active non-steroidal selective glucocorticoid receptor modulator with an IC50 value of 9 nM and 130 nM for NF-κB and AP-1, respectively. Glucocorticoid receptor modulator 1 can effectively reduce the expression of inflammatory factors IL-6, IL-1β, TNF-α, also can relieve dermatitis in mice .
|
-
- HY-145257
-
|
|
GABA Receptor
|
Neurological Disease
|
|
GABAA receptor agent 5 (compound 018) is a potent γ-GABAAR antagonist with an Ki of 0.020 µM. GABAA receptor agent 5 shows γ-GABAAR antagonist activity with low cellular membrane permeability .
|
-
- HY-168141
-
|
|
Androgen Receptor
|
Cancer
|
|
Androgen receptor antagonist 11 (compund N29) is a derivative of the androgen receptor (AR) antagonist M17-B15, and is a selective and orally active AR antagonist (IC50=18 nM). .
|
-
- HY-148198
-
-
- HY-162951
-
|
|
P2X Receptor
|
Cancer
|
|
P2X7 receptor antagonist-5 (compund 13a) is a potent, orally active and long-lasting P2X7 receptor antagonist .
|
-
- HY-169786
-
|
|
5-HT Receptor
|
Neurological Disease
|
|
5-HT2A receptor agonist-5 (compound I-3) is a potent 5-HT2A receptor agonist with a Ki value of 0.017 µM. 5-HT2A receptor agonist-5 shows antidepressant activity .
|
-
- HY-125819
-
|
|
Sigma Receptor
|
Neurological Disease
|
|
Sigma-1 receptor antagonist 2 is a potent and selective sigma 1 receptor (σ1 R) antagonist with Kis of 3.88 and 1288 nM for σ1 and σ2 receptor, respectively .
|
-
- HY-156830A
-
|
|
G protein-coupled Bile Acid Receptor 1
|
Metabolic Disease
|
|
(4′R)-TGR5 Receptor Agonist 4 is the R enantiomer of TGR5 Receptor Agonist 4 (HY-156830). TGR5 Receptor Agonist 4 is an agonist of Bile Acid Receptor (TGR5), with EC50 for hTGR5 and mTGR5 of 2 nM and 3 nM, respectively. TGR5 Receptor Agonist 4 plays important roles in hypoglycemic and weight loss .
|
-
- HY-19733
-
|
ITI-007 tosylate
|
5-HT Receptor
Dopamine Receptor
|
Neurological Disease
Cancer
|
|
Lumateperone (ITI-007) tosylate is a 5-HT2A receptor antagonist (Ki = 0.54 nM), a partial agonist of presynaptic D2 receptors and an antagonist of postsynaptic D2 receptors (Ki = 32 nM), and a dopamine D1 receptor modulator. Lumateperone tosylate has anticancer activity and can also be used in studies of psychiatric disorders such as schizophrenia .
|
-
- HY-148115
-
|
|
LPL Receptor
|
Inflammation/Immunology
|
|
S1p receptor agonist 2 (compound 1) is an agonist of S1P5 receptor, exhibits selectivity over the S1P1 and/or S1P3 receptors. S1p receptor agonist 2 can be used for endogenous SIP signaling system research, and alleviating or preventing CNS disorders research, such as neurodegenerative disorders .
|
-
- HY-156239
-
-
- HY-129657
-
|
|
GCGR
|
Metabolic Disease
|
|
GLP-1 receptor agonist 4 is a glucagon-like peptide-1 receptor (GLP-1R) agonist extracted from patent WO2009111700A2, compound 87, has an EC50 of 64.5 nM. GLP-1 receptor agonist 4 can be used in the research for treatment of diabetes .
|
-
- HY-136459
-
|
|
iGluR
|
Neurological Disease
|
|
NMDA receptor antagonist 2 is a potent and orally active NR2B subtype-selective NMDA antagonist with an IC50 and a Ki of 1.0 nM and 0.88 nM, respectively. NMDA receptor antagonist 2 is used for the study of neuropathic pain and Parkinson’s disease .
|
-
- HY-17637
-
|
ITI-007
|
Dopamine Receptor
5-HT Receptor
|
Neurological Disease
Cancer
|
|
Lumateperone (ITI-007) is an orally active 5-HT2A receptor antagonist (Ki = 0.54 nM), a partial agonist of presynaptic D2 receptors and an antagonist of postsynaptic D2 receptors (Ki = 32 nM), and a dopamine D1 receptor modulator. Lumateperone has anticancer activity and can also be used for the study of schizophrenia and bipolar depression .
|
-
- HY-169859
-
|
|
Prostaglandin Receptor
Interleukin Related
|
Inflammation/Immunology
Cancer
|
|
EP4 receptor antagonist 7 (Compound 14) is an antagonist of the prostaglandin E2 (PGE2) receptor subtype EP4 with an IC50 value of 1.1 nM. EP4 receptor antagonist 7 inhibits PGE2-induced β-arrestin recruitment in HEK293 cells with an IC50 value of 0.9 nM. EP4 receptor antagonist 7 decreases PGE2-induced expression of mRNA encoding IL-4, macrophage mannose receptor 1 (Mrc1), chitinase-like protein 3 (Chil3), chemokine (C-X-C) motif ligand 1 (Cxcl1), triggering receptor expressed on myeloid cells 2 (Trem2), and arginase-1 (Arg1), in RAW 264.7 macrophages. EP4 receptor antagonist 7 combined with an anti-PD-1 antibody inhibits tumor growth and increases infiltration of CD 8+ T cells into tumors in a CT26 murine colon cancer model .
|
-
- HY-P1308A
-
-
- HY-P10203
-
|
|
Opioid Receptor
|
Inflammation/Immunology
|
|
μ/κ/δ opioid receptor agonist 1 is a μ opioid receptor (MOR), κ opioid receptor (KOR), and δ opioid receptor (DOR) agonist. μ/κ/δ opioid receptor agonist 1 produces a strong and long-lasting analgesic effect through peripheral MOR and KOR in the tail-flick test .
|
-
- HY-153476
-
|
|
GCGR
|
Metabolic Disease
|
|
GIP/GLP-1 dual receptor agonist-1 (compound 4) is a GIP/GLP-1 receptor agonist. GIP/GLP-1 dual receptor agonist-1 can be used in the research of metabolic disorders and fatty liver diseases, including nonalcoholic steatohepatitis (NASH) and nonalcoholic fatty liver disease (NAFLD) .
|
-
- HY-163394
-
|
|
Cannabinoid Receptor
|
Neurological Disease
Inflammation/Immunology
|
|
CB2 receptor agonist 6 (compound 70) is an agonist of CB2R, with EC50 of 162 nM. The IC50 values of CB2 receptor agonist 6 are 4.83 μM for CB1R and 0.88 μM for CB2R.
CB2 receptor agonist 6 is a neuroprotective agent that can be used for the reseach of neurological disease .
|
-
- HY-D2280
-
|
|
HDAC
Estrogen Receptor/ERR
|
Others
|
|
Estrogen receptor β/HDAC probe 1 (compound P1) is a near-infrared fluorescent probe that dual-targets the estrogen receptor (Estrogen Receptor/ERR) β/histone deacetylase HDAC .
|
-
- HY-146272
-
|
|
Vasopressin Receptor
|
Metabolic Disease
|
|
Vasopressin V2 receptor antagonist 1 (Compound 4g) is a vasopressin V2 receptor (V2R) antagonist with a Ki of 3.8 nM. Vasopressin V2 receptor antagonist 1 can be used for autosomal dominant polycystic kidney disease (ADPKD) research .
|
-
- HY-146588
-
|
|
iGluR
|
Neurological Disease
|
|
NMDA receptor antagonist 4 (IIc) is a uncompetitive, voltage-dependent, orally active NMDAR blocker, with an IC50 of 1.93 µM. NMDA receptor antagonist 4 shows a positive predicted blood-brain-barrier (BBB) permeability, and can be studied in Alzheimer's disease .
|
-
- HY-153964
-
|
|
Oxytocin Receptor
|
Cardiovascular Disease
|
|
PF-06478939 is a non-brain-penetrating peptide that is an agonist at oxytocin (OT) receptor and vasopressin receptor with EC50 values of 0.01 nM and 0.078 nM, respectively .
|
-
- HY-124463
-
-
- HY-P1276
-
|
Neurokinin-2 receptor antagonist
|
Neurokinin Receptor
|
Endocrinology
|
|
Men 10376 is a selective tachykinin NK-2 receptor antagonist, with a Ki of 4.4 μM for rat small intestine NK-2 receptor.
|
-
- HY-125821
-
|
|
Sigma Receptor
|
Neurological Disease
|
|
Sigma‑1 receptor antagonist 1 (compound 137) is a potent and selective sigma-1 receptor (σ1R) antagonist, with a high binding affinity to σ1R receptor (Ki = 1.06 nM). Sigma‑1 receptor antagonist 1 exhibits antineuropathic pain activity and acts as a promising agent for the treatment of neuropathic pain .
|
-
- HY-153912
-
|
|
5-HT Receptor
|
Others
|
|
5-HT2A receptor agonist-3 is the most selective agonist for the human 5-HT2A receptor yet discovered, with a Ki of 2.5 nM, and with 124-fold selectivity for 5-HT2A over the structurally similar 5-HT2C receptor .
|
-
- HY-153964A
-
|
|
Oxytocin Receptor
|
Cardiovascular Disease
|
|
PF-06478939 TFA is a non-brain-penetrating peptide that is an agonist at oxytocin (OT) receptor and vasopressin receptor with EC50 values of 0.01 nM and 0.078 nM, respectively .
|
-
- HY-19950
-
-
- HY-164005
-
-
- HY-150693
-
|
|
Estrogen Receptor/ERR
|
Cancer
|
|
Estrogen receptor β antagonist 2 is a potent and selective estrogen receptor β (ERβ) antagonist with IC50s of 109.10, 0.63 µM for Erα and Erβ, respectively .
|
-
- HY-162394
-
|
|
Vasopressin Receptor
|
Metabolic Disease
|
|
Vasopressin V2 receptor antagonist 2 (Compound 33) is an antagonist of the arginine vasopressin V2 receptor (V2R) with a Ki value of 6.2 nM. Vasopressin V2 receptor antagonist 2 can effectively reduce cAMP levels, thereby inhibiting the growth of renal cysts[1].
|
-
- HY-155417
-
|
|
ERK
Orphan Receptor
|
Neurological Disease
|
|
GPR34 receptor antagonist 3 (Compound 5e) is a class of GRP34 antagonists, IC50 is 0.680?μM. GPR34 receptor antagonist 3 inhibited ERK1/2 phosphorylation induced by lysophosphatidylserine in a dose-dependent way without obvious cytotoxicity. GPR34 receptor antagonist 3 shows antisensory activity in mouse neuropathic pain model .
|
-
- HY-125820
-
|
|
Sigma Receptor
Potassium Channel
|
Neurological Disease
|
|
Sigma-1 receptor antagonist 3 (compound135) is a potent and selective Sigma-1 (σ1) receptor antagonist with a Ki of 1.14 nM. Sigma-1 receptor antagonist 3 inhibits Human Ether-a-go-go-Related Gene (hERG) with an IC50 of 1.54 μM. Sigma-1 receptor antagonist 3 has the potential for the neuropathic pain .
|
-
- HY-148436
-
-
- HY-170516
-
-
- HY-159848
-
-
- HY-144672
-
-
- HY-103360A
-
|
UCB35625
|
CCR
|
Inflammation/Immunology
|
|
cis-J-113863 is a competitive chemokine receptor 1 (CCR1) antagonist, with IC50 values of 0.9 and 5.8 nM for human and mouse CCR1 receptors, respectively .
|
-
- HY-W095200
-
-
- HY-118609
-
-
- HY-148558
-
|
|
P2X Receptor
|
Neurological Disease
|
|
P2X7 receptor antagonist-3 is a potent P2X7 receptor antagonist with P2X7R IC50 values of 4.2 nM in humans and 6.8 nM in rats .
|
-
- HY-164774
-
-
- HY-U00321
-
-
- HY-123829
-
-
- HY-162759
-
|
|
Sigma Receptor
|
Neurological Disease
|
|
Sigma-1 receptor antagonist 6 (Compound 12) is an antagonist of the Sigma-1 receptor (σ1R). Sigma-1 receptor antagonist 6 exerts a robust antiallodynic effect by antagonizing σ1R. Sigma-1 receptor antagonist 6 can be used in neuropathic pain animal models to alleviate mechanical allodynia induced by paclitaxel (HY-B0015) .
|
-
- HY-147810
-
|
|
5-HT Receptor
|
Neurological Disease
|
|
5-HT7 receptor ligand 1 (Compound 5c) is a 5-HT7 receptor ligand with a Ki of 8 nM. 5-HT7 receptor ligand 1 is not hepatotoxic and exhibit moderate potential interaction with other agents metabolized by CYP3A4 or CYP2D6 .
|
-
- HY-P3852
-
|
SPR393-407
|
Neurokinin Receptor
|
Neurological Disease
Inflammation/Immunology
|
|
Neurokinin Receptor (393-407), rat (SPR393–407) is a rat neurokinin 1 receptor (NK1R) fragment. NK1R is rapidly internalized by endocytosis and recycled to the plasma membrane when binding to substance P (SP). Neurokinin Receptor (393-407), rat can be used in the research of neurogenic inflammation .
|
-
- HY-P1758
-
|
IRRP1
|
IFNAR
|
Infection
|
|
IFN-α Receptor Recognition Peptide 1 is a peptide of IFN-α associated with receptor interactions .
|
-
- HY-13724
-
-
- HY-19320
-
-
- HY-10658
-
-
- HY-138695
-
-
- HY-P1536
-
-
- HY-156339
-
|
|
GABA Receptor
|
Others
|
|
GABA receptor Antagonist 1 (compound 7w) inhibits Px RDL1 GABAR with an IC50 value of 7.08 nmol/L. GABA receptor Antagonist 1 shows insecticide activity against P. xylostella, S. frugiperda, S. exigua, and S. litura, with LC50 of 0.09, 0.84, 0.87, and 0.68 mg/L respectively. GABA receptor Antagonist 1 shows a medium toxicity to honeybee (48 h, ID50 = 2.22 μg/adult), and low toxicity to zebrafish (LC50: 42.4 mg/L) .
|
-
- HY-148524
-
|
|
mAChR
Adrenergic Receptor
|
Cardiovascular Disease
|
|
β2AR/M-receptor agonist-1 (example 131) is a muscarinic antagonist and β2 adrenoceptor agonist (MABA). β2AR/M-receptor agonist-1 shows potency to β2 adrenoceptor with an EC50 value of 9.2 nM. β2AR/M-receptor agonist-1 also has potency to muscarinic receptor with a Ki value of 30.2 nM. β2AR/M-receptor agonist-1 shows MABA potency with an EC50 value of 4.0 nM .
|
-
- HY-153816A
-
-
- HY-P1868A
-
|
DGEA peptide TFA
|
Integrin
|
Others
|
|
α2β1 Integrin Ligand Peptide TFA interacts with the α2β1 integrin receptor on the cell membrane and mediates extracellular signals into cells. It is a potential antagonist of collagen receptors .
|
-
- HY-102024
-
-
- HY-129648
-
-
- HY-129357
-
|
|
Cholecystokinin Receptor
|
Metabolic Disease
|
|
CCK-B Receptor Antagonist 2, compound 15b, is a potent and orally active Gastrin/CCK-B antagonist with an IC50 value of 0.43 nM. CCK-B Receptor Antagonist 2 also inhibits gastrin/CCK-A activity with an IC50 of 1.82 μM .
|
-
- HY-143267
-
-
- HY-115833
-
|
|
Histamine Receptor
|
Cancer
|
|
Histamine H4 receptor antagonist-2 serves as a potent activator of p53, demonstrating significant antitumor efficacy.
|
-
- HY-158262
-
|
|
Bradykinin Receptor
|
Neurological Disease
|
|
Bradykinin B1 receptor antagonist 1 (compound 6B) is a potent and cross the blood-brain barrier bradykinin B1 antagonist. Bradykinin B1 receptor antagonist 1 has the potential for the research of pain .
|
-
- HY-138996
-
|
|
GCGR
|
Metabolic Disease
|
|
GLP-1 receptor agonist 8 is a potent agonist of GLP-1 R. GLP-1 receptor agonist 8 has the potential for the research of diabetes, obesity, and nonalcoholic fatty liver disease (NAFLD) (extracted from patent WO2019239319A1, compound 17) .
|
-
- HY-120468
-
-
- HY-121906
-
-
- HY-103551
-
|
|
mGluR
|
Neurological Disease
|
|
(±)-LY395756 is an agonist of mGlu2 receptor and an antagonist of mGlu3 receptor. (±)-LY395756 can distinguish the native mGlu2 and mGlu3 receptors .
|
-
- HY-101704
-
-
- HY-P10175
-
|
|
Opioid Receptor
|
Neurological Disease
|
|
Acetalin-1 (Ac-RFMWMK-NH2), a hexapeptide, is a μ opioid receptor antagonist with high affinity for μ and κ3 opioid receptor, weak affinity for κ1 receptors and no affinity for κ2 receptors .
|
-
- HY-144603
-
-
- HY-146453
-
|
|
G protein-coupled Bile Acid Receptor 1
|
Metabolic Disease
|
|
TGR5 Receptor Agonist 3 (Compound 19) is a soft-agent G-protein-coupled bile acid receptor 1 (GPBAR1, TGR5) agonist with reduced gallbladder-filling effects (favorable gallbladder safety), with EC50s of 16.4 and 209 nM for hTGR5 and mTGR5, respectively.
|
-
- HY-145370
-
|
|
iGluR
|
Neurological Disease
|
|
GluN2B receptor modulator-1 is a selective GluN2B negative allosteric modulator with an IC50 value of 31 nM.
|
-
- HY-50713
-
|
|
CaSR
|
Others
|
|
Calcium-Sensing receptor antagonist I is a click chemistry reagent, it contains an Alkyne group and can undergo copper-catalyzed azide-alkyne cycloaddition (CuAAc) with molecules containing Azide groups.
|
-
- HY-145841
-
|
|
5-HT Receptor
|
Cardiovascular Disease
|
|
5-HT2A receptor agonist-2 is a highly potent serotonin 5-HT2 receptor agonists. 5-HT2A receptor agonist-2 inspires 5-HT2A, 5-HT2B, and 5-HT2C with EC50 values of 1.7, 0.58, and 0.50 nM, respectively .
|
-
- HY-110047
-
-
- HY-149645
-
|
|
Cannabinoid Receptor
|
Others
|
|
CB2 receptor antagonist 2 (compound 39) is a potent antagonist of CB2 with an IC50 value of 0.33 μM. CB2 receptor antagonist 2 has strong interactions with L17, W6.48, V6.51, and C7.42 .
|
-
- HY-156095
-
|
|
Wnt
|
Cancer
|
|
F7H is a Frizzled receptor FZD7 antagonist (IC50: 1.25 μM). Frizzled receptors (FZDs) influence Wnt signaling, mediating embryonic development and tissue homeostasis. F7H is a potent ligand for the FZD7 transmembrane domain (TMD) .
|
-
- HY-12709
-
-
- HY-119985
-
|
Z 1170
|
Adrenergic Receptor
|
Others
|
|
Broxaterol (Z 1170) is the an agonist of β2 adrenergic receptor that affects the smooth muscle receptors in the body. Broxaterol plays an important role in respiratory disease .
|
-
- HY-P10597
-
|
|
Angiotensin Receptor
|
Others
|
|
Angiotensin II type 1 receptor (181-187) is a 9-amino acid sequence of the second extracellular loop of angiotensin II (Ang II) in the renin-angiotensin system. Angiotensin II type 1 receptor (181-187) serves as the localization epitope of angiotensin II receptor autoantibodies (AT1RaAb) and is used to detect and quantify AT1RaAb levels in serum .
|
-
- HY-W580721A
-
|
|
Histamine Receptor
|
Others
|
|
4-Methylhistamine (hydrochloride) is a potent, high affinity H4 receptor agonist Ki of 7 nM. 4-Methylhistamine (hydrochloride) displays more than 100-fold selectivity over other human histamine receptor subtypes .
|
-
- HY-P1276A
-
|
Neurokinin-2 receptor antagonist TFA
|
Neurokinin Receptor
|
Endocrinology
|
|
Men 10376 TFA is a selective tachykinin NK-2 receptor antagonist, with a Ki of 4.4 μM for rat small intestine NK-2 receptor .
|
-
- HY-117040
-
|
Norbinaltorphimine; NorBNI
|
Opioid Receptor
|
Others
|
|
nor-Binaltorphimine is a selective antagonist of kappa-opioid receptor. nor-Binaltorphimine has a long-lasting effect in vivo .
|
-
- HY-101704A
-
|
H 409-22 isomer formic
|
Neurokinin Receptor
|
Neurological Disease
|
|
Y1 receptor antagonist 1 formic (H 409-22 isomer formic) is the formic salt form of Y1 receptor antagonist 1 (HY-101704). Y1 receptor antagonist 1 formic is a neuropeptide Y1 receptor antagonist.
|
-
- HY-P990867
-
|
|
Insulin Receptor
|
Others
|
|
Anti-CD220/Insulin Receptor Antibody (IR 83-22) is a kind of mouse IgG1 chimeric antibody, targeting to human CD220/Insulin Receptor. The recommend isotype control of Anti-CD220/Insulin Receptor Antibody (IR 83-22): Mouse IgG1 kappa, Isotype Control (HY-P99977).
|
-
- HY-P10006
-
|
|
Opioid Receptor
|
Neurological Disease
|
|
Leumorphin, human is a potent kappa opioid receptor (κ opioid receptor) agonist. Leumorphin, human inhibits the contraction of the myenteric plexus-longitudinal muscle preparation of the guinea pig ileum .
|
-
- HY-167842
-
-
- HY-44132
-
|
RS 42358-197
|
5-HT Receptor
|
Neurological Disease
|
|
Dehydro Palonosetron (RS 42358-197) is a potent, seslective and orally active 5-HT3 receptor antagonist. Dehydro Palonosetron has no effect on the activities of 5-HT1 receptors, 5-HT2 receptors or 5-HT4 receptors .
|
-
- HY-113537
-
-
- HY-103170
-
|
|
Adenosine Receptor
|
Others
|
|
LUF5834 is a selective A2B adenosine receptor (A2BR) partial agonist (EC50 = 12 nM). LUF5834 is also a partial A1/A2A adenosine receptor agonist (lacking selectivity) with Ki values of 2.6 and 28 nM, respectively .
|
-
- HY-P0320
-
|
|
Phosphatase
|
Others
|
|
EGF Receptor Substrate 2 (Phospho-Tyr5) acetate, a biologically active peptide, is a tyrosine phosphate substrate. EGF Receptor Substrate 2 (Phospho-Tyr5) acetate can be used to detect protein tyrosine phosphatases activity .
|
-
- HY-128040
-
-
- HY-P3748
-
|
|
Casein Kinase
|
Others
|
|
Casein Kinase II Receptor Peptide is a substrate for casein kinase II with an Km value of 500 µM. Casein Kinase II Substrate can be used for measure casein kinase II activity in crude enzyme preparations .
|
-
- HY-107603
-
|
|
iGluR
|
Neurological Disease
|
|
NS3763 is a selective and noncompetitive GLUK5 receptor antagonist with an IC50 of 1.6 µM. NS3763 does not show significant antagonistic properties on GLUK6, AMPA or NMDA receptors .
|
-
- HY-129656
-
|
|
GCGR
|
Metabolic Disease
|
|
GLP-1 receptor agonist 3 (compound (R)-4A-1) is a GLP-1 receptor agonist (WO2018109607A1), used for diabetes research. compound (S)-4A-1 shows EC50s of 1.1 nM and 13 nM in Clone H6 and Clone C6 cell lines assay, respectively .
|
-
- HY-145412
-
|
|
GCGR
|
Metabolic Disease
|
|
GLP-1 receptor agonist 7 is a potent agonist of glucagon-like peptide-1 (GLP-1). GLP-1 receptor agonist 7 has the potential for the research of GLP-1-associated diseases, disorders, and conditions including diabetes mellitus (extracted from patent WO2021219019A1, compound 130b) .
|
-
- HY-145611
-
-
- HY-W909173
-
|
|
Trace Amine-associated Receptor (TAAR)
Histamine Receptor
mAChR
|
Neurological Disease
|
|
TAAR1 agonist 2 (compound 30) is a full agonist of trace amine-associated receptor 1 (TAAR1) (pEC50=7.5). TAAR1 agonist 2 also exhibits agonist activity at H1 receptors and activates several members of the muscarinic acetylcholine receptor family, such as the M2 receptor (pEC50=5). TAAR1 agonist 2 can be used in the study of neuropsychiatric diseases .
|
-
- HY-101139B
-
|
XAC trihydrochloride
|
Adenosine Receptor
|
Neurological Disease
|
|
Xanthine amine congener trihydrochloride (XAC dihydrochloride) is a potent Adenosine A1 receptor and A2?receptor antagonist with IC50 values of 1.8 and 114 nM, respectively. Xanthine amine congener acts as a convulsant agent in mice model .
|
-
- HY-110303
-
|
XAC dihydrochloride
|
Adenosine Receptor
|
Neurological Disease
|
|
Xanthine amine congener dihydrochloride (XAC dihydrochloride) is a potent Adenosine A1 receptor and A2 receptor antagonist with IC50 values of 1.8 and 114 nM, respectively. Xanthine amine congener acts as a convulsant agent in mice model .
|
-
- HY-145466
-
|
|
P2X Receptor
|
Neurological Disease
|
|
EVT-401 (P2X7 receptor antagonist-1) is a purinergic P2X7 receptor antagonist. EVT-401 has efficacy of combating neuroinflammation .
|
-
- HY-50175A
-
-
- HY-50175
-
-
- HY-400356
-
|
|
ADC Linker
|
Cancer
|
|
Glucocorticoid receptor agonist-1 phosphate Gly-Glu (TFA) is a cleavable linker, that can be used to synthesize Antibody-Drug Conjugates (ADCs).
|
-
- HY-U00382
-
-
- HY-B1510S
-
-
- HY-P1776
-
|
|
Insulin Receptor
|
Metabolic Disease
|
|
[pTyr1146][pTyr1150][pTyr1151]Insulin Receptor (1142-1153) binds to insulin and can be used as insulin receptor tyrosine kinase substrates .
|
-
![[pTyr1146][pTyr1150][pTyr1151]Insulin Receptor (1142-1153)](//file.medchemexpress.com/product_pic/hy-p1776.gif)
- HY-112699
-
|
|
iGluR
|
Neurological Disease
|
|
AMPA receptor modulator-1 is a potent, orally active and selective AMPAR regulatory protein TARP γ-8 negative modulator with a pIC50 of 9.7, more selective over GluA1/γ-2 (pIC50=5) .
|
-
- HY-N7247
-
|
|
mAChR
|
Metabolic Disease
|
|
Thiochrome, a natural oxidation product and metabolite of thiamine, is a selective M4 muscarinic receptor of acetylcholine (ACh) affinity enhancer. Thiochrome has neutral cooperativity with ACh at M1 to M3 receptors .
|
-
- HY-145610
-
-
- HY-121867
-
-
- HY-111194
-
-
- HY-100920
-
-
- HY-P2057
-
-
- HY-170771
-
|
|
GABA Receptor
|
Neurological Disease
|
|
α5-GABAA receptor modulator 1 (Compound A-4) is a silencing allosteric modulator (SAM) specifically targeting the a5 subunit of the GABAA receptor, suitable for research into central nervous system (CNS) disorders .
|
-
- HY-148525
-
|
β2AR/M-receptor agonist-2
|
mAChR
Adrenergic Receptor
|
Cardiovascular Disease
Inflammation/Immunology
|
|
β2AR/M-receptor agonist-2 (compound 15) is a muscarinic antagonist and β2 adrenoceptor agonist (MABA). β2AR/M-receptor agonist-2 shows potency to β2 adrenoceptor with an EC50 value of 3.7 nM. β2AR/M-receptor agonist-2 also has potency to human cloned M3 receptor with a Ki value of 0.73 nM. β2AR/M-receptor agonist-2 is a potent bronchodilator, it can be used for the research of chronic obstructive pulmonary disease (COPD) .
|
-
- HY-159179
-
|
|
Integrin
|
Inflammation/Immunology
|
|
α4 integrin receptor antagonist 3 (Compound 11) is an orally active α4integrin receptor antagonist. α4 integrin receptor antagonist 3 can inhibit the adhesion of K562 cells mediated by the interaction between α4β1/VCAM-1 and α4β7/MAdCAM-1, with IC50 values of 130 nM and 2 nM, respectively. α4 integrin receptor antagonist 3 has the potential to be used in the study of dextran sulfate sodium (DSS) colitis mouse model .
|
-
- HY-11065A
-
|
|
GABA Receptor
|
Neurological Disease
|
|
(iodo-125)-CGP 71872 is a iodo-125-labeled CGP 71872 (GABABR1 receptor agonist),containing an azido group that can be photoactivated,and can be used to characterize GABAB receptors .
|
-
- HY-107557
-
|
|
Histamine Receptor
|
Neurological Disease
|
|
Proxyfan is a potent histamine H3 receptor antagonist with Ki values of 2.9 nM and 2.7 nM for rat and human H3 receptor, respectively. Proxyfan is over 1000-fold more potent at H3 receptors than other histamine receptors .
|
-
- HY-145553
-
-
- HY-100966
-
-
- HY-P0320B
-
|
|
Phosphatase
Biochemical Assay Reagents
|
Others
|
|
EGF Receptor Substrate 2 (Phospho-Tyr5) acetate, a biologically active peptide, is a tyrosine phosphate substrate. EGF Receptor Substrate 2 (Phospho-Tyr5) acetate can be used to detect protein tyrosine phosphatases activity .
|
-
- HY-P0320A
-
|
|
Phosphatase
Biochemical Assay Reagents
|
Others
|
|
EGF Receptor Substrate 2 (Phospho-Tyr5) acetate, a biologically active peptide, is a tyrosine phosphate substrate. EGF Receptor Substrate 2 (Phospho-Tyr5) acetate can be used to detect protein tyrosine phosphatases activity .
|
-
- HY-126123
-
|
|
iGluR
Potassium Channel
|
Neurological Disease
|
|
NR2B-selective NMDA receptor antagonist 1 (compound 29) is a potent antagonist of NR1/NR2B receptors, with IC50s of 0.05 μM, 0.73 μM, 2.4 μM to NR1/NR2B NMDA receptor, hERG, α1-AdR, respectivity. NR2B-selective NMDA receptor antagonist 1 exhibites efficient permeability across the blood–brain barrier .
|
-
- HY-100837
-
|
|
iGluR
|
Neurological Disease
|
|
5-Iodowillardiine is a potent and selective kainate receptor agonist. 5-Iodowillardiine is selective for kainate receptors composed of hGluR5 subunits .
|
-
- HY-149335
-
|
|
Sigma Receptor
Histamine Receptor
|
Neurological Disease
|
|
Sigma-1 receptor antagonist 5 (compound 12)，a 4-pyridylpiperidine derivative with analgesic activity，is an antagonist of sigma receptor (Ki=4.5 nM (σ1R)，10 nM (σ2R)) and histamine H3 (hH3R，Ki=7.7 nM，IC50=215 nM). Sigma-1 receptor antagonist 5 suppresses Capsaicin-induced nociception with antinociceptive activity and shows potent efficacy in nociceptive and neuropathic pain models .
|
-
- HY-107557A
-
|
|
Histamine Receptor
|
Neurological Disease
|
|
Proxyfan Oxalate is a potent histamine H3 receptor antagonist with Ki values of 2.9 nM and 2.7 nM for rat and human H3 receptor, respectively. Proxyfan Oxalate is over 1000-fold more potent at H3 receptors than other histamine receptors .
|
-
- HY-155481A
-
|
|
Cannabinoid Receptor
|
Others
|
|
CB2 receptor antagonist 4 (compound (R)-1) is a CB2R-selective inverse agonist with a Kd value of 39 nM .
|
-
- HY-19947
-
|
Glucagon receptor antagonists-4
|
GCGR
|
Metabolic Disease
|
|
PF-06291874 is a highly potent, non-peptide and orally active glucagon receptor antagonist. PF-06291874 is under the study for type 2 diabetes mellitus (T2DM) .
|
-
- HY-148325
-
|
|
nAChR
|
Neurological Disease
|
|
α7 Nicotinic receptor agonist-1 (Preparation 5) is an α7 nAChR agonist. α7 Nicotinic receptor agonist-1 can be used in studies of psychiatric disorders (such as schizophrenia, manic or hypomanic depression and anxiety disorders) and intellectual disorders (such as alzheimer's disease, learning deficits, cognitive deficits, attention deficits, memory loss, lewy body dementia and attention deficit hyperactivity disorder) .
|
-
- HY-105315
-
|
|
Prostaglandin Receptor
|
Endocrinology
|
|
AFP-07 is a derivative of 7, 7-difluoroprostacyclic and is a highly potent and selective prostacyclin receptor IP receptor agonist with a Ki value of 0.561 nM .
|
-
- HY-106957
-
|
|
Histamine Receptor
|
Inflammation/Immunology
|
|
Efletirizine (EFZ) is an orally active antihistamine with high selectivity and affinity to the H1-receptor. Efletirizine can be used for allergic disease research .
|
-
- HY-123249
-
|
|
GABA Receptor
|
Neurological Disease
|
|
HZ166 is a GABAA receptor subtype-selective benzodiazepine site agonist with preferential activity at α2- and α3-GABAA receptors. HZ166 shows anti-hyperalgesic effects . HZ166 is a click chemistry reagent, it contains an Alkyne group and can undergo copper-catalyzed azide-alkyne cycloaddition (CuAAc) with molecules containing Azide groups.
|
-
- HY-124534
-
-
- HY-120633A
-
-
- HY-124391
-
-
- HY-125101A
-
-
- HY-107559
-
|
|
Histamine Receptor
|
Neurological Disease
|
|
GT-2016 is a potent, selective, and brain penetrant histamine H3 receptor antagonist with a Ki of 43.8 nM. GT-2016 displays selectivity against H1 and H2 receptors, and has non-active against histamine methyltransferase .
|
-
- HY-112074A
-
|
HOE 440 hydrochloride
|
Adrenergic Receptor
|
Cardiovascular Disease
|
|
Tiamenidine hydrochloride (HOE 440 hydrochloride) is a centrally acting α1-adrenergic receptor antagonist with hypotensive activity. Tiamenidine hydrochloride regulates blood pressure levels by binding to α1 receptors. Tiamenidine hydrochloride can be used in the study of hypertension .
|
-
- HY-141865
-
|
|
Adenosine Receptor
|
Cancer
|
|
Adenosine receptor antagonist 1 is a A2aR-selective antagonist with an IC50 of 0.29 nM and displays 14-fold more selective for A2aR than A2bR.
|
-
- HY-W329175
-
|
SKF-104557
|
Dopamine Receptor
|
Neurological Disease
|
|
N-Despropyl Ropinirole (SKF-104557) is an active metabolite of the dopamine D2 receptor agonist Ropinirole (HY-B0623). N-Despropyl Ropinirole is a full agonist at human D2 and D3 receptors. N-Despropyl Ropinirole is a partial agonistof the hD4 receptor .
|
-
- HY-129293
-
|
|
Prostaglandin Receptor
|
Endocrinology
|
|
AFP-07 free acid is a derivative of 7, 7-difluoroprostacyclic and is a highly potent and selective prostacyclin receptor IP receptor agonist with a Ki value of 0.561 nM .
|
-
- HY-P3506
-
|
LY3437943
|
GCGR
GLP Receptor
|
Metabolic Disease
|
|
Retatrutide (LY3437943) is a triple agonist peptide of the glucagon receptor (GCGR), glucosedependent insulinotropic polypeptide receptor (GIPR), and glucagon-like peptide-1 receptor (GLP-1R). Retatrutide binds human GCGR, GIPR, and GLP-1R with EC50 values of 5.79, 0.0643 and 0.775 nM, respectively. Retatrutide can be used for the research of obesity .
|
-
- HY-P3506B
-
|
LY3437943 acetate
|
GCGR
GLP Receptor
|
Metabolic Disease
|
|
Retatrutide (LY3437943) acetate is a triple agonist peptide of the glucagon receptor (GCGR), glucosedependent insulinotropic polypeptide receptor (GIPR), and glucagon-like peptide-1 receptor (GLP-1R). Retatrutide acetate inhibits human GCGR, GIPR, and GLP-1R with EC50 values of 5.79, 0.0643 and 0.775 nM, respectively. Retatrutide acetate can be used for the research of obesity .
|
-
- HY-111669
-
CT1812
1 Publications Verification
Sigma-2 receptor antagonist 1
|
Sigma Receptor
|
Neurological Disease
|
|
CT1812 (Sigma-2 receptor antagonist 1) is an orally active and brain penetrant sigma-2 receptor antagonist with a Ki of 8.5 nM. CT1812 can be used for the research of Alzheimer’s disease .
|
-
- HY-116495
-
-
- HY-169822
-
-
- HY-152270
-
-
- HY-136969
-
-
- HY-146077
-
|
|
5-HT Receptor
|
Neurological Disease
|
|
5-HT6/5-HT2A receptor ligand-2 (compound 42) is a brain-penetrant dual 5-HT6/5-HT2A receptor antagonist, with a Ki of 25 nM and 32 nM, respectively. 5-HT6/5-HT2A receptor ligand-2 shows pro-cognitive properties .
|
-
- HY-146076
-
|
|
5-HT Receptor
|
Neurological Disease
|
|
5-HT6/5-HT2A receptor ligand-1 (compound 33) is a dual 5-HT6/5-HT2A receptor antagonist, with a Ki of 2 nM and 11 nM, respectively. 5-HT6/5-HT2A receptor ligand-1 has the potential for neurological and psychiatric disorders research .
|
-
- HY-107554
-
-
- HY-101078A
-
|
CMI 545 dihydrochloride
|
Dopamine Receptor
|
Neurological Disease
|
|
(±)-Epibatidine (CMI 545) dihydrochloride is an agonist of nicotinic with potent analgetic activity. (±)-Epibatidine (CMI 545) dihydrochloride is an alkaloid originally characterized from frog skin. (±)-Epibatidine (CMI 545) dihydrochloride have little or no activity at a variety of other central receptors, including opioid receptors, muscarinic receptors, adrenergic receptors, dopamine receptors, serotonin receptors, and gamma-aminobutyric acid receptors .
|
-
- HY-126044
-
|
|
Endogenous Metabolite
|
Metabolic Disease
|
|
6-Hydroxy bexarotene is the main circulating metabolite of bexarotene, found in rats, dogs, and humans. Compared to the parent compound, 6-hydroxy-bexarotene shows a significantly reduced ability to bind to retinoid receptors and exhibits very minimal activity in activating retinoic acid receptors .
|
-
- HY-P3506A
-
|
LY3437943 TFA
|
GLP Receptor
GCGR
|
Metabolic Disease
|
|
Retatrutide (LY3437943) TFA is a triple agonist peptide of the glucagon receptor (GCGR), glucosedependent insulinotropic polypeptide receptor (GIPR), and glucagon-like peptide-1 receptor (GLP-1R). Retatrutide TFA binds human GCGR, GIPR, and GLP-1R with EC50 values of 5.79, 0.0643 and 0.775 nM, respectively. Retatrutide TFA can be used for the research of obesity .
|
-
- HY-103188
-
|
|
Adenosine Receptor
|
Neurological Disease
|
|
PD81723 is an adenosine receptor binding enhancer. PD81723 enhances the inhibition of exogenous adenosine in a dose-dependent manner in hippocampal brain sections .
|
-
- HY-120928
-
-
- HY-12701A
-
|
U-99194A; PNU-99194A maleate; JPC-211 maleate
|
Dopamine Receptor
|
Neurological Disease
|
|
U-99194 maleate is a potent and selective Dopamine3 Receptor (D3 receptor) antagonist. U-99194 maleate also enhances prolactin secretion and striatal dopamine synthesis .
|
-
- HY-114550
-
|
|
iGluR
|
Neurological Disease
|
|
LY339434 is a potent and selective agonist for the hydrochloride receptor GluR5. LY339434 affects the rapid death of neurons through n-methyl-D-aspartate (NMDA) receptors .
|
-
- HY-117139
-
|
|
Cannabinoid Receptor
|
Neurological Disease
|
|
NESS 0327 is a cannabinoid antagonist with high selectivity for the cannabinoid CB1 receptor. NESS 0327 is more than 60,000-fold selective for the CB1 receptor .
|
-
- HY-170587
-
-
- HY-13221A
-
|
|
5-HT Receptor
|
Cardiovascular Disease
|
|
BRL 54443 (MALEATE) is a potent 5-HT1E/1F receptor agonist (Ki values are 1.1 nM and 0.7 nM respectively); displays > 30-fold selectivity over other 5-HT and dopamine receptors .
|
-
- HY-169139
-
-
- HY-156981
-
-
- HY-135270
-
-
- HY-118279
-
|
|
Sigma Receptor
|
Neurological Disease
|
|
KSCM-1 is a selective sigma-1 receptor ligand with a Ki of 27.5 nM. KSCM-1 shows more selective for sigma-1 over sigma-2, and shows no significant affinity at non-sigma receptors .
|
-
- HY-N7247R
-
|
|
mAChR
|
Metabolic Disease
|
|
Thiochrome (Standard) is the analytical standard of Thiochrome. This product is intended for research and analytical applications. Thiochrome, a natural oxidation product and metabolite of thiamine, is a selective M4 muscarinic receptor of acetylcholine (ACh) affinity enhancer. Thiochrome has neutral cooperativity with ACh at M1 to M3 receptors .
|
-
- HY-118958
-
|
Ro 23-3544
|
Leukotriene Receptor
|
Inflammation/Immunology
|
|
Ablukast (Ro 23-3544) is a specific and active leukotriene receptor antagonist. Ablukast effectively reduces LTC4- and antigen-induced bronchoconstriction . Ablukast is LTD4 receptor antagonist .
|
-
- HY-P3450
-
-
- HY-120523
-
|
|
iGluR
|
Neurological Disease
|
|
UBP646 is a potent GluN1/GluN2D receptors potentiator, and also potentiates the other three subtypes, GluN1/GluN2A, GluN1/GluN2B, and GluN1/GluN2C receptors .
|
-
- HY-107471
-
|
GP2a
|
Cannabinoid Receptor
|
Cancer
|
|
CB2 receptor agonist 3 is a robust and selective CB2 cannabinoid agonist with Kis of 7.6 and 900 nM for CB2 and CB1, respectively. CB2 receptor agonist 3 significantly increases P-ERK 1/2 expression in HL-60 cells .
|
-
- HY-P1016
-
|
|
Endothelin Receptor
|
Cardiovascular Disease
|
|
BQ-3020 is a selective endothelin receptor (ETB receptor) agonist that displaces [ 125I] ET-1 binding to ETB receptors, with an IC50 value of 0.2 nM. BQ-3020 elicits vasoconstriction in the rabbit pulmonary artery. BQ-3020 makes relaxation of the pig urinary bladder neck and can be used for cardiovascular disease research 1 2.
|
-
- HY-P1106A
-
|
|
CFTR
|
Cardiovascular Disease
|
|
K41498 TFA is a potent and highly selective CRF2 receptor antagonist with Ki values of 0.66 nM, 0.62 nM and 425 nM for human CRF2α, CRF2β and CRF1 receptors respectively. K41498 TFA is an analogues of antisauvagine-30 (aSvg-30), inhibits sauvagine-stimulated cAMP accumulation in hCRF2α- and hCRF2β-expressing cells. K41498 TFA can be used for hypotension study .
|
-
- HY-135329
-
|
|
mAChR
|
Neurological Disease
|
|
Solifenacin D5 hydrochloride is a deuterium labeled Solifenacin hydrochloride. Solifenacin hydrochloride is a muscarinic receptor antagonist with pKis of 7.6, 6.9 and 8.0 for M1, M2 and M3 receptors, respectively .
|
-
- HY-100547
-
|
|
iGluR
|
Neurological Disease
|
|
IEM-1754, a dicationic adamantane derivative, is a potent blocker of open channels of native ionotropic glutamate receptors including quisqualate-sensitive receptors in insect muscles, NMDAR in cultured rat cortical neurons, and AMPAR in freshly isolated hippocampal cells. IEM-1754 shows anticonvulsant potency in vivo .
|
-
- HY-137883
-
|
|
Drug-Linker Conjugates for ADC
|
Cancer
|
|
Glucocorticoid receptor agonist-1 phosphate Gly-Glu-Br is a drug-linker conjugate for ADC that can be used to synthesize ABBV-154, ABBV-927, ABBV-368 or their analogs .
|
-
- HY-101265
-
|
S1p receptor agonist 1
|
LPL Receptor
|
Inflammation/Immunology
|
|
Icanbelimod (S1p receptor agonist 1) is a potent and orally active S1P receptor agonist, exhibits an activity of inducing S1P1 internalization (EC50=9.83 nM). Icanbelimod has the potential for the study of arthritis and EAE (experimental autoimmune encephalitis). Icanbelimod is extracted from patent WO2015039587A1, Compound 2.
|
-
- HY-103235
-
|
|
iGluR
|
Neurological Disease
|
|
NPEC- caged-(S)-AMPA, a caged neurotransmitter analog, is a NPEC photoprotecting group caged the (S)-AMPA (HY-100815A) to make caged ligands specific for glutamate receptor sub-types. NPEC- caged-(S)-AMPA selectively activates AMPA receptor .
|
-
- HY-105154A
-
-
- HY-111295
-
|
|
Adenosine Receptor
|
Others
|
LAS38096 is a potent, selective, and efficacious A2B Adenosine Receptor antagonist, with a Ki of 17 nM .
|
-
- HY-119482
-
|
|
Progesterone Receptor
|
Others
|
|
Cymipristone (ZXH-951), a progesterone receptor antagonist, is used potentially for termination of intrauterine pregnancy .
|
-
- HY-120846
-
-
- HY-100842
-
-
- HY-135436
-
|
|
IGF-1R
|
Cancer
|
|
AG 538 is a potent, competitive inhibitor of IGF-1 receptor kinase, with an IC50 of 400 nM .
|
-
- HY-170410
-
|
|
iGluR
|
Neurological Disease
|
|
EMD-95885 is a selective NR2B-containing NMDA receptors antagonist with an IC50 of 3.9 nM. EMD-95885 does not interact with other sites on the NMDA receptor .
X
|
-
- HY-120223
-
|
|
Adrenergic Receptor
|
Metabolic Disease
|
|
BMS-196085 is an orally active, potent and selective full agonist against human β3 adrenergic receptor with a Ki value of 21 nM. BMS-196085 also has partial agonist activity at the β1 receptor. BMS-196085 is promising for research of obesity and type-II diabetes .
|
-
- HY-101010
-
|
|
Others
|
Neurological Disease
|
|
Methylfurmethide is an acetylcholine receptor. Methylfurmethide blocks the uptake of atropine. Methylfurmethide can be used to study the properties of acetylcholine receptors in intestinal smooth muscle .
|
-
- HY-154789
-
-
- HY-172244
-
-
- HY-147421
-
-
- HY-109147A
-
-
- HY-168986
-
-
- HY-103550
-
|
|
mGluR
|
Neurological Disease
|
|
A-841720 is a potent, non-competitive and selective mGlu1 receptor antagonist with an IC50 of 10 nM for human mGlu1 receptor. A-841720 displays 34-fold selectivity over mGlu5 (IC50 of 342 nM), and no significant activity at a range of other neurotransmitter receptors, ion channels, and transporters. A-841720 has the potential for chronic pain research .
|
-
- HY-103232
-
|
|
mGluR
|
Neurological Disease
|
IEM-1925 bromide is an orally active glutamate receptor antagonist, increases the latent period and decreases the duration of status epilepticus in rats in a lithium-pilocarpine model of epilepsy .
|
-
- HY-18764
-
|
|
PTEN
|
Metabolic Disease
|
|
BpV(pic) potassium hydrate is a PTEN inhibitor with IC50 31 nM. BpV(pic) potassium hydrate is also an insulin simulator that activates insulin receptor kinase in cultured liver cancer cells, stimulates adipogenesis in adipocytes, and inhibits the dephosphorylation of autophosphorylated insulin receptors and epidermal growth factor receptors in rat hepatosomes .
|
-
- HY-W140282
-
|
|
Angiotensin Receptor
|
Cardiovascular Disease
|
|
Angiotensin II antipeptide, a peptide, is an inverse agonist of AR1 receptor. Angiotensin II antipeptide is encoded by mRNA, complementary to that encoding Angiotensin II (HY-13948) itself .
|
-
- HY-147279
-
|
|
LDLR
|
Others
|
|
Milpocitide is a low-density lipoprotein receptor (human LDL receptor, LDLR), (293-333)-peptide fragment (EGF-like domain 1) .
|
-
- HY-N3398
-
-
- HY-129422
-
-
- HY-103336
-
|
T1117
|
GPR55
Cannabinoid Receptor
|
Cardiovascular Disease
|
|
Tocrifluor 1117 (T1117), a fluorescent form of the cannabinoid CB1 receptor antagonist AM251 (HY-15443), is a selective fluorescent GPR55 ligand. Tocrifluor 1117 is a potent tool for identifying the cellular location of cannabinoid receptors (including GPR55 in living tissues) (Ex/Em=543/590 nm) .
|
-
- HY-105346
-
|
|
Neurokinin Receptor
|
Neurological Disease
|
|
WIN 51708 is a nonpeptide antagonist of neurokinin (NK)-1 receptor. WIN 51708 has a higher affinity for the rat NK-1 receptor compared to the human NK-1 receptor .
|
-
- HY-125692
-
-
- HY-N7767
-
-
- HY-129636A
-
|
GABAB receptor antagonist 1
|
GABA Receptor
ERK
|
Neurological Disease
|
|
(E/Z)-CLH304a (GABAB receptor antagonist 1) is a mixture of (E)-CLH304a and (Z)-CLH304a. (E)-CLH304a (CLH304a; HY-129636) is a specific and noncompetitive GABAB receptor negative allosteric modulator (NAM). CLH304a inhibits Baclofen (HY-B0007)-induced ERK1/2 phosphorylation in HEK293 cells overexpressing GABAB receptors .
|
-
- HY-P1016B
-
|
|
Endothelin Receptor
|
Cardiovascular Disease
|
|
BQ-3020 ammonium is a selective endothelin receptor (ETB receptor) agonist. BQ-3020 ammonium inhibits [ 125I] ET-1 binding to ETB receptors, with an IC50 value of 0.2 nM. BQ-3020 ammonium elicits vasoconstriction in the rabbit pulmonary artery. BQ-3020 ammonium makes relaxation of the pig urinary bladder neck and can be used for cardiovascular disease research . .
|
-
- HY-155394
-
-
- HY-108498
-
|
|
Somatostatin Receptor
|
Endocrinology
|
|
L-817818 is a potent and subtype-selective agonist of the somatostatin receptor. L-817818 provides a direct approach to defining somatostatin receptor physiological functions
|
-
- HY-103532
-
|
|
GABA Receptor
|
Neurological Disease
|
|
CGP 46381 is an orally active GABAB receptor antagonist with IC50 of 4.9 μM. CGP 46381 blocks the neuronal depression induced by iontophoretically applied baclofen (HY-B0007) .
|
-
- HY-148088A
-
|
|
Adenosine Receptor
|
Cancer
|
|
M1069 (free base) is a selective and orall active, dual A2A/A2B adenosine receptor antagonist with a selectivity of >100 fold against the A1 and A3 receptors. M1069 (free base) counteracts immune-suppressive mechanisms of adenosine, and exhibits anti-tumor activity .
|
-
- HY-148252
-
|
|
Adrenergic Receptor
|
Endocrinology
|
|
ADRA1D receptor antagonist 1 (free base) (compound (R)-9s) is an orally active, potent and selective human α1D-adrenoceptor (α1D-AR) antagonist (Ki=1.6 nM). ADRA1D receptor antagonist 1 (free base) dose-dependently inhibits bladder contraction with an IC30 value of 15 nM. ADRA1D receptor antagonist 1 (free base) can be used in studies of overactive bladder disorders such as urinary urgency, frequency and incontinence.
|
-
- HY-P5158
-
|
|
Adrenergic Receptor
|
Others
|
|
Conopeptide rho-TIA is a peptide derived from the venom contained in the predatory sea snail Conus tulipa, has highly selective and noncompetitive inhibitor at human α1B-Adrenergic Receptor. Conopeptide rho-TIA acts a competitive inhibitor at human α1A-Adrenergic Receptor and α1D-Adrenergic Receptor. Conopeptide rho-TIA binds to each subtype and may provide useful information for the development of novel α1-Adrenergic Receptor subtype-selective drugs .
|
-
- HY-128127
-
|
|
LPL Receptor
|
Others
|
|
NAEPA, a phosphate-mimetic derivative, is a lysophosphatidic acid (LPA) receptor agonist .
|
-
- HY-120948
-
|
|
Fluorescent Dye
|
Others
|
|
RU 45196 is an 11 beta-substituted 19-norsteroid of the estra-4,9-diene series. RU 45196 displays fluorescence properties (excitation at 480 nm, emission at 525 nm) as well as high binding affinities for the glucocorticoid and progesterone receptors .
|
-
- HY-107748
-
|
5'-GNTI hydrochloride
|
Opioid Receptor
|
Neurological Disease
|
|
5'-Guanidinonaltrindole (5'-GNTI) hydrochloride is a highly selective and potent κ-opioid receptor antagonist with a Ki of 0.18 nM for human κ-opioid receptor .
|
-
- HY-B0098S
-
-
- HY-19467
-
-
- HY-103141
-
|
|
5-HT Receptor
|
Neurological Disease
|
|
SB-258585 is a high affinity ligand for the 5-HT6 receptor. SB-258585 binds highly to a single receptor population in a human cell line that recombines 5-HT6 receptors. SB-258585 can be used to label recombinant and natural 5-HT6 receptor .
|
-
- HY-10308
-
|
|
Others
|
Metabolic Disease
|
|
Lefradafiban is an orally active glycoprotein IIb/IIIa receptor antagonist. Lefradafiban can be metabolized to its active form, Fradafiban, a non-peptide GP IIb/IIIa receptor antagonist .
|
-
- HY-153963
-
|
|
Oxytocin Receptor
|
Endocrinology
|
|
PF-06655075 is a novel andnon–brain-penetrant oxytocin receptor agonist with increased selectivity for the oxytocin receptor and significantly increased pharmacokinetic stability. PF-06655075 can be used as a tool compound to further explore the role of peripheral oxytocin in behavioral response .
|
-
- HY-103115
-
|
EMD 281014; LY 2422347 hydrochloride
|
5-HT Receptor
|
Neurological Disease
|
|
Pruvanserin hydrochloride (EMD 281014) is a selective serotonin 5-HT2A receptor antagonist with IC50 values of 0.35 nM and 1 nM for human and rat 5-HT2A receptors. Pruvanserin (hydrochloride) can be used for the research of schizophrenia .
|
-
- HY-106917
-
|
Ro 41-3696
|
GABA Receptor
|
Neurological Disease
|
|
Lirequinil (Ro 41-3696) is an orally active partial agonist of the benzodiazepine (BDZ) receptor. Lirequinil has the effect of promoting sleep .
|
-
- HY-103407A
-
|
|
Dopamine Receptor
|
Neurological Disease
Cancer
|
|
PD 168568 dihydrochloride is a orally active and potent dopamine receptor D4 (DRD4) antagonist. PD 168568 dihydrochloride contains an isoindolinone and is selective for the D4 receptor versus D2 and D3, with Ki values of 8.8, 1842, and 2682 nM, respectively. PD 168568 dihydrochloride can be used for glioblastoma (GBM) research .
|
-
- HY-159840
-
|
|
FGFR
|
Cancer
|
|
Fanregratinib is a fibroblast growth factor receptor (FGFR) tyrosine kinase inhibitor .
|
-
- HY-W742957
-
|
|
iGluR
|
Neurological Disease
|
|
Pregnanolone sulfate pyridinium is an endogenous neurosteroid that inhibits NMDA receptors and is neuroprotective .
|
-
- HY-12701
-
-
- HY-107218
-
|
|
RAR/RXR
VD/VDR
|
Infection
|
|
11-Hydroxysugiol regulates the SUMOylation of intracellular receptors by modulating RARα and vitamin D3 receptor (VDR) .
|
-
- HY-P2165
-
-
- HY-157020
-
|
|
Ephrin Receptor
|
Cancer
|
|
UniPR1449 is an antagonist of EphA2 receptor, with th KD of 3.8±2.4 μM, that plays an important role in cancer .
|
-
- HY-111306
-
-
- HY-115553
-
|
|
Dopamine Receptor
|
Neurological Disease
|
|
DETQ is a selective, allosteric and orally active dopamine D1 receptor (Dopamine Receptor) potentiator. In HEK293 cells expressing the human D1 receptor, DETQ increases cAMP with an EC50 of 5.8 nM and a Kb of 26 nM. DETQ shows ~30-fold less potent at rat and mouse D1 receptors and is inactive at the human D5 receptor .
|
-
- HY-135021
-
|
|
5-HT Receptor
|
Others
|
|
3,4-Dihydro Naratriptan is a serotonin 5-HT1-receptor agonist. 3,4-Dihydro Naratriptan exhibits selective vasoconstrictor activity. 3,4-Dihydro Naratriptan can be used for migraine diseases research .
|
-
- HY-101348
-
|
|
Dopamine Receptor
|
Neurological Disease
|
|
L-741626 is a selective D2 dopamine receptor antagonist, with the Ki values of 2.4, 100 and 220 nM for human D2, D3 and D4 receptors respectively .
|
-
- HY-101372A
-
|
|
mAChR
|
Neurological Disease
|
|
Oxotremorine M iodide is a potent and non-selective muscarinic acetylcholine receptor (mAChR) agonist. Oxotremorine M iodide potentiates NMDA receptors by muscarinic receptor dependent and independent mechanisms .
|
-
- HY-P1335
-
|
|
Opioid Receptor
|
Neurological Disease
|
|
CTAP is a potent, highly selective, and BBB penetrant μ opioid receptor antagonist, with an IC50 of 3.5 nM. CTAP displays over 1200-fold selectivity over δ opioid (IC50=4500 nM) and somatostatin receptors. CTAP can be used for the study of L-DOPA-induced dyskinesia (LID) and opiate overdose or addiction .
|
-
- HY-13715
-
-
- HY-P1818
-
-
- HY-13715A
-
-
- HY-105960A
-
-
- HY-118328
-
|
|
5-HT Receptor
Potassium Channel
|
Cancer
|
|
Hymenidin is a natural antagonist of serotonergic receptor and inhibitor of voltage-gated potassium channels. Hymenidin also induces cancer cell apoptosis .
|
-
- HY-P3702
-
|
|
TRP Channel
|
Others
|
|
CEDAEVFKDSMVPGEK is the rat vanilloid receptor subtype 1 (VR1) peptides sequence, can be used to determine the presence and distribution of VR1 .
|
-
- HY-129507
-
|
DAB-452 fumarate
|
Dopamine Receptor
|
Neurological Disease
|
|
Aplindore fumarate (DAB-452 fumarate) is a dopamine D2 receptor partial agonist. Aplindore fumarate could be used in studies of Parkinson's disease and schizophrenia .
|
-
- HY-103526
-
|
|
GABA Receptor
|
Neurological Disease
|
|
DPNI-GABA is a nitroindoline cage compound that inhibits GABA(A) receptors and reduces GABA-evoked peak responses with an IC50 value of 0.5 mM .
|
-
- HY-A0229A
-
-
- HY-123744
-
-
- HY-103577
-
|
|
Androgen Receptor
|
Cancer
|
|
LG-121071 is an orally active and selective androgen receptor modulator with a Ki of 17 nM .
|
-
- HY-B1494
-
|
|
Chloride Channel
GABA Receptor
|
Neurological Disease
|
|
Picrotoxinin, a potent convulsant, is a chloride channel blocker. Picrotoxinin is a noncompetitive GABAA receptor antagonist, which negatively modulates the action of GABA on GABAA receptors. Picrotoxinin inhibits α1β2γ2L GABAA receptor with an IC50 of 1.15 μM .
|
-
- HY-156751
-
|
|
PROTACs
Androgen Receptor
|
Cancer
|
|
PROTAC AR Degrader-6 (Compound 1) is a PROTAC androgen receptor degrader (DC50: 10 nM in VCaP cell). PROTAC AR Degrader-6 blocks the process of androgen receptor transduction and also degrades the receptor itself. PROTAC AR Degrader-6 can be used for prostate cancer research. Pink: AR ligand (HY-130845); Blue: E3 ligase ligand (HY-W1003189); Black: linker (HY-169975) .
|
-
- HY-153584
-
|
|
GABA Receptor
|
Neurological Disease
|
|
MRK-898 is an orally active GABA(A) receptor modulator. MRK-898 binds to α1, α2, α3 or α5 subunit of GABA(A) receptor with Ki values of 1.2 nM, 1.0 nM, 0.73 nM, and 0.50 nM, respectively. However, α1-containing GABA(A) receptors are identified as the "sedative" and α2- and/or α3-containing receptors as the "anxiolytic" subtype(s) .
|
-
- HY-103246
-
|
|
Androgen Receptor
|
Cancer
|
|
TFM-4AS-1 is a selective androgen receptor modulator (SARM), and a potent androgen receptor (AR) ligand with an IC50 of 38 nM. TFM-4AS-1 is a gene-selective agonist .
|
-
- HY-13715B
-
-
- HY-A0172
-
-
- HY-14793
-
|
|
Dopamine Receptor
|
Neurological Disease
|
|
Lensiprazine is a potent dopamine D2 receptor (D2R) antagonist that acts as a serotonin reuptake inhibitor. Lensiprazine can be used to study bipolar disorder and schizophrenia .
|
-
- HY-163017
-
-
- HY-P10079
-
-
- HY-153958
-
-
- HY-124117
-
|
|
5-HT Receptor
|
Neurological Disease
|
|
LY 278584 is a potent, highly selective 5-HT3 receptor antagonist with a Ki of 1.62 nM. LY 278584 has no activity on 5-HT1A, 5-HT1B, 5-HT1C, 5-HT1D, or 5-HT2 receptors .
|
-
- HY-148533
-
|
|
mAChR
Adrenergic Receptor
|
Neurological Disease
|
|
β2AR agonist /M-receptor antagonist-1 is a potent dual muscarinic antagonist/beta 2 agonist (MABA). β2AR agonist /M-receptor antagonist-1 potently relaxes either Carbachol (HY-B1208)-induced contraction, in the absence (MABA) or presence of Propranolol (M3; HY-B1208), or Histamine (HY-B1204)-induced contraction (β2) .
|
-
- HY-101747A
-
-
- HY-107395
-
-
- HY-10666
-
-
- HY-101630A
-
|
EGIS-3886 fumarate
|
5-HT Receptor
|
Others
|
|
Deramciclane fumarate is an antagonist of 5-HT Receptor. Deramciclane fumarate is an inverse agonist of 5-HT2C Receptor with an IC50 of 168 nM. Deramciclane fumarate also decreases basal phosphoinositide hydrolysis .
|
-
- HY-13715C
-
-
- HY-101344
-
-
- HY-19401
-
-
- HY-120939
-
-
- HY-P2000
-
-
- HY-W009215
-
|
L-Met-L-Ala-L-Ser
|
Amino Acid Derivatives
|
Others
|
|
H-Met-Ala-Ser-OH (L-Met-L-Ala-L-Ser) is a tripeptide. H-Met-Ala-Ser-OH can act as a formyl receptor .
|
-
- HY-107700
-
|
GV 150526A
|
iGluR
|
Cardiovascular Disease
|
|
Gavestinel (GV 150526A) is a potent, selective, orally active and non-competitive antagonist of NMDA receptor. Gavestinel binds to the glycine site of the NMDA receptor, with a pKi of 8.5. Gavestinel can be used for the research of acute ischemic stroke .
|
-
- HY-P2572
-
-
- HY-120941
-
-
- HY-115413
-
-
- HY-W040046
-
|
Nafoxidene hydrochloride
|
Estrogen Receptor/ERR
|
Cancer
|
|
Nafoxidine hydrochloride is a non-steroidal estrogen receptor antagonist with antitumor activity for breast cancer .
|
-
- HY-P1207
-
-
- HY-P5175
-
|
|
mAChR
|
Neurological Disease
|
|
Muscarinic toxin 7 is a peptide toxin with selective and noncompetitive antagonism at the muscarinic M1 receptor .
|
-
- HY-107782
-
|
|
GABA Receptor
|
Neurological Disease
|
|
Picrotin is an active compound, also is one of the composition of picrotoxin (an antagonist of GABAA receptors (GABAARs) and glycine receptors (GlyRs)). Picrotin has sensitivity for GlyRs with IC50 values range from 5.2 μM to 106 μM. Picrotin can be used for the research of neurotransmission .
|
-
- HY-P4042
-
|
hepatitis B peptide 4980
|
HBV
|
Infection
Inflammation/Immunology
|
|
Hepatitis B Virus Receptor Binding Fragment (hepatitis B peptide 4980) is a synthetic peptide analog which specifically binds to Hep G2 cells. Hepatitis B Virus Receptor Binding Fragment is a promising immunogen expected to elicit protective antibodies based on the concept of the attachment blockade pathway of virus neutralization .
|
-
- HY-128113
-
-
- HY-135542
-
|
|
CRFR
|
Others
|
|
NBI-27914 is a potent and selective antagonist of CRFR1. The CRF receptors, CRFR1 and CRFR2, are members of the G protein-coupled receptor superfamily .
|
-
- HY-P3851
-
-
- HY-P10080
-
-
- HY-149274
-
|
|
Sigma Receptor
|
Neurological Disease
|
|
Sigma-1 receptor antagonist 4 (Compound 32) is a potent σ1R antagonist that significantly enhances the analgesic effect of morphine and rescues morphine-induced analgesic tolerance, with potential to prevent morphine tolerance .
|
-
- HY-151230
-
|
|
Estrogen Receptor/ERR
|
Cancer
|
|
(-)-Erteberel is a selective estrogen receptor beta (ERβ) agonist. (-)-Erteberel can be utilized in the study of diseases mediated by estrogen receptor beta (ERβ), such as prostate cancer .
|
-
- HY-P2355A
-
-
- HY-105183
-
|
|
Endothelin Receptor
|
Others
|
|
PD 145065 is a highly potent but non-selective endothelin receptor antagonist with an IC50 value of 4 nM for the ETA receptor for rabbit renal artery vascular smooth muscle cells .
|
-
- HY-105068
-
-
- HY-101747
-
-
- HY-107747
-
-
- HY-136623
-
-
- HY-108483
-
|
|
Neurokinin Receptor
|
Neurological Disease
Inflammation/Immunology
|
|
RP 67580 is a non-peptide antagonist of substance P (SP), competitively inhibits the binding of [3H]SP to neurokinin receptor 1 (NK1 receptor) in rat brain membranes with a Ki value of 4.16 nM. RP 67580 is a specific antagonist of NK1 receptors and can be used in the research of pain and neurogenic inflammation .
|
-
- HY-124372
-
|
|
mGluR
|
Neurological Disease
|
|
JNJ-46356479 is a selective and orally bioavailable mGlu2 receptor positive allosteric modulator (PAM), with the EC50 of 78 nM. JNJ-46356479 shows active in vivo .
|
-
- HY-P5072
-
|
|
Bombesin Receptor
|
Metabolic Disease
|
|
GRP (14-27) (human, porcine, canine) is a bombesin receptor ligand. The specific binding of GRP (14-27) is inhibited by GTP and GDP, whereas GMP was without effect .
|
-
- HY-100616A
-
|
trans-1-Aminocyclobutane-1,3-dicarboxylic acid
|
iGluR
|
Neurological Disease
|
|
trans-ACBD (trans-1-Aminocyclobutane-1,3-dicarboxylic acid) is a very potent and selective NMDA receptor agonist that modulates glutamatergic neurotransmission .
|
-
- HY-108679
-
|
|
Oxytocin Receptor
|
Neurological Disease
|
|
WAY-267464 hydrochloride is a non-peptide oxytocin receptor (OTR) agonist. WAY-267464 hydrochloride can impair social recognition memory in rats through a vasopressin 1A receptor antagonist action. WAY-267464 hydrochloride can be used for the research of psychiatric disorders, such disorders include autism spectrum disorder, schizophrenia, and social anxiety disorder .
|
-
- HY-109111
-
|
AMG 986
|
Apelin Receptor (APJ)
|
Others
|
|
Azelaprag (Example 263.0) is a candidate active molecule for an Apelin receptor agonist with an EC50 of 0.32 nM for the apelin receptor .
|
-
- HY-107606A
-
|
|
iGluR
|
Neurological Disease
|
|
UBP301 hydrochloride is a potent and selective antagonist of kainate receptor with IC50 and KD of 164 μM and 5.94 μM, respectively. UBP301 hydrochloride has ～30-fold selectivity of kainate receptor over AMPA receptor. UBP301 hydrochloride is the derivative of willardiine .
|
-
- HY-107606
-
|
|
iGluR
|
Neurological Disease
|
|
UBP301 is a potent and selective antagonist of kainate receptor with IC50 and KD of 164 μM and 5.94 μM, respectively. UBP301 has ∼30-fold selectivity of kainate receptor over AMPA receptor. UBP301 is the derivative of willardiine .
|
-
- HY-106933
-
-
- HY-107704
-
-
- HY-119544
-
|
UP-2696
|
Angiotensin Receptor
|
Cardiovascular Disease
|
|
Ripisartan (UP-2696) is an angiotensin II receptor antagonist. Ripisartan is orally available. Ripisartan binds to angiotensin II receptors, dilates blood vessels, and lowers blood pressure .
|
-
- HY-P2355
-
-
- HY-147707
-
|
|
Cannabinoid Receptor
|
Others
|
|
Hexyl resorcinol derivative 29 has been proved to be a CB2 selective competitive antagonist / reverse agonist with good potency. Olivanol and 5- (2-methyloctane-2-yl) resorcinol derivatives 23 and 24 showed significant antinociceptive activity. Compound 24 was shown to activate cannabinoid and TRPV1 receptors.
|
-
- HY-107566
-
|
|
Histamine Receptor
Parasite
|
Infection
|
|
Conessine, a steroidal alkaloid, is a potent and selective histamine H3 receptor antagonist with Kis of 5.4, 6.0, 5.7 and 25 nM for human, dog, guinea pig, and rat H H3 receptor, respectively. Anti-malarial activity .
|
-
- HY-103501
-
|
|
GABA Receptor
|
Neurological Disease
|
|
SB-205384 is a GABAA receptor modulator. The primary effect of SB-205384 on GABAA-activated currents is a prolonged response decay half-life upon removal of the agonist .
|
-
- HY-W008645
-
|
|
GABA Receptor
|
Neurological Disease
|
|
NCS-382 (sodium) is a potent GABA receptor antagonist. NCS-382 (sodium) has anti-sedative and anti-hypnotic activities and can be used in research related to neurological diseases .
|
-
- HY-149644
-
-
- HY-167901
-
|
|
Dopamine Receptor
|
Neurological Disease
|
|
Dinoxyline is a potent agonist at dopamine receptors (Ki = 7 nM, 6 nM, 5 nM, 43 nM for D1, D2, D3 and D4). Dinoxyline can be utilized in neurological research .
|
-
- HY-129995A
-
|
|
TSH Receptor
|
Endocrinology
|
|
TSHR antagonist S37a is a highly selective thyrotropin receptor (TSHR) antagonist, with potential for the treatment of Graves' orbitopathy .
|
-
- HY-137452A
-
-
- HY-132827
-
-
- HY-A0125
-
-
- HY-101262
-
-
- HY-B1494R
-
|
|
Chloride Channel
GABA Receptor
|
Neurological Disease
|
|
Picrotoxinin (Standard) is the analytical standard of Picrotoxinin. This product is intended for research and analytical applications. Picrotoxinin, a potent convulsant, is a chloride channel blocker. Picrotoxinin is a noncompetitive GABAA receptor antagonist, which negatively modulates the action of GABA on GABAA receptors. Picrotoxinin inhibits α1β2γ2L GABAA receptor with an IC50 of 1.15 μM .
|
-
- HY-14336
-
|
|
5-HT Receptor
|
Neurological Disease
|
|
SB 271046 is a potent, selective and orally active 5-HT6 receptor antagonist with a pKi of 8.92-9.09. SB 271046 show >200-fold selective for the 5-HT6 receptor over other receptors, binding sites and ion channels. SB 271046 has anticonvulsant activity .
|
-
- HY-153963A
-
|
|
Oxytocin Receptor
|
Endocrinology
|
|
PF-06655075 (TFA) is the TFA form of PF-06655075 (HY-153963). PF-06655075 is a novel andnon–brain-penetrant oxytocin receptor agonist with increased selectivity for the oxytocin receptor and significantly increased pharmacokinetic stability. PF-06655075 can be used as a tool compound to further explore the role of peripheral oxytocin in behavioral response .
|
-
- HY-138453
-
|
LPA1 receptor antagonist 2
|
LPL Receptor
|
Inflammation/Immunology
|
|
ACT-1016-0707 (Compound 49) is an orally active and selective LPA1 receptor antagonist. ACT-1016-0707 can be used for the research of fibrotic diseases .
|
-
- HY-133533
-
|
|
Cannabinoid Receptor
|
Neurological Disease
|
|
O-2050 is a high affinity cannabinoid CB1 receptor antagonist with a Ki of 2.5 nM. O-2050 inhibits cannabinoid CB2 receptor (Ki=0.2 nM). O-2050 can cause locomotor stimulation in mice .
|
-
- HY-P3802
-
|
|
Neurokinin Receptor
|
Neurological Disease
|
|
[D-Trp2,7,9] Substance P is a tachykinin (Neurokinin Receptor) antagonist with Ki values of 1 μM, 1.3 μM, and ~9 μM for NK-1, NK-2,and NK-3 receptor, respectively .
|
-
![[D-Trp2,7,9] Substance P](//file.medchemexpress.com/product_pic/hy-p3802.gif)
- HY-112074
-
|
HOE 440
|
Adrenergic Receptor
|
Cardiovascular Disease
|
|
Tiamenidine (HOE 440) is an orally active α2-adrenergic receptor agonist with antihypertensive effect. Tiamenidine is used as an antihypertensive agent for hypertension research .
|
-
- HY-19401A
-
-
- HY-112185A
-
|
LY3502970 hemicalcium hydrate; GLP-1 receptor agonist 1 hemicalcium hydrate
|
GCGR
|
Metabolic Disease
|
|
Orforglipron hemicalcium hydrate (LY3502970 hemicalcium hydrate; GLP-1 receptor agonist 1 hemicalcium hydrate) is the calcium salt hydrate form of Orforglipron (HY-112185). Orforglipron is an orally active agonist for Glucagon-like peptide-1 receptor (GLP-1R), which exhibits potency in ameliorating the type 2 diabete .
|
-
- HY-107747A
-
-
- HY-124462
-
|
R 2498
|
Sigma Receptor
|
Neurological Disease
|
|
Trifluperidol hydrochloride is a Sigma-1 receptor antagonist with a Ki value of 3.3 nM. Trifluperidol hydrochloride is used in the study of psychosis .
|
-
- HY-78168
-
-
- HY-101199
-
|
|
Opioid Receptor
|
Neurological Disease
|
|
N-Benzylnaltrindole hydrochloride is a potent δ2-selective opioid receptor antagonist. Benzylnaltrindole hydrochloride has a long duration of action in vivo than Naltriben (NTB). N-Benzylnaltrindole hydrochloride iserve as a useful tool in the pharmacologic characterization of δ-opioid receptor function .
|
-
- HY-P1121A
-
|
|
Formyl Peptide Receptor (FPR)
|
Inflammation/Immunology
|
|
WKYMVM-NH2 TFA is a potent N-formyl peptide receptor (FPR1) and FPRL1/2 agonist, also activates several leukocyte effector functions such as chemotaxis, mobilization of complement receptor-3, and activation of the NADPH oxidase .
|
-
- HY-116116
-
|
SIM010603
|
c-Kit
RET
VEGFR
|
Cancer
|
|
Tafetinib (SIM010603) is an oral multi-targets receptor tyrosine kinases inhibitor. Tafetinib inhibitsstem cell factor receptor (Kit),vascular endothelial growth factor receptor-2 (VEGFR-2),platelet-derived growth factor receptor-β (PDGFR-β),glial cell line-derived neurotrophic factor receptor (Rearranged during Transfection; RET), andFms-like tyrosine kinase-3 (FLT3)withIC50values between 5.0 and 68.1 nmol/l. Tafetinib inhibits the phosphorylation ofPDGFR-βandVEGFR-2. Tafetinib inhibits endothelial cell proliferation, endothelial cells chemotaxis, and corneal angiogenesis .
|
-
- HY-103427
-
|
|
Dopamine Receptor
|
Neurological Disease
|
|
NPEC-caged-dopamine is a caged version of dopamine. NPEC-caged-Dopamine was used by applying focal photolysis with UV light (360 nm) to releases dopamine, which leads to D1 receptor activation .
|
-
- HY-123499
-
|
|
Somatostatin Receptor
|
Cardiovascular Disease
|
|
SRA880 is a non-peptide and selective somatostatin sst(1) receptor antagonist. SRA880 exhibits antidepressant-like effects when in combination with Imipramine (HY-B1490A) .
|
-
- HY-123669
-
|
|
P2Y Receptor
|
Cardiovascular Disease
|
|
R-138727, the thiol-containing active metabolite of Prasugrel, is an irreversible platelet P2Y12 receptor inhibitor. R-138727 inhibits ADP-induced platelet aggregation .
|
-
- HY-107045
-
|
|
Estrogen Receptor/ERR
|
Endocrinology
|
|
CHF 4227 free base is an orally active and selective estrogen receptor modulator (SERM) with high affinity to the human estrogen receptor-α and -β (Ki values of 0.017 nM and 0.099 nM, respectively) .
|
-
- HY-157563
-
|
|
Dopamine Receptor
|
Neurological Disease
|
|
Dopamine D4 receptor ligand 2 (compound 17) is a potent and selective dopamine D4 ligand with IC50 values of 0.057, >1000, 220, 270 nM for D4, D2, 5-HT1A, α1, respectively .
|
-
- HY-131773
-
-
- HY-114630
-
-
- HY-P990089
-
-
- HY-B1115
-
-
- HY-119183
-
-
- HY-P4805
-
-
- HY-116958
-
|
|
Neurokinin Receptor
|
Inflammation/Immunology
|
|
SCH 206272 is a selective antagonist of the tachykinin (NK) receptor. SCH 206272 inhibits binding at human tachykinin NK(1), NK(2), and NK(3) receptors (Ki = 1.3, 0.4, and 0.3 nM, respectively). SCH 206272 has an orally active .
|
-
- HY-112071A
-
|
|
Adrenergic Receptor
|
Endocrinology
|
|
Prenalterol hydrochloride is a partial adrenal agonist with functional β1-receptor specificity and positive inotropic effects. Prenalterol hydrochloride is effective in suppressing acute heart failure, low output syndrome after myocardial infarction, shock, and reducing orthostatic hypotension in Shy-Drager syndrome .
|
-
- HY-77734
-
|
|
Drug Metabolite
|
Cardiovascular Disease
|
|
AR-C124910XX is a metabolite of Ticagrelor (HY-10064 ). Ticagrelor is a reversible oral P2Y12 receptor antagonist, and can be used for study of platelet aggregation .
|
-
- HY-116046
-
|
|
Melatonin Receptor
|
Others
|
|
GR 196429 is a melatonin receptor agonist with some selectivity for the MT1 subtype. GR 196429 produces both sleep-promoting effects and alterations of circadian rhythm, as well as stimulating melatonin release in mice .
|
-
- HY-160292
-
-
- HY-113555
-
-
- HY-P2159
-
|
|
Opioid Receptor
Endogenous Metabolite
|
Neurological Disease
|
|
Dynorphin A (1-8) is the predominant opioid peptide identified in placental tissue extracts. Dynorphin A (1-8) is the most likely natural ligand of the kappa receptor. The binding of 3H-Bremazocine to the purified kappa receptor is inhibited by Dynorphin A (1-8) (IC50=303 nM) .
|
-
- HY-105294
-
|
|
Dopamine Receptor
|
Others
|
FR 64822 is a dopamine D2 receptor agonist that can induce antinociceptive activity in rats and mice by indirectly stimulating dopamine D2 receptors. FR 64822 can promote penile erection in juvenile rats and improve amnesia in rats induced by scopolamine during passive avoidance tasks .
|
-
- HY-B1737
-
-
- HY-107072A
-
-
- HY-10822A
-
|
BGC 945 trisodium; Idetrexed trisodium; CB 300945 trisodium
|
Thymidylate Synthase
|
Cancer
|
|
ONX 0801 (BGC 945) trisodium is a thymidylate synthase (TS) inhibitor, targeted to α-folate receptor–overexpressing tumors .
|
-
- HY-113920A
-
|
EU4093 free base
|
Calcium Channel
|
Metabolic Disease
|
|
Azumolene (EU4093 free base), a Dantrolene analog, is a muscle relaxant. Azumolene is a ryanodine receptor (RyR) modulator and inhibits the calcium-release through ryanodine receptor. Azumolene can be used for malignant hyperthermia research .
|
-
- HY-119667
-
-
- HY-139436
-
-
- HY-122053
-
-
- HY-110213
-
|
|
Fluorescent Dye
|
Others
|
|
BODIPY 630/650X is a fluorescent conjugate of the adenosine receptor ligand N-ethylcarboxamido-adenosine (NECA). BODIPY 630/650X displays excitation/emission maxima of 630/650 nm, respectively .
|
-
- HY-P1167
-
-
![[Orn5]-URP](//file.medchemexpress.com/product_pic/hy-p1167.gif)
- HY-150790
-
-
- HY-123311
-
|
|
Adrenergic Receptor
|
Endocrinology
|
|
CP59430 is an azide analog of the α-adrenaline receptor antagonist Prazosin (HY-B0193). P59430 behaves as a competitive antagonist of α1-adrenaline receptor before photolysis. After photolysis, it specifically and irreversibly labels α1-adrenaline receptor and exhibits non-competitive antagonist activity. CP59430 can be used for the study of receptor molecular characterization .
|
-
- HY-107663
-
|
Pro-Leu-Gly-NH2; Melanostatin
|
Dopamine Receptor
|
Neurological Disease
|
|
MIF-1 (Melanostatin), an endogenous brain peptide, is a potent dopamine receptor allosteric modulator. MIF-1 inhibits melanin formation. MIF-1 blocks the effects of opioid receptor activation to modulate the analgesic effects. MIF-1 accesses from the blood to the CNS by directly crossing the blood-brain barrier (BBB) .
|
-
- HY-107782R
-
|
|
GABA Receptor
|
Neurological Disease
|
|
Picrotin (Standard) is the analytical standard of Picrotin. This product is intended for research and analytical applications. Picrotin is an active compound, also is one of the composition of picrotoxin (an antagonist of GABAA receptors (GABAARs) and glycine receptors (GlyRs)). Picrotin has sensitivity for GlyRs with IC50 values range from 5.2 μM to 106 μM. Picrotin can be used for the research of neurotransmission .
|
-
- HY-W654077
-
|
BPAF-d4; 4,4'-(Perfluoropropane-2,2-diyl)diphenol-d4
|
Estrogen Receptor/ERR
|
Endocrinology
|
Bisphenol AF-d4 is the isotope labelled analog of Bisphenol AF (HY-W013782). Bisphenol AF is a full agonist for the estrogen receptor. Bisphenol AF acts as an endocrine-disrupting chemical (EDC), activating estrogen through the estrogen receptor Era. Bisphenol AF-d4 can be used for the research of endocrinology and cancer .
|
-
- HY-108058A
-
|
|
Histamine Receptor
|
Inflammation/Immunology
|
|
Immethridine dihydrobromide is a selective histamine H3 receptor (H3R) agonist. Immethridine dihydrobromide displays 300-fold selectivity over the H4 receptor and does not bind to H1 or H2 receptors. Immethridine dihydrobromide can be used for experimental autoimmune encephalomyelitis (EAE) research .
|
-
- HY-151413
-
|
|
Neurokinin Receptor
|
Neurological Disease
|
|
MEN 10207 is a selective NK-2 tachykinin receptor (Neurokinin Receptor) antagonist. MEN 10207 has pA2 values of 5.2, 7.9 and 4.9 in three monoreceptor in vitro assays for NK-1, NK-2 and NK-3 tachykinin receptors, respectively.
|
-
- HY-13715BR
-
-
- HY-116031
-
|
|
MCHR1 (GPR24)
|
Metabolic Disease
|
|
ATC0175 (free base) is a potent and selective antagonist of melanin-concentrating hormone receptor 1 (MCH-R1) with an IC50 value of 3.4 nM, as well as good selectivity over the Y5 and the α2A receptors. ATC0175 (free base) is promising for research of obesity .
|
-
- HY-112185
-
|
LY3502970; GLP-1 receptor agonist 1
|
GCGR
|
Metabolic Disease
|
|
Orforglipron (LY3502970) (Compound 67) is an orally active agonist for Glucagon-like peptide-1 receptor (GLP-1R), which exhibits potency in ameliorates the type 2 diabete .
|
-
- HY-103414
-
|
|
Dopamine Receptor
|
Neurological Disease
|
|
Raclopride is a dopamine D2/D3 receptor antagonist with potential antipsychotic effects. Raclopride binds to D2 and D3 receptors with Kis of 1.8 nM and 3.5 nM, respectively .
|
-
- HY-122025
-
|
|
Androgen Receptor
|
Metabolic Disease
|
|
AC-262536 is a selective and non-steroidal androgen receptor modulators (SARMs) with beneficial anabolic effects. AC-262536 exhibits potent agonist activity at the androgen receptor, with an affinity in the low nanomolar range (1-10 nM) .
|
-
- HY-162163
-
|
|
Toll-like Receptor (TLR)
|
Cancer
|
|
TLR7 agonist 19 (Compound 14) is a Toll-like receptor 7 (TLR7) agonist with excellent pharmacokinetic properties and synergistic antitumor activity.
|
-
- HY-19814
-
-
- HY-156994
-
|
|
LYTACs
|
Others
|
|
ASGPR ligand-1 is an asialoglycoprotein receptor (ASGPR) ligand compound. ASGPR ligand-1 can be used for kinds of diseases research .
|
-
- HY-134661
-
|
|
GPR6
|
Neurological Disease
|
|
(S)-CVN424 is a potent G-Protein-Coupled Receptor 6 (GPR6) modulator. (S)-CVN424 has the potential for a variety of neurological and psychiatric disorders research, including Parkinson's disease .
|
-
- HY-15404
-
|
Lu-135252
|
Endothelin Receptor
|
Cardiovascular Disease
Endocrinology
|
|
Darusentan (Lu-135252) is a selective endothelin receptor A (ET-A) receptor antagonist, which binds with a Ki of 1.4 nM to the ET-A receptor and a Ki of 184 nM to ET-B receptor, respectively with a 100-fold selectivity for ETA rather than ETB receptors . Darusentan competes for radiolabeled endothelin binding in rat aortic vascular smooth muscle cells (RAVSMs) membranes with single-site kinetics, exhibiting a Ki of 13 nM .
|
-
- HY-105562
-
-
- HY-107749
-
-
- HY-123757
-
-
- HY-119076
-
-
- HY-112736
-
-
- HY-P1335A
-
|
|
Opioid Receptor
|
Neurological Disease
|
|
CTAP TFA is a potent, highly selective, and BBB penetrant μ opioid receptor antagonist, with an IC50 of 3.5 nM. CTAP TFA displays over 1200-fold selectivity over δ opioid (IC50=4500 nM) and somatostatin receptors. CTAP TFA can be used for the study of L-DOPA-induced dyskinesia (LID) and opiate overdose or addiction .
|
-
- HY-148212
-
|
|
GCGR
|
Cardiovascular Disease
Metabolic Disease
|
|
GLP-1R agonist 17 is a GLP-1 receptor agonist. GLP-1R agonist 17 shows excellent agonism on a GLP-1 receptor. GLP-1R agonist 17 can be used for the research of cardiovascular metabolic diseases .
|
-
- HY-100658
-
|
|
5-HT Receptor
Dopamine Receptor
|
Neurological Disease
|
|
Didesmethyl cariprazine is a metabolite of Cariprazine and acts as the predominant circulating active moiety. Didesmethyl cariprazine has a long half-life of 1-3 weeks. Cariprazine is a antipsychotic agent candidate that exhibits high affinity for the D3 and D2 receptors, and moderate affinity for the 5-HT1A receptor .
|
-
- HY-P1167A
-
-
![[Orn5]-URP TFA](//file.medchemexpress.com/product_pic/hy-p1167a.gif)
- HY-157455
-
|
|
Androgen Receptor
|
Cancer
|
|
AR antagonist 5 (compound 30a) is a selective androgen receptor (AR) antagonist with an IC50 value of 134.8 nM. AR antagonist 5 has favorable pharmacokinetic properties and shows a high skin exposure and low plasma exposure [1.
|
-
- HY-18200
-
|
E5555; ER-172594-00
|
Protease Activated Receptor (PAR)
JAK
Apoptosis
|
Cardiovascular Disease
Cancer
|
|
Atopaxar (E5555) is a potent, orally active, selective and reversible thrombin receptor protease-activated receptor-1 (PAR-1) antagonist. Atopaxar, an antiplatelet agent, interferes with platelet signaling. Atopaxar can be used for the research of atherothrombotic disease .
|
-
- HY-135588
-
|
|
Drug Metabolite
|
Metabolic Disease
|
|
Raloxifene 6,4'-Bis-β-D-glucuronide (compound IV) is a metabolite of Raloxifene. Raloxifene is a selective estrogen receptor antagonist for the prevention of osteoporosis .
|
-
- HY-164964
-
|
|
LPL Receptor
|
Neurological Disease
|
|
TRV045 is a selective Sphingosine-1-phosphate subtype 1 receptor agonist with no effect on lymphocyte transport. TRV045 has antiepileptic activity .
|
-
- HY-15706
-
|
|
LPL Receptor
|
Cardiovascular Disease
|
|
H2L 5765834 is an antagonist of lysophosphatidic acid receptors LPA1, LPA3, and LPA5, with IC50s of 94, 752, and 463 nM respectively .
|
-
- HY-103304
-
|
|
CGRP Receptor
|
Neurological Disease
|
|
CGRP antagonist 4 is an antagonist of calcitonin gene-related peptide (CGRP) receptor. CGRP antagonist 4 shows the highest affinity for CGRP receptors in the human brain. CGRP antagonist 4 can be used to study the binding properties of non-peptide calcitonin gene-related peptide (CGRP) receptor antagonist (gepants) in rat, pig and human menes .
|
-
- HY-145761
-
|
|
iGluR
|
Neurological Disease
|
|
AMPA-IN-1 is a potent inhibitor of AMPA receptor. AMPA receptors are receptors that are widely expressed in the brain, and play a central role in the regulation of fast excitatory synaptic transmission and synaptic plasticity. AMPA-IN-1 has the potential for the research of various central diseases including epilepsy (extracted from patent WO2017082288A1, compound 14) .
|
-
- HY-120970
-
|
|
Cholinesterase (ChE)
GABA Receptor
iGluR
|
Neurological Disease
|
|
Bis(7)-tacrine dihydrochloride is a dimeric AChE inhibitor derived from tacrine. Bis(7)-tacrine dihydrochloride prevents glutamate-induced neuronal apoptosis by blocking NMDA receptors. Bis(7)-tacrine dihydrochloride is a potent GABAAreceptor antagonist. Bis(7)-tacrine dihydrochloride has the potential for the research of Alzheimer's disease .
|
-
- HY-B0002B
-
|
GR 38032; SN 307
|
5-HT Receptor
|
Neurological Disease
Cancer
|
|
Ondansetron (GR 38032; SN 307) is a highly selective 5-HT3 receptor antagonist, with IC50 value of 103 pM. Ondansetron exerts antiemetic effects by antagonizing 5-HT receptor located on local neurons in the peripheral and central nervous system. Ondansetron suppresses nausea and vomiting caused by chemotherapy and radiation therapy. Ondansetron has orally bioactivity .
|
-
- HY-159829
-
-
- HY-135501
-
-
- HY-121453
-
-
- HY-107663A
-
|
Pro-Leu-Gly-NH2 TFA; Melanostatin TFA
|
Dopamine Receptor
|
Neurological Disease
|
|
MIF-1 TFA (Melanostatin), an endogenous brain peptide, is a potent dopamine receptor allosteric modulator. MIF-1 TFA inhibits melanin formation. MIF-1 TFA blocks the effects of opioid receptor activation to modulate the analgesic effects. MIF-1 TFA accesses from the blood to the CNS by directly crossing the blood-brain barrier (BBB) .
|
-
- HY-108976
-
|
|
Dopamine Receptor
|
Neurological Disease
|
|
Raclopride tartrate is a selective dopamine D2/D3 receptor antagonist with potential antipsychotic effects. Raclopride tartrate binds to D2 and D3 receptors with Kis of 1.8 nM and 3.5 nM, respectively .
|
-
- HY-107504
-
|
|
mGluR
|
Neurological Disease
|
|
VU0360172 hydrochloride is a potent and selective mGlu5 receptor positive allosteric modulator (PAM) with an EC50 value of 16 nM and a Ki of 195 nM, respectively. VU0360172 hydrochloride stimulates polyphosphoinositide (PI) hydrolysis in vivo, which is abrogated in mGlu5 receptors gene deleted mice .
|
-
- HY-131287
-
|
|
mGluR
|
Neurological Disease
|
|
MGS0028 is a selective metabotropic glutamate 2/3 (mGlu2/3) receptor agonist. MGS0028 can be used for psychiatric disorders research .
|
-
- HY-123127
-
-
- HY-P3546
-
-
![[DPen2, Pen5] Enkephalin](//file.medchemexpress.com/product_pic/hy-p3546.gif)
- HY-119802
-
-
- HY-122203
-
|
|
mAChR
Cholinesterase (ChE)
|
Neurological Disease
|
|
PCS1055 dihydrochloride is a potent, selective and competitive muscarinic M4 receptor antagonist with an IC50 of 18.1 nM and a Kd of 5.72 nM. PCS1055 dihydrochloride inhibits radioligand [ 3H]-NMS binding to the M4 receptor with a Ki of 6.5 nM. PCS1055 dihydrochloride exhibits >100-fold selectivity over M1-, M3-, and M5-receptors and 30-fold selectivity at the M2 receptor. PCS1055 dihydrochloride is also a potent AChE inhibitor with IC50 s of 22 nM and 120 nM for electric eel and human AChE, respectively .
|
-
- HY-146109
-
|
|
Parasite
|
Infection
|
|
RyRs activator 1 (compound 7f) is a potent activator of ryanodine receptors (RyRs). RyRs activator 1 at 0.5 mg/L displays 100% larvicidal activity. The larvicidal activity of RyRs activator 1 is 90% at 0.01 mg/L .
|
-
- HY-160210
-
|
|
Adrenergic Receptor
|
Cardiovascular Disease
|
|
BAY-6096 is a potent, selective, and highly water-soluble adrenergic receptor α2B antagonist with an IC50 of 14 nM. BAY-6096 can effectively reduceα 2B receptor agonist-induced rat vascular contraction .
|
-
- HY-18200B
-
|
E5555 hydrobromide; ER 172594-06
|
Protease Activated Receptor (PAR)
JAK
Apoptosis
|
Cardiovascular Disease
Cancer
|
|
Atopaxar (E5555) hydrobromide is a potent, orally active, selective and reversible thrombin receptor protease-activated receptor-1 (PAR-1) antagonist. Atopaxar hydrobromide, an antiplatelet agent, interferes with platelet signaling. Atopaxar hydrobromide can be used for the research of atherothrombotic disease .
|
-
- HY-103535
-
-
- HY-169753
-
-
- HY-W040146
-
|
Propiopromazine hydrochloride
|
Dopamine Receptor
|
Neurological Disease
|
|
Propionylpromazine hydrochloride (Propiopromazine hydrochloride), a dopamine receptor D2 (DRD2) antagonist, can be used in the research of Parkinson disease .
|
-
- HY-143226
-
|
|
Estrogen Receptor/ERR
|
Metabolic Disease
|
|
DK1 is a potent modulator of estrogen related receptor. DK1 has an ability in reducing blood glucose, and impacts the activity of ERRα receptor. DK1 has the potential for the research of diabetes .
|
-
- HY-P2526
-
LyP-1
2 Publications Verification
|
Complement System
|
Cancer
|
|
LyP-1 is a cyclic 9‐amino‐acids tumor homing peptide and selectively bind to p32 receptors overexpressed in various tumor-associated cells .
|
-
- HY-14325
-
|
|
Dopamine Receptor
|
Neurological Disease
|
|
L-745870 is a potent, selective, brain-penetrant and orally active dopamine D4 receptor antagonist with a Ki of 0.43 nM. L-745870 shows weaker affinity for D2 (Ki of 960 nM) and D3 (Ki of 2300 nM) receptors, and exhibits moderate affinity for 5-HT2 receptors, sigma sites and α-adrenoceptors .
|
-
- HY-14325B
-
|
|
Dopamine Receptor
|
Neurological Disease
|
|
L-745870 hydrochloride is a potent, selective, brain-penetrant and orally active dopamine D4 receptor antagonist with a Ki of 0.43 nM. L-745870 hydrochloride shows weaker affinity for D2 (Ki of 960 nM) and D3 (Ki of 2300 nM) receptors, and exhibits moderate affinity for 5-HT2 receptors, sigma sites and α-adrenoceptors .
|
-
- HY-129636
-
|
(E)-GABAB receptor antagonist 1
|
GABA Receptor
ERK
|
Neurological Disease
|
|
CLH304a (compound 14) is a specific and noncompetitive GABAB receptor negative allosteric modulator (NAM). CLH304a decreases GABA-induced IP3 production with an IC50 of 37.9 μM. CLH304a has no effect on other GPCR Class C members such as mGluR1, mGluR2, and mGluR5. CLH304a acts on the heptahelical domain of GB2 subunits and non-competitively inhibits the effect of agonists with inverse agonist properties. CLH304a inhibits Baclofen (HY-B0007)-induced ERK1/2 phosphorylation in HEK293 cells overexpressing GABAB receptor .
|
-
- HY-101299A
-
|
DAR-0100
|
Dopamine Receptor
|
Neurological Disease
|
|
Dihydrexidine (DAR-0100) is a high potent, selective and full efficacy D1-like dopamine receptor (D1/D5) agonist with an IC50 of 10 nM for D1 receptor. Dihydrexidine exhibits potent antiparkinsonian activity . Dihydrexidine can stimulate YAP phosphorylation .
|
-
- HY-112603A
-
|
|
Free Fatty Acid Receptor
|
Metabolic Disease
|
|
AP5 sodium is a potent, orall active, and selective GPR40 receptor agonist with a positive allosteric modulation of endogenous ligand (AgoPAM). AP5 sodium demonstrates rat and human inositol monophosphate (IP1) EC50 values of 0.49 nM and 0.8 nM against the GPR40 receptor, respectively. AP5 sodium has the potential for type II diabetes research .
|
-
- HY-101299B
-
|
DAR-0100 hydrochloride
|
Dopamine Receptor
|
Neurological Disease
|
|
Dihydrexidine hydrochloride (DAR-0100 hydrochloride) is a high potent, selective and full efficacy D1-like dopamine receptor (D1/D5) agonist, with an IC50 of 10 nM for D1 receptor. Dihydrexidine hydrochloride exhibits potent antiparkinsonian activity . Dihydrexidine hydrochloride can stimulate YAP phosphorylation .
|
-
- HY-112603
-
|
|
Free Fatty Acid Receptor
|
Metabolic Disease
|
|
AP5 is a potent, orlly active, and selective GPR40 receptor agonist with a positive allosteric modulation of endogenous ligand (AgoPAM). AP5 demonstrates rat and human inositol monophosphate (IP1) EC50 values of 0.49 nM and 0.8 nM against the GPR40 receptor, respectively. AP5 has the potential for type II diabetes research .
|
-
- HY-P5064
-
|
|
Neuropeptide Y Receptor
|
Neurological Disease
|
|
Galanin-Like Peptide (porcine) is a 60 amino acid neuropeptide that was first isolated from the porcine hypothalamus. Galanin-Like Peptide (porcine) has a high affinity for the GALR2 receptor (IC50 of 0.24 nM) and a lower affinity for the GALR1 receptor (IC50 of 4.3 nM) .
|
-
- HY-171175
-
|
|
Ephrin Receptor
|
Cancer
|
|
UniPR500, a UniPR129 derivative, is a competitive EphA2 receptor antagonist with a Ki of 0.78 μM. UniPR500 dose-dependently reduces binding of biotinylated ephrin-A1 to EphA2 with an IC50 value of 1.1 μM .
|
-
- HY-153258
-
|
|
CaSR
|
Metabolic Disease
|
|
CaSR
antagonist-1 is a calcium sensing receptor (CaSR) antagonist
with an IC50 value of 50 nM. CaSR
antagonist-1 can be used for the research of disorders associated with abnormal
bone or mineral homeostasis such as osteoporosis .
|
-
- HY-101165
-
|
|
iGluR
|
Neurological Disease
|
|
Cyclothiazide, a positive allosteric modulator of AMPA receptors, is used frequently to block the desensitization of both native and heterologously expressed AMPA receptors. Cyclothiazide is known to produce a fast inhibition of AMPA receptor desensitization and a much slower potentiation of the AMPA current .
|
-
- HY-13204
-
|
KL 373 hydrochloride
|
mAChR
|
Neurological Disease
|
|
Biperiden (KL 373) hydrochloride is a non-selective muscarinic receptor antagonist that competitively binds to M1 muscarinic receptors, thereby inhibiting acetylcholine and enhancing dopamine signaling in the central nervous system. Biperiden hydrochloride has the potential for the research of Parkinson's disease and other related psychiatric disorders .
|
-
- HY-13204A
-
|
KL 373
|
mAChR
|
Neurological Disease
|
|
Biperiden (KL 373) is a non-selective muscarinic receptor antagonist that competitively binds to M1 muscarinic receptors, thereby inhibiting acetylcholine and enhancing dopamine signaling in the central nervous system. Biperiden has the potential for the research of Parkinson's disease and other related psychiatric disorders .
|
-
- HY-B0649
-
-
- HY-122359B
-
|
L-Centchroman fumarate; L-Ormeloxifene fumarate
|
Estrogen Receptor/ERR
|
Others
|
|
Levormeloxifene (fumarate) is a stable salt form of Levormeloxifene. Levormeloxifene (fumarate) is an estrogen receptor modulator that plays an important role in prevention of postmenopausal bone loss .
|
-
- HY-N2911
-
|
|
Cannabinoid Receptor
|
Neurological Disease
|
|
Auriculasin is a nature product isolated from Limonium leptophyllum. Auriculasin has activity toward cannabinoid receptor type 1 (CB1) with an IC50 value of 8.92 µM .
|
-
- HY-145128
-
-
- HY-131914
-
|
|
Sigma Receptor
|
|
|
EST64454 (compound 9k) is a selective, orally active sigma-1 receptor antagonist with Ki 22 nM. EST64454 can be used to study pain .
|
-
- HY-101349A
-
|
|
Dopamine Receptor
|
Neurological Disease
|
|
L 741742 hydrochloride is an orally active and selective antagonist of hD4 receptors. L 741742 hydrochloride has a good brain penetration. L 741742 hydrochloride can be used in study nervous system disorders, particularly schizophrenia .
|
-
- HY-124910
-
-
- HY-14298
-
|
GSK-159797C
|
Adrenergic Receptor
|
Endocrinology
|
|
Milveterol hydrochloride is a long-acting β2-adrenergic receptor agonist. Milveterol hydrochloride can be used in study asthma and chronic obstructive pulmonary disease (COPD) .
|
-
- HY-157955A
-
-
- HY-123012A
-
|
LY-591281; LY-488756 fumarate
|
Androgen Receptor
|
Metabolic Disease
|
|
Lubabegron (LY-488756) fumarate is an antagonist of the adrenergic receptor (β-AR). Lubabegron fumarate can antagonize the stimulatory effects of β1-AR and β2-AR agonists on lipase respectively .
|
-
- HY-W700638A
-
-
- HY-124626
-
|
|
Histamine Receptor
|
Inflammation/Immunology
|
(R)-(+)-Mequitazine is a histamine H1 receptor antagonist that mainly undergoes bio-transformation via human liver microsomes, resulting in hydroxylated and S-oxidized metabolites. (R)-(+)-Mequitazine competitively binds to the H1 receptors in gastrointestinal, vascular, and respiratory effect cells, thus blocking the endogenous activity of histamine. (R)-(+)-Mequitazine has an inhibitory effect on CYP3A-catalyzed midazolam 1’-hydroxylase. (R)-(+)-Mequitazine can be used in the study of various allergic diseases .
|
-
- HY-14552
-
|
SB 223412
|
Neurokinin Receptor
|
Neurological Disease
Endocrinology
|
|
Talnetant (SB 223412) is a selective, competitive, brain-permeable NK3 receptor antagonist with a Ki of 1.4 nM in hNK-3-CHO cells. Talnetant is 100-fold more selective for hNK-3 relative to the hNK-2 receptor and has no affinity for hNK-1. Talnetant can be used in schizophrenia-related studies .
|
-
- HY-10847A
-
|
SB-277011A dihydrochloride
|
Dopamine Receptor
|
Neurological Disease
|
|
SB-277011 dihydrochloride (SB-277011A dihydrochloride) is a potent, selective, orally bioavailable and brain penetrate dopamine D3 receptor antagonist, with pKis of 8.0, 6.0, <5.2 and 5.9 for D3, D2, 5-HT1B, and 5-HT1D receptors, respectively.
|
-
- HY-14552A
-
|
SB 223412 hydrochloride; SB 223412-A
|
Neurokinin Receptor
|
Neurological Disease
Endocrinology
|
|
Talnetant (SB 223412) hydrochloride is a selective, competitive, brain-permeable NK3 receptor antagonist with a Ki of 1.4 nM in hNK-3-CHO cells. Talnetant hydrochloride is 100-fold more selective for hNK-3 relative to the hNK-2 receptor and has no affinity for hNK-1. Talnetant hydrochloride can be used in schizophrenia-related studies .
|
-
- HY-123335
-
|
|
Somatostatin Receptor
|
Others
|
|
L-796,778 is an agonist of the hsst3 receptor. In CHO-K1 cells expressing the hsst3 receptor, L-796,778 is a partial agonist that inhibits forskolin (HY-15371)-stimulated cAMP production with an IC50 value of 18 nM .
|
-
- HY-P10138
-
-
- HY-128205
-
|
|
TRP Channel
|
Neurological Disease
|
|
BTD is a selective transient receptor potential canonical 5 (TRPC5) activator. BTD can be used for the research of neurological disease .
|
-
- HY-147544
-
-
- HY-147543
-
-
- HY-103578
-
|
|
Androgen Receptor
|
Cancer
|
|
S-40503 is an orally active and selective androgen receptor modulator. S-40503 significantly increases the bone mineral density (BMD) and biomechanical strength of femoral cortical bone .
|
-
- HY-147545
-
-
- HY-127120
-
|
|
Dopamine Receptor
|
Neurological Disease
|
|
Timiperone has a strong affinity for cerebral dopamine D2 receptor. Timiperone has antipsychotic activity, and inhibits stereotyped behaviour. Timiperone can be used for research of schizophrenia .
|
-
- HY-120076
-
|
|
Dopamine Receptor
|
Neurological Disease
|
CP-293019 is a dopamine D4 receptor antagonist, with a Ki value of 3.4 nM. CP-293019 can inhibit Apomorphine (HY-12723) induced hyperactivity in rats .
|
-
- HY-169791
-
|
|
5-HT Receptor
|
Neurological Disease
|
|
ECPLA, a lysergamide lysergic acid diethylamidean (LSD) analog, is a potent 5-HT2A agonist (EC50 of 14.6 nM) for Gq-mediated calcium flux. ECPLA has high affinity for most serotonin receptors, α2-adrenoceptors, and D2-like dopamine receptors .
|
-
- HY-117824
-
|
|
Integrin
|
Others
|
|
L-703014 is a fibrinogen receptor antagonist, with the IC50 of 94 nM, that acts as a novel parenteral and potential oral antithrombotic agent .
|
-
- HY-168750
-
|
|
Cannabinoid Receptor
|
Neurological Disease
|
|
MDMB-FUBICA, a synthetic cannabinoid, is a potent agonist of the cannabinoid receptors with psychoactive properties. MDMB-FUBICA can be used in electronic cigarette .
|
-
- HY-101353
-
|
(-)-LY 235959
|
iGluR
|
Neurological Disease
|
|
LY 235959 is a competitive N-methyl-D-aspartate (NMDA)-receptor antagonist. LY 235959 potentiates the anticonvulsant action of antiepileptics .
|
-
- HY-P0210
-
|
|
Opioid Receptor
|
Cancer
|
|
DAMGO is a μ-opioid receptor (μ-OPR ) selective agonist with a Kd of 3.46 nM for native μ-OPR .
|
-
- HY-111480
-
|
|
Dopamine Receptor
|
Neurological Disease
|
|
Propionylpromazine is a dopamine receptor DRD2 antagonist. Propionylpromazine also is an effective tranquillizer. Propionylpromazine can be used in veterinary studies .
|
-
- HY-121276
-
|
|
Dopamine Receptor
|
Neurological Disease
|
|
Benperidol is a relatively old antipsychotic agent. Benperidol is a butyrophenone antipsychotic, with the highest neuroleptic potency in terms of D2 receptor blockade .
|
-
- HY-P3874
-
|
|
Opioid Receptor
|
Neurological Disease
|
|
Peptide E is a potent kappa opiate receptor agonist. Peptide E has opiate receptor binding activity with IC50 value of 0.39 μM. Peptide E can be used for the research of central nervous system .
|
-
- HY-120524
-
|
|
iGluR
|
Neurological Disease
|
|
CGP 31358 is an anticonvulsant agent that binds to a site on the NMDA receptor complex that is coupled to both the transmitter recognition site and to the channel domain. CGP 31358 inhibits the binding of L-Glutamate to the NMDA receptor complex with an IC50 of 53 μM .
|
-
- HY-123571
-
-
- HY-N6097
-
-
- HY-118497
-
|
|
Endothelin Receptor
|
Cardiovascular Disease
Metabolic Disease
|
|
BMS 182874 is an orallyactive, highly selective endothelin receptor (ETA receptor) antagonist, with IC50 value of 0.150 μM, Ki of 0.055 μM. BMS 182874 reduces the arterial pressure of Deoxycorticosterone acetate (HY-B1472) induced hypertension model in rats, and can be used for cardiovascular disease research .
|
-
- HY-103458
-
|
|
Endothelin Receptor
|
Cardiovascular Disease
Metabolic Disease
|
|
BMS 182874 hydrochloride is an orallyactive, highly selective endothelin receptor (ETA receptor) antagonist, with IC50 value of 0.150 μM, Ki of 0.055 μM. BMS 182874 hydrochloride reduces the arterial pressure of Deoxycorticosterone acetate (HY-B1472) induced hypertension model in rats, and can be used for cardiovascular disease research .
|
-
- HY-19007
-
|
DA 4577
|
Histamine Receptor
|
Endocrinology
|
|
Mifentidine (DA 4577) is a potent and selective H2 Receptor antagonist. Mifentidine has an anti-secretion effect and can antagonize the acid-promoting activity of histamine with EC50 3.28 μM .
|
-
- HY-155334
-
|
|
Parasite
|
Others
|
|
RyRs activator 4 (compound B18) is an insect ryanodine receptor activator. RyRs activator 4 has a larvicidal activity of Mythimna separata with an LC50 value of 1.32 mg/L .
|
-
- HY-12244
-
-
- HY-110065
-
|
|
Cannabinoid Receptor
|
Neurological Disease
|
|
SER-601 is a potent and selective peripheral cannabinoid (CB2) receptor agonist with a Ki of 6.3 nM. SER-601 has analgesic and antidiabetic properties and can be used for relevant research .
|
-
- HY-P10138A
-
-
- HY-B0298A
-
|
HS-592 fumarate; Meclastine fumarate
|
Histamine Receptor
|
Neurological Disease
Endocrinology
|
|
Clemastine (HS-592) fumarate is a selective histamine H1 receptor antagonist. Clemastine fumarate is an antihistamine mainly used for relieving symptoms of allergic reactions primarily by competing with histamine to bind H1 receptors. Anti-inflammatory effects .
|
-
- HY-B0002BR
-
|
|
5-HT Receptor
|
Neurological Disease
Cancer
|
|
Ondansetron (Standard) is the analytical standard of Ondansetron. This product is intended for research and analytical applications. Ondansetron (GR 38032; SN 307) is a highly selective 5-HT3 receptor antagonist, with IC50 value of 103 pM. Ondansetron exerts antiemetic effects by antagonizing 5-HT receptor located on local neurons in the peripheral and central nervous system. Ondansetron suppresses nausea and vomiting caused by chemotherapy and radiation therapy. Ondansetron has orally bioactivity .
|
-
- HY-N9141
-
|
|
5-HT Receptor
|
Neurological Disease
|
|
Nantenine is a serotonergic receptor antagonist. Nantenine selectively inhibits the contractile response of tissues to serotonin. Nantenine can be isolated from Nandina domestica .
|
-
- HY-120811
-
|
|
iGluR
|
Neurological Disease
|
|
PF-04701475 is a potent AMPA receptor potentiator with an EC50 of 123 nM. PF-04701475 can be used for the study of neurological disorders .
|
-
- HY-P0210B
-
|
|
Opioid Receptor
|
Cancer
|
|
DAMGO TFA is a μ-opioid receptor (μ-OPR ) selective agonist with a Kd of 3.46 nM for native μ-OPR .
|
-
- HY-P1465
-
-
- HY-106180
-
|
GR 56072; RG 14202; Selodenoson
|
Adenosine Receptor
|
Neurological Disease
|
|
DTI 0009 is a selective adenosine A1 receptor agonist used to reduce heart rate in patients with atrial fibrillation and to treat arrhythmias .
|
-
- HY-113246
-
|
15-keto-PGF2α
|
Prostaglandin Receptor
Endogenous Metabolite
|
Endocrinology
|
|
15-keto-Prostaglandin F2α (15-keto-PGF2α) is a metabolite of Prostaglandin F2α. Prostaglandin F2α. Prostaglandin F2α is an orally active, potent prostaglandin F (PGF) receptor (FP receptor) agonist and plays a key role in the onset and progression of labour .
|
-
- HY-110036A
-
|
L768242 hydrochloride
|
Cannabinoid Receptor
|
Neurological Disease
|
|
GW-405833 (L768242) hydrochloride is a potent, selective cannabinoid receptor 2 (CB2) agonist with an EC50 of 50.7 nM. GW-405833 hydrochloride also behaves as a noncompetitive CB1 antagonist. GW-405833 hydrochloride suppresses inflammatory and neuropathic pain .
|
-
- HY-148531
-
|
|
CCR
|
Inflammation/Immunology
|
|
PF-07054894 is an orally active and potent C-C Chemoattractant Cytokine (Chemokine) Receptor 6 (CCR6) antagonist that blocks CCR6-mediated chemotaxis with an IC50 value of 5.7 nM in vitro. PF-07054894 targets G protein-coupled receptor (GPCR). PF-07054894 can be used in research of inflammatory bowel disease .
|
-
- HY-122761
-
|
|
mAChR
|
Neurological Disease
|
|
Quifenadine (Compound 3a), the hydroxyl-(diphenyl)methyl quinuclidine derivative, is a M3 receptor antagonist with an IC50 value > 1000 nM. Quifenadine can be used for the research of neurological disease .
|
-
- HY-10307
-
-
- HY-19580
-
|
CM 57755A
|
Histamine Receptor
|
Endocrinology
|
Ramisotidine is a histamine H2 receptor antagonist that can inhibit gastric acid secretion stimulated by pentagastrin .
|
-
- HY-B1115A
-
-
- HY-145700
-
-
- HY-143576
-
-
- HY-W653723
-
|
NDCHA
|
Androgen Receptor
|
Endocrinology
|
|
N-Nitrosodicyclohexylamine (NDCHA) is a N-nitrosocompound with anti-androgenic activities. N-Nitrosodicyclohexylamine shows the competitive binding to androgen receptor (AR) against 5α-dihydrotestosterone and decreased the level of AR protein .
|
-
- HY-163667
-
|
|
Opioid Receptor
|
Neurological Disease
|
|
Atoxifent is a potent μ-opioid receptor agonist (EC50=0.39 nM). These receptors are found in brain regions that control pain, emotions, habitual learning, and cognition. Atoxifent exhibits strong analgesic effects and a lower risk of respiratory depression. Atoxifent can be used for research in opioid pharmacology and signal transduction .
|
-
- HY-108509
-
|
BMY-14802-1; BMS 181100 hydrochloride
|
Sigma Receptor
5-HT Receptor
Adrenergic Receptor
|
Neurological Disease
|
|
BMY-14802 hydrochloride (BMY-14802-1) is a selective and orally active sigma receptor antagonist with an IC50 of 112 nM. BMY-14802 hydrochloride is also a 5-HT1A and adrenergic α1 receptors agonist. BMY-14802 hydrochloride has antipsychotic effects .
|
-
- HY-155316
-
-
- HY-W725190A
-
|
|
Opioid Receptor
|
Neurological Disease
|
|
Piperidylthiambutene is a potent µ-opioid receptor (MOR) agonist with a Ki of 2.75 nM. Piperidylthiambutene exhibits analgesic and antitussive properties and can be utilized in relevant research .
|
-
- HY-113889
-
|
|
Progesterone Receptor
|
Cancer
|
|
ZK112993 is a potent progesterone receptor (PR) antagonist. ZK112993 significantly inhibits the growth of T61 human tumors in nude mice .
|
-
- HY-P1465A
-
-
- HY-111064
-
-
- HY-108237
-
|
(+)-PHNO; Dopazinol
|
Dopamine Receptor
|
Neurological Disease
|
|
Naxagolide ((+)-PHNO; Dopazinol) is a potent dopamine D2 (Dopamine Receptor) agonist. Naxagolide has the potential for the research of parkinson's disease (PD) .
|
-
- HY-P1165
-
-
- HY-B0298
-
|
HS-592; Meclastine
|
Histamine Receptor
|
Neurological Disease
|
|
Clemastine (HS-592) is a potent and orally active histamine receptor H1 antagonist. Clemastine is an antihistamine mainly used for relieving symptoms of allergic reactions primarily by competing with histamine to bind H1 receptors. Anti-inflammatory effects .
|
-
- HY-155748
-
|
|
MELK
Apoptosis
|
Cancer
|
|
Antitumor agent-116 (compound 6C) is an anti-tumor agent with anti-proliferative activities. Antitumor agent-11 induces cell apoptosis, and shows the binding affinity against the MELK receptor .
|
-
- HY-16413
-
|
Caytine hydrochloride; JB-251 hydrochloride
|
TRP Channel
Adrenergic Receptor
|
Others
|
|
Protokylol hydrochloride (Caytine hydrochloride; JB-251 hydrochloride) is the hydrochloride salt form of Protokylol (HY-114630). Protokylol hydrochloride is an agonist for β2-adrenergic receptor and TRPV1. Protokylol hydrochloride exhibits activity as a bronchodilator .
|
-
- HY-131388
-
-
- HY-112412
-
|
PDGF receptor Tyrosine Kinase Inhibitor III
|
PDGFR
|
Neurological Disease
|
|
PDGFR Tyrosine Kinase Inhibitor III (PDGF Receptor Tyrosine Kinase Inhibitor III), a multikinase inhibitor, inhibits PDGFR, EGFR, FGFR, PKA, and PKC, respectively. PDGFR Tyrosine Kinase Inhibitor III can be used for the research of amyotrophic lateral sclerosis .
|
-
- HY-153345
-
-
- HY-11052A
-
|
|
Opioid Receptor
|
Neurological Disease
|
|
Trap-101 hydrochloride is a potent, selective and competitive antagonist of NOP receptors over classical opioid receptors. Trap-101 stimulates GTPγ 35S binding to CHOhNOP membranes with pKi values of 8.65, 6.60, 6.14 and <5 for NOP, μ-, κ-, and δ-opioid receptors, respectively. Trap-101 attenuates motor deficits in a rat model of parkinson's disease and can be used for the research of nervous system diseases .
|
-
- HY-108977
-
-
- HY-103562
-
|
3,3'-Dimethoxybenzaldazine
|
mGluR
|
Neurological Disease
|
|
DMeOB is an agonist of mGluR5 receptor with an IC50 of 3 μM. DMeOB has a negative modulatory effect .
|
-
- HY-14612
-
|
|
mGluR
|
Neurological Disease
|
|
CPPHA is potent and selective positive allosteric modulator (PAM) of the mGluR5 and mGluR1 (metabotropic glutamate receptor). CPPHA can potentiate responses of mGluR5 and mGluR1 to activation of these receptors. CPPHA is developed for the research of central nervous system disorders .
|
-
- HY-W909149
-
-
- HY-42849
-
-
- HY-42849A
-
-
- HY-W362839
-
|
|
5-HT Receptor
|
Neurological Disease
|
|
Binospirone is a 5-HT1A Receptor agonist. Binospirone has anxiolytic activity. Binospirone can be used in the study of movement disorders .
|
-
- HY-101367A
-
|
|
5-HT Receptor
|
Neurological Disease
|
|
GR 55562 dihydrochloride is a selective 5-HT1B receptor antagonist. GR 55562 dihydrochloride can be used for the research of nerve disease .
|
-
- HY-P3043
-
|
|
Opioid Receptor
|
Neurological Disease
|
|
Bilaid A is a μ-opioid receptor agonist that can be extracted from Penicillium. The Ki value is 3.1 μM. Bilaid A can be used in pain research .
|
-
- HY-W010869
-
|
|
5-HT Receptor
|
Neurological Disease
|
|
GR 55562 hydrochloride is a selective 5-HT1B receptor antagonist. GR 55562 hydrochloride can be used for the research of nerve disease .
|
-
- HY-163728
-
-
- HY-76711
-
|
|
Opioid Receptor
|
Cancer
|
|
Naltrexone is an antagonist of Opioid receptor. Naltrexone inhibits cell proliferation in vivo. Naltrexone reduces tumor growth by interfering with cell signalling and modifying the immune system .
|
-
- HY-128038
-
|
|
Opioid Receptor
|
Neurological Disease
|
|
N-Desmethyl-loperamide is a major metabolite of loperamide, a drug that selectively activates peripheral μopioid receptors with a Ki value of 0.16 nM. N-Desmethyl-loperamide is a substrate of the ATP-dependent efflux transporter P-glycoprotein .
|
-
- HY-B1551
-
|
Benzononatine
|
Sodium Channel
|
Neurological Disease
|
|
Benzonatate (Benzononatine) is a peripheral oral antitussive that dampens the activity of cough stretch receptors. Benzonatate has sodium channel-blocking properties and local anesthetic effects on the respiratory stretch receptors due to a tetracaine-like metabolite .
|
-
- HY-108057
-
|
RG3487 free base
|
nAChR
5-HT Receptor
|
Neurological Disease
|
|
Facinicline (RG3487) is an orally active nicotinic α7 receptor partial agonist, with a Ki of 6 nM for α7 human nAChR. Facinicline improves cognition and sensorimotor gating in rodents. Facinicline hydrochloride shows high affinity (antagonist) to 5-HT3Rs with a Ki value of 1.2 nM .
|
-
- HY-107668
-
|
|
nAChR
|
Neurological Disease
|
|
TC-1698 dihydrochloride is a selective α7 nicotinic acetylcholine receptors agonist with EC50 value of 0.16 μM and 0.46 μM for monkey α7 nicotinic receptor and human α7 nicotinic receptor, respectively. TC-1698 dihydrochloride improves memory and has neuroprotective effects. TC-1698 dihydrochloride can be used for Alzheimer's disease research .
|
-
- HY-107668A
-
|
|
nAChR
|
Neurological Disease
|
|
TC-1698 is a selective α7 nicotinic acetylcholine receptors agonist with EC50 value of 0.16 μM and 0.46 μM for monkey α7 nicotinic receptor and human α7 nicotinic receptor, respectively. TC-1698 improves memory and has neuroprotective effects. TC-1698 can be used for Alzheimer's disease research .
|
-
- HY-N7312
-
|
(-)-Ditryptophenaline
|
Neurokinin Receptor
|
Inflammation/Immunology
|
|
Ditryptophenaline ((-)-Ditryptophenaline) is the metabolites of Aspergillus flavus. Ditryptophenaline inhibits substance P receptor and has anti-inflammatory activity .
|
-
- HY-150138
-
|
GV 150526
|
iGluR
|
Neurological Disease
|
|
Gavestinel (GV 150526) is a selective and potent the glycine site of the NMDA receptor antagonist. Gavestinel has neuroprotectant effects .
|
-
- HY-101165R
-
|
|
iGluR
|
Neurological Disease
|
|
Cyclothiazide (Standard) is the analytical standard of Cyclothiazide. This product is intended for research and analytical applications. Cyclothiazide, a positive allosteric modulator of AMPA receptors, is used frequently to block the desensitization of both native and heterologously expressed AMPA receptors. Cyclothiazide is known to produce a fast inhibition of AMPA receptor desensitization and a much slower potentiation of the AMPA current .
|
-
- HY-139727A
-
|
|
Adrenergic Receptor
|
Cardiovascular Disease
|
|
S(-)-Bisoprolol fumarate is a S(-)-enantiomer of Bisoprolol fumarate. Bisoprolol fumarate is a potent, selective and orally active β1-adrenergic receptor blocker. Bisoprolol has little activity on β2-receptor and has the potential for hypertension, coronary artery disease and stable ventricular dysfunction research .
|
-
- HY-139727
-
|
|
Adrenergic Receptor
|
Cardiovascular Disease
|
|
S(-)-Bisoprolol is a S(-)-enantiomer of Bisoprolol. Bisoprolol is a potent, selective and orally active β1-adrenergic receptor blocker. Bisoprolol has little activity on β2-receptor and has the potential for hypertension, coronary artery disease and stable ventricular dysfunction research .
|
-
- HY-14128
-
|
SB-723620
|
CRFR
|
Neurological Disease
|
|
NBI-34041 (SB-723620) is a selective and orally active nonpeptide CRF1 receptor antagonist with an IC50 of 58.9 nM and a Ki of 4.0 nM for human CRF1 receptor. NBI-34041 has no inhibitory effect on the CRF2 receptor. NBI-34041 can be used for depression and anxiety disorders research.
|
-
- HY-P3676
-
|
|
Neuropeptide Y Receptor
|
Neurological Disease
|
|
Neuropeptide Y (3-36) (porcine) is an agonist of neuropeptide Y (NPY) receptor subtype Y2, and stimulates feeding in rats. Neuropeptide Y (3-36) (porcine) is a highly Y2 selective ligand compared with nselective Y1/Y2 receptor ligand, Neuropeptide Y 1-36 .
|
-
- HY-124539
-
|
|
iGluR
|
Neurological Disease
|
|
ZK 187638 is an AMPA receptor antagonist. ZK 187638 antagonizes the kainate-induced currents in cultured hippocampal neurons with an IC50 of 3.4 μM in a noncompetitive fashion .
|
-
- HY-119739
-
|
|
GCGR
|
Metabolic Disease
Cancer
|
|
Skyrin is an anthraquinone compound that can be isolated from almond fruit. Skyrin is a receptor-selective glucagon antagonist. Skyrin can inhibit the growth of tumor cells .
|
-
- HY-19429A
-
-
- HY-N0050
-
|
(+)-Allomatrine
|
Others
|
Neurological Disease
|
|
Allomatrine ((+)-Allomatrine) is an alkaloid from the bark of Sophora japonica. Allomatrine has antinociceptive properties mediated mainly through the activation ofκ-opioid receptors .
|
-
- HY-100047
-
|
|
Taste Receptor
|
Others
|
|
Nα,Nα-Bis(carboxymethyl)-L-lysine is a competitive inhibitor of bitter taste receptor 4, with an IC50 of 59 nM. Nα,Nα-Bis(carboxymethyl)-L-lysine can be used in bitter receptors related study .
|
-
- HY-W843885
-
|
L-α-Glutamyl-L-threonine
|
CaSR
|
Others
|
|
H-Glu-Thr-OH (L-α-Glutamyl-L-threonine) is a dipeptide made up of two amino acids—glutamic acid (Glu) and threonine (Thr)—connected by a peptide bond, and it acts as an agonist for the extracellular calcium-sensing receptor (CaSR) .
|
-
- HY-13204B
-
|
KL 373 lactate
|
mAChR
|
Neurological Disease
|
|
Biperiden (KL 373) lactate is an orally active non-selective muscarinic receptor antagonist that competitively binds to M1 muscarinic receptors. Biperiden (KL 373) lactate inhibits acetylcholine and enhances dopamine signaling in the central nervous system. Biperiden (KL 373) lactate has the potential for the research of Parkinson's disease and other related psychiatric disorders .
|
-
- HY-13204AR
-
|
|
mAChR
|
Neurological Disease
|
|
Biperiden (Standard) is the analytical standard of Biperiden. This product is intended for research and analytical applications. Biperiden (KL 373) is a non-selective muscarinic receptor antagonist that competitively binds to M1 muscarinic receptors, thereby inhibiting acetylcholine and enhancing dopamine signaling in the central nervous system. Biperiden has the potential for the research of Parkinson's disease and other related psychiatric disorders .
|
-
- HY-119103
-
|
|
5-HT Receptor
|
Neurological Disease
|
|
PF-03246799 (PF-3246799) is a potent and selective 5-HT2C receptor agonist with an EC50 of 190 nM and a Ki of 160 nM. PF-03246799 shows selectivity for 5-HT2C over 5-HT2A and 5-HT2B receptors. PF-03246799 has the potential for stress urinary incontinence (SUI) research .
|
-
- HY-P2034
-
-
- HY-105604
-
-
- HY-119191
-
|
|
Adenosine Receptor
|
Neurological Disease
|
|
KF26777 (free base) is a potent and selective adenosine A3 receptor antagonist with an Ki value of 0.2 nM and possesses 9000-, 2350- and 3100-fold selectivity against adenosine A1, A2A and A2B receptors, respectively. KF26777 (free base) potently inhibits the [125I]AB-MECA binding to adenosine A3 receptors. KF26777 (free base) is promising for research of brain ischemia and inflammatory disease including asthma .
|
-
- HY-10886
-
|
|
Opioid Receptor
|
Neurological Disease
|
|
MCOPPB is an orally active and selective agonist of Nociceptin/Orphanin FQ–Receptor. MCOPPB inhibits signaling through the NOP receptor in the mouse brain. MCOPPB is used in anxiety disorders research .
|
-
- HY-103110
-
ST1936
1 Publications Verification
|
5-HT Receptor
Adrenergic Receptor
|
Neurological Disease
|
|
ST1936 is a selective, nanomolar affinity 5-HT6 receptor agonist with Ki values of 13 nM, 168 nM and 245 nM for human 5-HT6, 5-HT7 and 5-HT2B receptors, respectively. ST1936 also shows moderate affinity (Ki of 300 nM) for human and rat α2 adrenergic receptor .
|
-
- HY-141468
-
|
β-CNA dihydrochloride
|
Opioid Receptor
|
Neurological Disease
|
|
β-Chlornaltrexamine dihydrochloride (β-CNA dihydrochloride) is a potent long-term opioid receptor blocker. β-Chlornaltrexamine dihydrochloride can effectively block the inhibitory effect of κ opioid receptor agonists on dopamine release. β-Chlornaltrexamine dihydrochloride can be used to study the mechanism of pain perception .
|
-
- HY-118409
-
|
|
Androgen Receptor
|
Endocrinology
Cancer
|
|
VPC-3033 is an androgen receptor antagonist. VPC-3033 has a strong androgen DHT replacement potency (IC50: 0.625-2.5 μM), can effectively inhibit androgen receptor transcriptional activity (IC50=0.3 μM), and has a strong androgen receptor degradation ability. In addition, VPC-3033 exhibits significant anti-androgen receptor activity against prostate cancer cells resistant to Enzalutamide (HY-70002) .
|
-
- HY-19365
-
AB-MECA
1 Publications Verification
|
Adenosine Receptor
|
Neurological Disease
|
|
AB-MECA is a high affinity A3 adenosine receptor agonist with a binding Ki of 430.5 nM for human A3 receptors in CHO cells. AB-MECA can enhance plasma histamine level .
|
-
- HY-W041308
-
|
Kathon 930
|
GnRH Receptor
|
Endocrinology
|
|
DCOIT is a representative isothiazolinone that stimulates the gonadotropin-releasing hormone receptor (GnRHR)-mediated synthesis of follicle-stimulating hormone and luteinizing hormone in the brain. DCOIT interferes with G protein-coupled receptors, MAPK and Ca 2+ signaling cascades .
|
-
- HY-120396
-
|
|
5-HT Receptor
|
Neurological Disease
|
|
LY 293284 is a potent and selective 5-HT1A receptor agonist. LY 293284 results in a significant drop in core temperature and consumes more food in cholestasis rat induced by bile duct resection .
|
-
- HY-153471
-
-
- HY-B1161A
-
|
(+)-Methoprene; (7S)-Methoprene
|
Cannabinoid Receptor
|
Others
|
|
S-Methoprene is an insect juvenile hormone analog and effective insecticide that blocks the transition from pupa to adult. S-Methoprene is also a CB(1) receptor ligand and inhibits the binding of the CB1 receptor antagonist [ 3H]CP-55940 to the CB1 receptor (IC50: 19.31 μM) .
|
-
- HY-P3584A
-
|
(Pro3) Gastric Inhibitory Peptide, human TFA
|
Insulin Receptor
|
Metabolic Disease
|
|
(Pro3) GIP, human TFA is an efficacious, stable and specific human GIP receptor (hGIPR) full agonist. (Pro3) GIP, human TFA has high binding affinity for human GIPR with Ki/ Kd value of 0.90 nM. (Pro3) GIP, human TFA human can be used for the research of obesity-related diabetes .
|
-
- HY-120519
-
-
- HY-79576
-
|
Oestrone methyl ether; 3-O-Methylestrone
|
Drug Intermediate
|
Cancer
|
|
Estrone 3-methyl ether (Oestrone methyl ether; 3-O-Methylestrone) is a synthetic intermediate useful for synthesis of estrogen receptor modulator .
|
-
- HY-101986C
-
|
AR-H 053591 dihydrochloride
|
Neuropeptide Y Receptor
|
Neurological Disease
|
|
BIIE-0246 dihydrochloride (AR-H 053591 dihydrochloride) is a potent and highly selective non-peptide neuropeptide Y (NPY) Y2 receptor antagonist, with an IC50 value of 15 nM .
|
-
- HY-W344044
-
-
- HY-103136
-
-
- HY-125972
-
-
- HY-105793
-
|
|
mAChR
|
Neurological Disease
|
|
Mazaticol is an anticholinergic agent. Mazaticol blocks the muscarinic acetylcholine receptors and cholinergic nerve activity. Mazaticol is a potent 3H-QNB and 3H-PZ binding inhibitor, can bind to the M2 receptors with high affinity. Mazaticol exhibits inhibitory effects on dopamine uptake in the striatal nerve terminal. Mazaticol can be used for parkinsonian syndrome research .
|
-
- HY-101962
-
|
|
Insulin Receptor
|
Metabolic Disease
|
|
HNMPA is a membrane impermeable insulin receptor tyrosine kinase inhibitor. HNMPA inhibits serine and tyrosine autophosphorylation by the human insulin receptor. HNMPA has no effect on protein kinase C or cyclic AMP-dependent protein kinase activities
|
-
- HY-103110A
-
|
|
5-HT Receptor
Adrenergic Receptor
|
Neurological Disease
|
|
ST1936 oxalate is a selective, nanomolar affinity 5-HT6 receptor agonist with Ki values of 13 nM, 168 nM and 245 nM for human 5-HT6, 5-HT7 and 5-HT2B receptors, respectively. ST1936 oxalate also shows moderate affinity (Ki of 300 nM) for human and rat α2 adrenergic receptor .
|
-
- HY-107669
-
|
|
nAChR
|
Neurological Disease
|
|
nAChR-IN-1 (hydrochloride) is a tetramethylpiperidine heptanoate, a selective nicotinic acetylcholine receptor (nAChR) inhibitor that inhibits nAChRs lacking α5, α6, or β3 subunits. nAChR-IN-1 has the effect of preventing nerve disorder, can be used for nicotinic acetylcholine receptor dysfunction or neurological disorders research .
|
-
- HY-119802R
-
|
|
Adrenergic Receptor
|
Cardiovascular Disease
|
|
Practolol (Standard) is the analytical standard of Practolol. This product is intended for research and analytical applications. Practolol is a potent and selective β1-adrenergic receptor antagonist. Practolol can be used for the research of cardiac arrhythmias .
|
-
- HY-14542C
-
|
CP-88059 mesylate
|
5-HT Receptor
Dopamine Receptor
|
Neurological Disease
|
|
Ziprasidone (CP-88059) mesylate is an orally active combined 5-HT and dopamine receptor antagonist . Ziprasidone mesylate has affinities for Rat D2 (Ki=4.8 nM), 5-HT2A (Ki=0.42 nM) and 5-HT1A (Ki=3.4 nM) .
|
-
- HY-108057A
-
|
RG3487 hydrochloride
|
nAChR
5-HT Receptor
|
Neurological Disease
|
Facinicline hydrochloride (RG3487 hydrochloride) is an orally active nicotinic α7 receptor partial agonist, with a Ki of 6 nM for α7 human nAChR. Facinicline hydrochloride (RG3487 hydrochloride) improves cognition and sensorimotor gating in rodents. Facinicline hydrochloride (RG3487 hydrochloride) shows high affinity (antagonist) to 5-HT3Rs with a Ki value of 1.2 nM .
|
-
- HY-17407
-
|
CP 88059 hydrochloride monohydrate
|
5-HT Receptor
Dopamine Receptor
|
Neurological Disease
|
|
Ziprasidone (CP-88059) hydrochloride monohydrate is an orally active combined 5-HT and dopamine receptor antagonist . Ziprasidone hydrochloride monohydrate has affinities for Rat D2 (Ki=4.8 nM), 5-HT2A (Ki=0.42 nM) and 5-HT1A (Ki=3.4 nM) .
|
-
- HY-113683
-
|
AZD7268
|
Opioid Receptor
|
Neurological Disease
|
|
AZ 12488024 (AZD7268) is a SNC80 (HY-101202) derivative and a δ-opioid receptor agonist. AZ 12488024 is available for research into major depressive disorder .
|
-
- HY-124501
-
|
p-NH2-PE-TFMPP
|
5-HT Receptor
|
Neurological Disease
|
|
LY 165163 is a potent 5-HT presynaptic receptor agonist. LY 165163 significantly decreases 5-HTP accumulation and increases DOPA accumulation in the cortex and striatum .
|
-
- HY-101106
-
|
|
RAR/RXR
|
Neurological Disease
Cancer
|
|
AR7 is an atypical RARA/RARα (retinoic acid receptor, alpha) antagonist. AR7 specifically activates chaperone-mediated-autophagy (CMA) activity without affecting macroautophagy .
|
-
- HY-168363
-
|
WE-973
|
GABA Receptor
|
Neurological Disease
|
|
Ciclotizolam (WE-973) is a thienotriazolodiazepine with anticonvulsant and anti-aggressive activities. Ciclotizolam binds to benzodiazepine receptors in the central nervous system. Ciclotizolam decreases total sleep time in cats .
|
-
- HY-124830
-
|
|
Others
|
Cancer
|
|
SPA70 is a potent and selective antagonist of human pregnane X receptor (hPXR), with an IC50 of 540 nM (Ki=390 nM). SPA70 can enhance the chemosensitivity of cancer cells .
|
-
- HY-111323
-
|
|
ROR
|
Neurological Disease
|
|
ASN06917370 is a former orphan receptor GPR17 ligand for the study of neurodegenerative diseases. ASN06917370 has an EC50 of 268 pM in [35S]GTPyS experiments .
|
-
- HY-103221
-
-
- HY-117184
-
-
- HY-14551
-
|
SR142801
|
Neurokinin Receptor
|
Neurological Disease
|
|
Osanetant (SR142801) is a selective NK3 receptor antagonist. Osanetant produces anxiolytic- and antidepressant-like effects and is researched for schizophrenia .
|
-
- HY-105010
-
-
- HY-14551C
-
|
SR142801 monohydrochloride
|
Neurokinin Receptor
|
Neurological Disease
|
|
Osanetant (SR142801) monohydrochloride is a selective NK3 receptor antagonist. Osanetant monohydrochloride produces anxiolytic- and antidepressant-like effects .
|
-
- HY-10419A
-
-
- HY-101626A
-
|
|
Sigma Receptor
|
Neurological Disease
|
|
Sigma-LIGAND-1 hydrochloride is a selective sigma receptor ligand with an IC50s of 16 nM, 19 nM at the DTG site and the PPP site, respectively. Sigma-LIGAND-1 hydrochloride has a Ki of 4000 nM at the dopamine D2 receptor .
|
-
- HY-101626
-
|
|
Sigma Receptor
|
Neurological Disease
|
|
Sigma-LIGAND-1 is a selective sigma receptor ligand with an IC50s of 16 nM, 19 nM at the DTG site and the PPP site, respectively. Sigma-LIGAND-1 has a Ki of 4000 nM at the dopamine D2 receptor .
|
-
- HY-W795507
-
|
|
Adrenergic Receptor
5-HT Receptor
|
Neurological Disease
|
|
Cyanopindolol is an β3-adrenoceptor antagonist. Cyanopindolol is a potent and selective antagonist at the presynaptic serotonin autoreceptor in the rat brain cortex. Cyanopindolol has binding affinity for 5-HT1A and 5-HT1B receptor (Ki: 2.1 and 3 nM respectively) .
|
-
- HY-107725A
-
|
|
Neuropeptide Y Receptor
|
Metabolic Disease
|
|
BIBO3304 (diTFA) is an orally effective and selective neuropeptide Y (NPY) Y1 receptor antagonist. BIBO3304 (diTFA) has a high affinity for both human and rat Y1 receptors, with IC50 values of 0.38 and 0.72 nM, respectively. BIBO3304 (diTFA) promotes bone-tendon healing through the Wnt/β-catenin signaling pathway .
|
-
- HY-P0036B
-
|
SMS 201-995 pamoate
|
Somatostatin Receptor
Apoptosis
|
Cardiovascular Disease
Inflammation/Immunology
Endocrinology
Cancer
|
|
Octreotide (SMS 201-995) pamoate is a somatostatin receptor agonist and synthetic octapeptide endogenous somatostatin analogue. Octreotide pamoate can bind to the somatostatin receptors which are mainly subtypes 2, 3 and 5. Octreotide pamoate increases Gi activity and reduces intracellular cAMP production. Octreotide pamoate has antitumor activity, mediates apoptosis and may also be used in disease studies in acromegaly .
|
-
- HY-P0036
-
|
SMS 201-995
|
Somatostatin Receptor
Apoptosis
|
Cardiovascular Disease
Inflammation/Immunology
Endocrinology
Cancer
|
|
Octreotide (SMS 201-995) is a somatostatin receptor agonist and synthetic octapeptide endogenous somatostatin analogue. Octreotide (SMS 201-995) can bind to the somatostatin receptor and mainly subtypes 2, 3, and 5, increases Gi activity, and reduces intracellular cAMP production. Octreotide (SMS 201-995) has antitumor activity, mediates apoptosis and may also be used in disease studies in acromegaly .
|
-
- HY-N9326
-
|
|
Phosphatase
|
Metabolic Disease
|
|
Uralenol is a natural PTP1B inhibitor (IC50=21. 5 μM) from Broussonetia papyrifera. PTP1B have been shown to play a major role in the dephosphorylation of the insulin receptor in many cellular and biochemical studies .
|
-
- HY-12288
-
|
RPC-1063
|
LPL Receptor
|
Neurological Disease
Inflammation/Immunology
|
|
Ozanimod (RPC-1063), a sphingosine 1-phosphate (S1P) receptor modulator that binds with high affinity selectively to S1P receptor subtypes 1 (S1P1) and 5 (S1P5). Ozanimod has modulate effect for hS1P1 and hS1P5 receptor with EC50s of 1.03 nM and 8.6 nM, respectively. Ozanimod can be used for the research of relapsing multiple sclerosis (MS) .
|
-
- HY-12288A
-
|
RPC-1063 hydrochloride
|
LPL Receptor
|
Neurological Disease
Inflammation/Immunology
|
|
Ozanimod (RPC-1063) hydrochloride, a sphingosine 1-phosphate (S1P) receptor modulator that binds with high affinity selectively to S1P receptor subtypes 1 (S1P1) and 5 (S1P5). Ozanimod hydrochloride has modulate effect for hS1P1 and hS1P5 receptor with EC50s of 1.03 nM and 8.6 nM, respectively. Ozanimod hydrochloride can be used for the research of relapsing multiple sclerosis (MS) .
|
-
- HY-108972
-
-
- HY-121453R
-
|
|
Adenosine Receptor
|
Cardiovascular Disease
|
|
Bamifylline (hydrochloride) (Standard) is the analytical standard of Bamifylline (hydrochloride). This product is intended for research and analytical applications. Bamifylline hydrochloride is a drug in the chemical class of xanthine that acts as a selective adenosine A1 receptor antagonist .
|
-
- HY-111258
-
-
- HY-17497S
-
-
- HY-114706
-
|
MDL-26479
|
GABA Receptor
|
Neurological Disease
|
|
Suritozole (MGL-26479) is a cognitive enhancer that acts as a partial inverse agonist of benzodiazepine receptor sites on GABAA ion channel complexes. Suritozole can be used in the study of neurodegenerative diseases .
|
-
- HY-124030
-
|
|
Drug Metabolite
|
Neurological Disease
|
|
3-Hydroxyphenazepam is an active metabolite of Cinazepam. Cinazepam is a GABAA receptor agonist. 3-Hydroxyphenazepam can inhibit synaptosomal transporter-mediated [ 3H]GABA uptake .
|
-
- HY-W077477
-
|
|
5-HT Receptor
|
Neurological Disease
|
|
IHCH-7113 (Compound 166) is an agonist of 5-HT2A serotonin receptor with antidepressant activity. IHCH-7113 is promising for research of antipsychotic agent .
|
-
- HY-14542B
-
|
CP-88059 mesylate trihydrate
|
5-HT Receptor
Dopamine Receptor
|
Neurological Disease
|
|
Ziprasidone (CP-88059) mesylate trihydrate is an orally active combined 5-HT and dopamine receptor antagonist . Ziprasidone mesylate trihydrate has affinities for Rat D2 (Ki=4.8 nM), 5-HT2A (Ki=0.42 nM) and 5-HT1A (Ki=3.4 nM) .
|
-
- HY-150204
-
-
- HY-119605
-
|
|
GABA Receptor
|
Neurological Disease
|
|
DAA-1097 is an orally active and selective agonist for the peripheral benzodiazepine receptor (PBR). DAA-1097 has anxiolytic effects .
|
-
- HY-12237
-
|
(±)-SKF-38393 hydrobromide
|
Dopamine Receptor
|
Neurological Disease
|
|
SKF 38393 ((±)-SKF-38393) hydrobromide is a selective agonist of the dopamine D1 receptor (D1DR) with an IC50 of 110 nM .
|
-
- HY-100945
-
|
|
mAChR
|
Neurological Disease
|
|
Nitrocaramiphen hydrochloride is a selective M1 receptor antagonist (Ki: 5.5 nM). Nitrocaramiphen Hydrochloride inhibits the hyperpolarizing effect of muscarine in the muscle fibers .
|
-
- HY-110312
-
|
K201 fumarate
|
Calcium Channel
|
Cardiovascular Disease
|
|
JTV-519 fumarate (K201 fumarate) is a Ca 2+-dependent blocker of sarcoplasmic reticulum Ca 2+-stimulated ATPase (SERCA) and a partial agonist of ryanodine receptors in striated muscle. JTV-519 fumarate is a cardioprotective agent with antiarrhythmic effects .
|
-
- HY-19888
-
|
|
P2X Receptor
|
Inflammation/Immunology
|
|
GSK-1482160 is an orally available negative allosteric modulator of the P2X7 receptor. P2X7 receptors are involved in the production of pro-inflammatory cytokines, such as Il-1β, by central and peripheral immune cells. GSK-1482160 has the potential for the research of inflammation diseases .
|
-
- HY-107556
-
|
|
Histamine Receptor
|
Neurological Disease
|
|
VUF 5681 dihydrobromide is a neutral antagonist of histamine H3 receptor. VUF 5681 dihydrobromide also has partial agonist function of H3 receptor. VUF 5681 dihydrobromide blocks the effects of Thioperamide (HY-12206). VUF 5681 dihydrobromide is used in central nervous system disease research .
|
-
- HY-115613
-
ML-180
1 Publications Verification
SR1848
|
Orphan Receptor
|
Cancer
|
|
ML-180 (SR1848) is a potent orphan nuclear receptor liver receptor homolog 1 (LRH-1; NR5A2) inverse agonist with an IC50 of 3.7 μM. ML-180 is inactive for steroidogenic factor-1 (SF-1; NR5A1; IC50>10 μM). ML-180 has the potential for LRH-1-dependent cancers .
|
-
- HY-130221
-
|
Dafachronic acid A; Δ7-Dafachronic acid
|
Insecticide
|
Others
|
|
(25S)-Δ7-Dafachronic acid is a ligand and activator of DAF-12 receptor. DAF-12 is a nuclear hormone receptor that regulates larval diapause, developmental age, and adult longevity in Caenorhabditis elegans .
|
-
- HY-110003
-
|
ACPA
|
Cannabinoid Receptor
|
Neurological Disease
|
|
Arachidonylcyclopropylamide (ACPA) is a potent and selective CB1 receptors agonist. Arachidonylcyclopropylamide inhibits forskolin-stimulated cAMP production in CHO cells transfected with human cannabinoid CB1 receptors (IC50=2 nM) .
|
-
- HY-B2089
-
-
- HY-106224
-
|
Hypocretin-1 (human, rat, mouse)
|
Orexin Receptor (OX Receptor)
|
Neurological Disease
|
|
Orexin A (human, rat, mouse) (Hypocretin-1 (human, rat, mouse)), a 33 amino acid excitatory neuropeptide, orchestrates diverse central and peripheral processes. Orexin A (human, rat, mouse) binds and activates two types of G protein-coupled receptors, the orexin-1 receptor (OX1R) and the orexin-2 receptor (OX2R). Orexin A (human, rat, mouse) has a role in the regulation of feeding behavior. Orexin A (human, rat, mouse) is an effective anti-nociceptive and anti-hyperalgesic agent in mice and rats .
|
-
- HY-P2199
-
-
- HY-W040146R
-
|
|
Dopamine Receptor
|
Neurological Disease
|
|
Propionylpromazine (hydrochloride) (Standard) is the analytical standard of Propionylpromazine (hydrochloride). This product is intended for research and analytical applications. Propionylpromazine hydrochloride (Propiopromazine hydrochloride), a dopamine receptor D2 (DRD2) antagonist, can be used in the research of Parkinson disease .
|
-
- HY-128128
-
-
- HY-131822
-
|
Uridine-5'-O-monophosphorothioate
|
P2Y Receptor
|
Cancer
|
|
5'-UMPS (Uridine-5'-O-monophosphorothioate) is a P2Y14 receptor agonist. 5'-UMPS can induce HeLa cell growth slightly .
|
-
- HY-129436
-
-
- HY-P2537
-
|
|
HIV
Apelin Receptor (APJ)
|
Others
|
|
Apelin-12 is one of the most potent C-terminal fragments of the polypeptide that possesses a high affinity to orphan receptor APJ receptor. Apelin-12 is involved in the regulation of body fluid homeostasis and in the central control of feeding. Apelin-12 blocks HIV-1 entry through APJ receptor. Apelin-12 exerts neuroprotective effect .
|
-
- HY-P3044
-
|
|
Opioid Receptor
|
Neurological Disease
|
|
Bilaid A1e (Compound 1e) is a tetrapeptide agonist of the µ-opioid receptor (Ki = 750 nM). Bilaid A1e can be isolated from an Australian estuarine isolate of Penicillium sp. Bilaid A1e can be used for pain research .
|
-
- HY-P10148
-
|
Ac-[Leu28,31]-NPY (24-36)
|
Neuropeptide Y Receptor
|
Neurological Disease
|
|
N-Acetyl [Leu28, Leu31] neuropeptide Y (24–36) is a selective agonist of neuropeptide Y Y2 receptor. N-Acetyl [Leu28, Leu31] neuropeptide Y (24–36) attenuates cardiac vagal action in anaesthetised rats .
|
-
![N-Acetyl [Leu28, Leu31] neuropeptide Y (24–36)](//file.medchemexpress.com/product_pic/hy-p10148.gif)
- HY-B1505A
-
-
- HY-19022
-
-
- HY-121008
-
-
- HY-17032A
-
|
(rac)-AS1069562 hydrochloride; YM-08054
|
5-HT Receptor
|
Neurological Disease
|
|
Indeloxazine hydrochloride is a 5-HT receptor and norepinephrine (NE) reuptake inhibitor. Indeloxazine hydrochloride is an antidepressant and cerebral activator .
|
-
- HY-W015169
-
-
- HY-W015169A
-
|
|
5-HT Receptor
Endogenous Metabolite
|
Neurological Disease
Cancer
|
|
5-Methoxytryptamine hydrochloride, a metabolite of Melatonin, is a nonselective 5-HT receptor agonist. 5-Methoxytryptamine hydrochloride has no affinity for the 5-HT3 receptor. 5-Methoxytryptamine hydrochloride is also a potent antioxidant and has radioprotective action .
|
-
- HY-14542
-
|
CP-88059
|
5-HT Receptor
Dopamine Receptor
|
Neurological Disease
|
|
Ziprasidone (CP-88059), an orally active antipsychotic agent, is a combined 5-HT and dopamine receptor antagonist . Ziprasidone mesylate trihydrate has affinities for Rat D2 (Ki=4.8 nM), 5-HT2A (Ki=0.42 nM) and 5-HT1A (Ki=3.4 nM) .
|
-
- HY-123854
-
|
|
IRAK
|
Inflammation/Immunology
|
|
PF-06426779 is a potent and selective inhibitor of interleukin‑1 receptor associated kinase 4 (IRAK4), with an IC50 of 0.3 nM .
|
-
- HY-30234S
-
|
|
Histamine Receptor
HCV
TRP Channel
|
Cancer
|
|
Clemizole-d4 is a deuterium labeled Clemizole. Clemizole is an H1 histamine receptor antagonist, is found to substantially inhibit HCV replication .
|
-
- HY-143259
-
|
|
LXR
|
Cancer
|
|
BE1218 is a liver X receptor (LXR) inverse agonist with IC50 values of 9 nM and 7 nM against LXRα and LXRβ, respectively .
|
-
- HY-101341
-
|
|
5-HT Receptor
|
Neurological Disease
|
|
RS 67333 hydrochloride is a potent and selective 5-HT4 receptor (5-HT4R) partial agonist with a pKi of 8.7 in guinea-pig striatum. RS 67333 hydrochloride exhibits lower affinities at several other receptors including 5-HT1A, 5-HT1D, 5-HT2A, 5-HT2C, dopamine D1, D2 and muscarinic M1-M3 receptors. RS 67333 hydrochloride has neuroprotective effects, and can be used for Alzheimer's disease research .
|
-
- HY-100406
-
|
(+)-MCPG
|
mGluR
|
Neurological Disease
|
|
(S)-MCPG ((+)-MCPG) is a potent group I/II metabotropic glutamate receptor (mGluRs) antagonist and the active isomer of (RS)-MCPG (HY-100371) . (S)-MCPG can be used for the study of the function of mGluRs in spatial learning .
|
-
- HY-106444A
-
|
MPV-1730 hydrochloride; JP-1730 hydrochloride
|
Adrenergic Receptor
|
Neurological Disease
|
|
Fipamezole hydrochloride is a potent and orally active α2-adrenergic receptor antagonist with Ki values of 9.2 nM, 17 nM, and 55 nM for human α2A, α2B, and α2C, receptors, respectively. Fipamezole hydrochloride is an anti-dyskinetic agent, and can be used for the study of Parkinson's disease .
|
-
- HY-155001
-
|
|
c-Fms
|
Others
|
|
CSF1R-IN-15 (compound 23) is an inhibitor targeting CSF1R. The colony-stimulating factor-1 receptor (CSF1R) is a tyrosine kinase embedded in the cell membrane of macrophages. The receptor is activated by colony-stimulating factor-1 (CSF-1) and interleukin-34, and signaling via CSF1R is crucial for the differentiation, proliferation, and survival of macrophages .
|
-
- HY-P1302
-
|
|
Opioid Receptor
|
Neurological Disease
|
|
Orphanin FQ(1-11), a orphanin FQ or nociceptin (OFQ/N) fragment, is a potent NOP receptor (ORL-1; OP4) agonist, with a Ki of 55 nM. Orphanin FQ(1-11) has no affinity for μ, δ, κ1 and κ3 receptors (Ki>1000 nM). Orphanin FQ(1-11) is analgesic in CD-1 mice .
|
-
- HY-161692
-
|
|
Estrogen Receptor/ERR
|
Cancer
|
|
ERα degrader 8 (Compound 18j) is a selective Estrogen Receptor degrader. ERα degrader 8 is degrader to MCF-7 cells with IC50 value of 0.15 μM .
|
-
- HY-164394
-
|
|
c-Met/HGFR
|
Cancer
|
|
EMD 1204831 is a potent and highly selective c-Met inhibitor which selectively suppresses the c-Met receptor tyrosine kinase activity with an IC50 of 9 nM. EMD 1204831 can be utilized in cancer research .
|
-
- HY-112071
-
|
|
Adrenergic Receptor
|
Cardiovascular Disease
|
|
Prenalterol is a selective β1-adrenergic receptor agonist. Prenalterol has no effect on gut smooth muscle contractile activity. Prenalterol can be used for researching cardiovascular disease .
|
-
- HY-147533
-
|
|
ROR
|
Inflammation/Immunology
|
|
RORγt inverse agonist 30 (Compound 1) is a potent RORγt inverse agonist with the IC50 of 46 nM. Targeting the nuclear receptor RORγt is effective in autoimmune disorders .
|
-
- HY-13607
-
|
|
Androgen Receptor
|
Cancer
|
|
BMS-641988 (compound 23) is an oral active nonsteroidal androgen receptor antagonist with the Ki of 1.7 nM. BMS-641988 shows anticancer activity .
|
-
- HY-132259
-
|
ABT-414
|
Antibody-Drug Conjugates (ADCs)
EGFR
|
Cancer
|
|
Depatuxizumab mafodotin is an antibody-drug conjugate (ADC) that specifically targets the epidermal growth factor receptor (EGFR). Depatuxizumab mafodotin can be used for cancer research .
|
-
- HY-B1478
-
|
|
Histamine Receptor
NO Synthase
|
Endocrinology
|
|
Dimaprit dihydrochloride is a selective histamine H2 receptor agonist, it also inhibits nNOS with an IC50 of 49 μM. Dimaprit dihydrochloride can stimulate gastric acid secretion .
|
-
- HY-104026B
-
-
- HY-10307A
-
|
DMP 754
|
Integrin
|
Cardiovascular Disease
|
Roxifiban (acetate) is the acetate form of Roxifiban (HY-10307). Roxifiban (acetate) is a platelet glycoprotein (GP) IIb/IIIa receptor inhibitor that can be used in research related to angina .
|
-
- HY-105962
-
|
Eresepine
|
Others
|
Others
|
|
Erizepine is an octopamine receptor class 3 (OAR3) antagonist with a Ki of 474 nM. Erizepine can be utilized in insect research .
|
-
- HY-N10301
-
|
|
Toll-like Receptor (TLR)
|
Infection
|
|
Guignardone L is a metabolite isolated from the endophytic fungus Guignardia mangiferae with toll-like receptor 3 regulating activity .
|
-
- HY-P10920
-
|
|
Drug Derivative
|
Cancer
|
|
DOTAMTATE is a somatostatin analogue. DOTAMTATE marked 212Pb is promising for research of somatostatin receptor positive neuroendocrine tumors .
|
-
- HY-100794
-
|
|
5-HT Receptor
|
Neurological Disease
|
|
GR127935 hydrochloride is a potent and orally active 5-HT1D and 5-HT1B receptor antagonist with pKis of 8.5 for both isoforms. GR127935 hydrochloride has 100-fold selectivity for 5-HT1B/1D receptors over 5-HT1A, 5-HT2A, and 5-HT2C receptors. GR127935 hydrochloride can be used in neurological disease research .
|
-
- HY-106224A
-
|
Hypocretin-1 (human, rat, mouse) (TFA)
|
Orexin Receptor (OX Receptor)
|
Neurological Disease
|
|
Orexin A (human, rat, mouse) (Hypocretin-1 (human, rat, mouse)) TFA, a 33 amino acid excitatory neuropeptide, orchestrates diverse central and peripheral processes. Orexin A (human, rat, mouse) TFA binds and activates two types of G protein-coupled receptors, the orexin-1 receptor (OX1R) and the orexin-2 receptor (OX2R). Orexin A (human, rat, mouse) TFA has a role in the regulation of feeding behavior. Orexin A (human, rat, mouse) TFA is an effective anti-nociceptive and anti-hyperalgesic agent in mice and rats .
|
-
- HY-107562A
-
|
|
Histamine Receptor
|
Neurological Disease
|
|
JNJ-10181457 is a selective non-imidazole histamine H3 receptor antagonist that normalizes acetylcholine neurotransmission . JNJ-10181457 is a click chemistry reagent, it contains an Alkyne group and can undergo copper-catalyzed azide-alkyne cycloaddition (CuAAc) with molecules containing Azide groups.
|
-
- HY-B1115AR
-
|
|
5-HT Receptor
Dopamine Receptor
Reactive Oxygen Species
|
Neurological Disease
Cancer
|
|
Buspirone (Standard) is the analytical standard of Buspirone. This product is intended for research and analytical applications. Buspirone is an orally active 5-HT1A receptor agonist, and a dopamine D2 autoreceptorsant antagonist. Buspirone is an anxiolytic agent, and can be used for the generalized anxiety disorder research .
|
-
- HY-103200
-
-
- HY-100672
-
-
- HY-P1302A
-
|
|
Opioid Receptor
|
Neurological Disease
|
|
Orphanin FQ(1-11) TFA, a orphanin FQ or nociceptin (OFQ/N) fragment, is a potent NOP receptor (ORL-1; OP4) agonist, with a Ki of 55 nM. Orphanin FQ(1-11) TFA has no affinity for μ, δ, κ1 and κ3 receptors (Ki>1000 nM). Orphanin FQ(1-11) TFA is analgesic in CD-1 mice .
|
-
- HY-160264
-
|
|
PROTACs
Estrogen Receptor/ERR
|
Cancer
|
|
PROTAC ER Degrader-12 (Compound 70) is an estrogen receptor PROTAC degrader (DC50: <10 nM), and inhibits MCF-7 proliferation (DC50: <10 nM). PROTAC ER Degrader-12 has anticancer effect. Pink: ER ligand (HY-169978); Blue: E3 ligase ligand (HY-138793); Black: linker (HY-30756) .
|
-
- HY-110186
-
|
|
Adenosine Receptor
|
Metabolic Disease
|
|
PQ-69 is a potent and selective adenosine A1 receptor antagonist with inverse agonist activity. PQ-69 binds to hA1 receptor with a Ki value of 0.96 nM, is 217-fold more selective compared with hA2A receptors (Ki=208 nM) and >1,000-fold selectivity over hA3 receptor (Ki >100 μM). PQ-69 can be used for the research of renal dysfunction .
|
-
- HY-119943
-
|
|
Dopamine Receptor
|
Neurological Disease
|
|
PF-06256142 is a potent, selective, CNS-penetrant and orally active agonist of the D1 receptor, with an EC50 and Ki of 33 nM and 12 nM, respectively. PF-06256142 has the potential for the research of schizophrenia and Parkinson's disease .
|
-
- HY-P4779
-
|
|
Androgen Receptor
|
Neurological Disease
|
|
Acetyl-ACTH (2-24) (human, bovine, rat) is a fragment of proopiomelanocortin (POMC) peptide. POMC peptides such as adrenocorticotrophin (ACTH), which is the precursor of α-MSH, is also an agonist at the MC-1 receptor .
|
-
- HY-129103
-
|
|
Dopamine Receptor
|
Neurological Disease
|
|
A-412997 is a selective Dopamine D4 agonist with Ki values of 12 and 7.9 nM for the rat and human receptors. A-412997 improves short term memory and cognitive properties in rodent models .
|
-
- HY-P10327
-
|
|
GLP Receptor
|
Metabolic Disease
|
|
PP18 is a novel OXM-based dual GLP-1 and glucagon receptor agonist with EC50 values of 0.487 nM target hGLP-1R and 0.188 nM target hGcgR .
|
-
- HY-122168
-
|
|
Prostaglandin Receptor
|
Inflammation/Immunology
|
|
AAT-008 is a potent, selective, and orally active prostaglandin EP4 receptor antagonist with Kis of 0.97 and 6.1 nM for recombinant human EP4 and recombinant rat EP4, respectively .
|
-
- HY-136654
-
|
|
Opioid Receptor
|
Neurological Disease
|
|
LPK-26 hydrochloride is a selective kappa-opioid receptor agonist with a Ki of 0.68 nM. LPK-26 exhibits potent antinociceptive effects with low physical dependence potential and can be utilized in relevant research .
|
-
- HY-P4782
-
|
|
Androgen Receptor
|
Neurological Disease
|
|
Acetyl-ACTH (3-24) (human, bovine, rat) is a fragment of proopiomelanocortin (POMC) peptide. POMC peptides such as adrenocorticotrophin (ACTH), which is the precursor of α-MSH, is also an agonist at the MC-1 receptor .
|
-
- HY-169114
-
|
|
5-HT Receptor
Phospholipase
|
Cardiovascular Disease
|
|
Goxalapladib is a 5-HT6 receptor modulator that blocks lipoprotein-associated phospholipase A2 (Lp-PLA2) activity. Goxalapladib is promising for research of atherosclerosis-associated cardiovascular diseases .
|
-
- HY-119061
-
|
|
5-HT Receptor
|
Neurological Disease
|
|
SB-357134 is a potent, selective, brain penetrant, and orally active 5-HT6 receptor antagonist. SB-357134 enhances memory and learning and increases seizure threshold in rats .
|
-
- HY-156972
-
|
|
Opioid Receptor
|
Metabolic Disease
|
|
NOP agonist-1(compound 4) is a nociceptin opioid receptor (NOP) partial agonist. NOP agonist-1attenuate parkinsonian disabilities in 6-OHDA hemilesioned rats .
|
-
- HY-P4784
-
|
|
Androgen Receptor
|
Neurological Disease
|
|
Acetyl-ACTH (4-24) (human, bovine, rat) is a fragment of proopiomelanocortin (POMC) peptide. POMC peptides such as adrenocorticotrophin (ACTH), which is the precursor of α-MSH, is also an agonist at the MC-1 receptor .
|
-
- HY-130176
-
|
|
Opioid Receptor
ERK
Adenylate Cyclase
|
Neurological Disease
|
|
UFP-512 is a selective and potent σ-opioid receptor (DOP receptor) peptidic agonist with antidepressant- and anxiolytic-like effects. UFP-512 exhibits as a potent agonist on adenylyl cyclase inhibition and Erk1/2 activation. UFP-512 induces phosphorylation of DOP receptors on Ser 363 with a low desensitization of the cAMP pathway. UFP-512 is promising for research of mood disorders .
|
-
- HY-107534
-
|
|
GnRH Receptor
|
Endocrinology
|
|
AG-045572 is a GnRH receptor antagonist with Kis of 6.0 nM and 3.8 nM for human and rat GnRH receptor, respectively. AG-045572 is metabolized by CYP3A and ressuppresses testosterone .
|
-
- HY-12288R
-
|
|
LPL Receptor
|
Neurological Disease
Inflammation/Immunology
|
|
Ozanimod (Standard) is the analytical standard of Ozanimod. This product is intended for research and analytical applications. Ozanimod (RPC-1063), a sphingosine 1-phosphate (S1P) receptor modulator that binds with high affinity selectively to S1P receptor subtypes 1 (S1P1) and 5 (S1P5). Ozanimod has modulate effect for hS1P1 and hS1P5 receptor with EC50s of 1.03 nM and 8.6 nM, respectively. Ozanimod can be used for the research of relapsing multiple sclerosis (MS) .
|
-
- HY-118520
-
|
|
Prostaglandin Receptor
|
Endocrinology
|
|
16-Phenoxy tetranor Prostaglandin F2α methyl ester is a metabolically stable form of Prostaglandin F2α that can binds to FP receptor. 16-Phenoxy tetranor Prostaglandin F2α methyl ester serves as prodrug that can be hydrolyzed to generate bioactive free acid .
|
-
- HY-B1551R
-
|
|
Sodium Channel
|
Neurological Disease
|
|
Benzonatate (Standard) is the analytical standard of Benzonatate. This product is intended for research and analytical applications. Benzonatate (Benzononatine) is a peripheral oral antitussive that dampens the activity of cough stretch receptors. Benzonatate has sodium channel-blocking properties and local anesthetic effects on the respiratory stretch receptors due to a tetracaine-like metabolite .
|
-
- HY-W001909
-
|
|
nAChR
|
Metabolic Disease
|
|
Myosmine, a specific tobacco alkaloid in nuts and nut products, has low affinity for a4b2 nicotinic acetylcholinergic receptors (nAChR) with a Ki of 3300 nM .
|
-
- HY-156601
-
|
LP352
|
5-HT Receptor
|
Neurological Disease
|
|
Bexicaserin (LP352) is a 5-HT2C receptor agonist with potential for studying obesity and psychiatric-related disorders (such as epilepsy) .
|
-
- HY-115854
-
|
|
GABA Receptor
|
Neurological Disease
|
|
Ro 15-1310 is an imidazobenzodiazepine that exhibits high affinity and selectivity for alpha 5-containing GABAA receptors. Ro 15-1310 is promising for research of convulsions .
|
-
- HY-W335976
-
|
|
5-HT Receptor
|
Cancer
|
|
Almotriptan hydrochloride is a selective agonist of 5-HT 1B/1D Receptor. Almotriptan hydrochloride can used in study of migraine attacks .
|
-
- HY-123442
-
-
- HY-160020
-
|
|
Androgen Receptor
|
Cancer
|
|
ET516 is a potent inhibitor of Androgen Receptor. ET516 significantly inhibits the proliferation and tumor growth of prostate cancer cells expressing AR-resistant mutants .
|
-
- HY-P3267
-
|
|
Transferrin Receptor
|
Others
|
|
Holo-Bovine Transferrin, a blood-plasma glycoprotein, is a target ligand for transferrin receptor. Holo-Bovine Transferrin can bind to and mediate the transport of iron .
|
-
- HY-124204
-
|
|
iGluR
|
Neurological Disease
|
|
LY 274614 is an orally active, competitive NMDA receptor antagonist. LY 274614 can be used for Neurological Disease study .
|
-
- HY-70002B
-
|
MDV3100 carboxylic acid
|
Drug Metabolite
|
Cancer
|
|
Enzalutamide carboxylic acid (MDV3100 carboxylic acid) is an inactive metabolite of Enzalutamide (MDV3100). Enzalutamide is an androgen receptor (AR) antagonist .
|
-
- HY-A0158
-
|
|
Glucocorticoid Receptor
|
Inflammation/Immunology
|
|
Diflorasone act as a corticosteroid hormone receptor agonist with anti-inflammatory and immunosuppressive properties. Diflorasone enters the cell by diffusion across the cell membrane and binds to the glucocorticoid receptor (GR) in the cytoplasm. Diflorasone is used for the research of skin diseases such as eczema or psoriasis .
|
-
- HY-A0215
-
|
BW-A 938U; Nuromax
|
nAChR
|
Neurological Disease
|
|
Doxacurium chloride (BW A938U) is a potent non-depolarizing neuromuscular blocking agent. Doxacurium chloride binds to cholinergic receptors to antagonize acetylcholine, resulting in a block of neuromuscular transmission. Doxacurium chloride can be used for the research of neurological diseases .
|
-
- HY-112469
-
|
|
ERK
Insulin Receptor
|
Metabolic Disease
|
|
ERK Inhibitor II (Negative control) is an effective inhibitor of extracellular signal-regulated kinase (ERK). ERK Inhibitor II (Negative control) inhibits the activation of insulin receptor, which can be used in the study of diabetes .
|
-
- HY-147203
-
|
|
5-HT Receptor
|
Cardiovascular Disease
Metabolic Disease
Endocrinology
Cancer
|
|
5-HT2B antagonist-1 is an orally active 5-HT2B receptor antagonist with an IC50 value of 33.4 nM. 5-HT2B antagonist-1 can be used in studies of diseases characterized by 5-HT2B receptor signaling, such as hepatocellular carcinoma, cardiovascular disease or gastrointestinal disease .
|
-
- HY-400897
-
|
|
Ligands for Target Protein for PROTAC
EBI2/GPR183
|
Cancer
|
|
7α,25-Dihydroxycholesterol intermediate-1 is an intermediate in the synthesis of 7α,25-Dihydroxycholesterol (HY-113962). 7α,25-Dihydroxycholesterol (7α,25-OHC) can be used as a ligand to target the orphan GPCR receptor EBI2 (GPR183). body, used to synthesize the corresponding PROTEACs .
|
-
- HY-114072
-
|
|
Opioid Receptor
|
Neurological Disease
|
|
J-113397 is the first potent and selective nonpeptidyl ORL1 receptor antagonist (Ki: cloned human ORL1=1.8 nM) without any agonistic effects on other opioid receptors .
|
-
- HY-106444
-
|
MPV 1730; JP-1730
|
Adrenergic Receptor
|
Neurological Disease
|
|
Fipamezole (MPV 1730; JP-1730) is a potent and orally active α2-adrenergic receptor antagonist with Ki values of 9.2 nM, 17 nM, and 55 nM for human α2A, α2B, and α2C, receptors, respectively. Fipamezole is an anti-dyskinetic agent, and can be used for the study of Parkinson's disease .
|
-
- HY-W653723R
-
|
|
Androgen Receptor
|
Endocrinology
|
|
N-Nitrosodicyclohexylamine (Standard) is the analytical standard of N-Nitrosodicyclohexylamine. This product is intended for research and analytical applications. N-Nitrosodicyclohexylamine (NDCHA) is a N-nitrosocompound with anti-androgenic activities. N-Nitrosodicyclohexylamine shows the competitive binding to androgen receptor (AR) against 5α-dihydrotestosterone and decreased the level of AR protein .
|
-
- HY-151129
-
|
|
nAChR
|
Neurological Disease
|
|
nAChR-IN-1 (2,2,6,6-Tetramethylpiperidin-4-yl heptanoate) is a tetramethylpiperidine heptanoate, a selective nicotinic acetylcholine receptor (nAChR) inhibitor that inhibits nAChRs lacking α5, α6, or β3 subunits. nAChR-IN-1 has the effect of preventing nerve disorder, can be used for nicotinic acetylcholine receptor dysfunction or neurological disorders research .
|
-
- HY-15997C
-
|
(±)-Trans-(1R,2R)-U-50488 hydrate hydrochloride
|
Opioid Receptor
|
Neurological Disease
|
|
(±)-U-50488 ((±)-Trans-(1R,2R)-U-50488) hydrate hydrochloride is a selective κ opioid receptor (KOR) agonist .
|
-
- HY-103290
-
|
|
Bradykinin Receptor
|
Others
|
|
R715 is a selective bradykinin B1 receptor antagonist. R715 significantly attenuates the hyperalgesic effect developed in Streptozotocin(HY-13753)-diabetic mice .
|
-
- HY-15997B
-
|
(±)-Trans-(1R,2R)-U-50488 hydrochloride
|
Opioid Receptor
|
Neurological Disease
|
|
(±)-U-50488 ((±)-Trans-(1R,2R)-U-50488) hydrochloride is a selective κ opioid receptor (KOR) agonist .
|
-
- HY-90010
-
|
Kabi-2234; PNU-200583E
|
mAChR
|
Neurological Disease
Cancer
|
|
Tolterodine Tartrate (Kabi-2234; PNU-200583E) is a potent muscarinic receptor antagonist and shows selectivity for the urinary bladder over salivary glands in vivo.
|
-
- HY-122620
-
|
Hetrombopag (tautomerism); SHR-8735 (tautomerism)
|
Thrombopoietin Receptor
|
Inflammation/Immunology
Cancer
|
|
Rafutrombopag (tautomerism) is a potent thrombopoietin receptor agonist. Rafutrombopag (tautomerism) is efficacious and well tolerated with a manageable safety profile. Rafutrombopag (tautomerism) has the potential for the research of immune thrombocytopenia .
|
-
- HY-122230
-
|
|
Integrin
|
Cardiovascular Disease
|
|
UR-3216 is a selective, and orally active platelet surface glycoprotein (GPIIb/IIIa) receptor antagonist. UR-3216 has the potential for cardiovascular diseases research .
|
-
- HY-123376
-
-
- HY-A0191
-
|
(+)-Brompheniramine; (S)-Brompheniramine
|
Endogenous Metabolite
Histamine Receptor
|
Inflammation/Immunology
|
|
Dexbrompheniramine is an orally active H1 receptor antagonist. Dexbrompheniramine is an antihistamine that reduces the effects of natural chemical histamine. Dexbrompheniramine can be used for the research of hay fever and urticaria .
|
-
- HY-N3072
-
|
|
Opioid Receptor
|
Neurological Disease
|
|
Picraline is a natural alkaloid that targets opioid receptors with binding affinities with Ki values of 132 μM, 2.38 μM and 98.8 μM for μOR, κOR and δOR, respectively .
|
-
- HY-164863
-
|
|
Biochemical Assay Reagents
|
Others
|
|
β-GalNAc-PEG4-Azide is an asialoglycoprotein receptor ligand with PEG4 linker and azide group that can be utilized in onward click chemistry .
|
-
- HY-A0191A
-
|
(+)-Brompheniramine maleate; (S)-Brompheniramine maleate
|
Endogenous Metabolite
Histamine Receptor
|
Inflammation/Immunology
|
|
Dexbrompheniramine maleate is an orally active H1 receptor antagonist. Dexbrompheniramine maleate is an antihistamine that reduces the effects of natural chemical histamine. Dexbrompheniramine maleate can be used for the research of hay fever and urticaria .
|
-
- HY-14338A
-
|
Lu AE58054 hydrochloride
|
5-HT Receptor
|
Neurological Disease
|
|
Idalopirdine hydrochloride (Lu AE58054 hydrochloride) is a potent, selective 5-HT6 receptor antagonist with a Ki value of 0.83 nM. Idalopirdine hydrochloride may be used in studies of Alzheimer's disease and schizophrenia, among other related disorders .
|
-
- HY-130226
-
-
- HY-14338
-
|
Lu AE58054
|
5-HT Receptor
|
Neurological Disease
|
|
Idalopirdine (Lu AE58054 ) is a potent, selective 5-HT6 receptor antagonist with a Ki value of 0.83 nM. Idalopirdine may be used in studies of Alzheimer's disease and schizophrenia, among other related disorders .
|
-
- HY-17407R
-
|
|
5-HT Receptor
Dopamine Receptor
|
Neurological Disease
|
|
Ziprasidone (hydrochloride monohydrate) (Standard) is the analytical standard of Ziprasidone (hydrochloride monohydrate). This product is intended for research and analytical applications. Ziprasidone (CP-88059) hydrochloride monohydrate is an orally active combined 5-HT and dopamine receptor antagonist . Ziprasidone hydrochloride monohydrate has affinities for Rat D2 (Ki=4.8 nM), 5-HT2A (Ki=0.42 nM) and 5-HT1A (Ki=3.4 nM) .
|
-
- HY-116020
-
|
|
Dopamine Receptor
|
Neurological Disease
|
|
FAUC 365 is a highly dopamine D3 receptor-selective antagonist with Ki values of 0.5 nM, 340, 2600, and 3600 nM at D3, D4.4, D2short, and D2Long receptors, respectively. FAUC 365 can be used for the research of schizophrenia, and Parkinson's disease .
|
-
- HY-12560A
-
|
|
nAChR
5-HT Receptor
|
Neurological Disease
|
|
PNU-282987 is a potent α7 nicotinic acetylcholine receptor (nAChR) agonist with an EC50 of 154 nM. PNU-282987 is also a functional antagonist of the 5-HT3 receptor with an IC50 of 4541 nM. PNU-282987 can be used for the research of central and peripheral nervous systems .
|
-
- HY-123206
-
|
|
5-HT Receptor
|
Inflammation/Immunology
|
|
R-96544 (free base) is a potent, selective and competitive 5-HT2 receptor antagonist. R-96544 (free base) inhibits platelet aggregation induced by serotonin, and inhibits 5-HT2A receptor-mediated contraction of guinea pig trachea .
|
-
- HY-123310
-
|
|
Androgen Receptor
|
Cancer
|
|
JNJ-26146900 is a potent and orally active androgen receptor antagonist with a Ki value of 400nM for rat AR. JNJ-26146900 is a nonsteroidal androgen receptor (AR) ligand. JNJ-26146900 reduces prostate tumor size and prevents bone loss. JNJ-26146900 can be used in research of cancer .
|
-
- HY-15997A
-
|
(+)-Trans-(1R,2R)-U-50488 hydrochloride
|
Opioid Receptor
|
Neurological Disease
|
|
(+)-U-50488 (hydrochloride) (+)-Trans-(1R,2R)-U-50488 hydrochloride) is a less active κ opioid receptor (KOR) agonist than the enantiomer of (-)-Trans-(1S,2S)-U-50488 (HY-15997) .
|
-
- HY-P5896
-
-
- HY-122153
-
-
- HY-B1067B
-
|
Phenazoline phosphate
|
Histamine Receptor
|
Neurological Disease
|
|
Antazoline phosphate is an H1 receptor antagonist that affects the activity of the central nervous system, has a potent antiarrhythmic effect .
|
-
- HY-101588
-
|
MK-7264; AF-219
|
P2X Receptor
|
Inflammation/Immunology
|
|
Gefapixant is an orally active and potent purinergic P2X3 receptor (P2X3R) antagonist, with IC50 values of ~30 nM versus recombinant hP2X3 homotrimers and 100-250 nM at hP2X2/3 heterotrimeric receptors. Gefapixant can be used for the research of chronic cough and knee osteoarthritis .
|
-
- HY-76711R
-
|
|
Opioid Receptor
|
Cancer
|
|
Naltrexone (Standard) is the analytical standard of Naltrexone. This product is intended for research and analytical applications. Naltrexone is an antagonist of Opioid receptor. Naltrexone inhibits cell proliferation in vivo. Naltrexone reduces tumor growth by interfering with cell signalling and modifying the immune system .
|
-
- HY-130842
-
|
β-NF-CH2-Br
|
E3 Ligase Ligand-Linker Conjugates
|
Cancer
|
|
β-Naphthoflavone-CH2-Br (β-NF-CH2-Br) is an arylhydrocarbon receptor (AhR) ligand. β-Naphthoflavone-CH2-Br can be used to synthesize the PROTAC β-NF-JQ1(HY-130256) .
|
-
- HY-W926789
-
-
- HY-129759
-
|
|
Cholecystokinin Receptor
|
Inflammation/Immunology
|
|
KSG-504 (anhydrous) is a CCK receptor antagonist. KSG-504 (anhydrous) inhibits the development of Ethionine-induced acute pancreatitis in rats and facilitates the regeneration of acinar cells .
|
-
- HY-15023
-
|
PF-3274167
|
Oxytocin Receptor
|
Endocrinology
|
|
Cligosiban (PF-3274167) is an orally active, highly selective, and centrally permeable oxytocin receptor antagonist with good pharmacokinetics in rats and can inhibit physiological ejaculation in rodents [1][2].
|
-
- HY-134801
-
|
|
GPR35
|
Metabolic Disease
Inflammation/Immunology
|
|
CID1231538, a benzothiazole analog, is a potent GPR35 antagonist with no significant activity against rodent orthologs of GPR35, which is also a G protein-coupled receptor (GPCR) .
|
-
- HY-145341
-
|
|
Estrogen Receptor/ERR
|
Cancer
|
|
GNE-149 is an orally bioavailable full antagonist of estrogen receptor α (ERα; IC50=0.053 nM). GNE-149 is a selective estrogen receptor degrader (SERD). GNE-149 can be used for the research of breast cancer .
|
-
- HY-108677
-
|
|
Oxytocin Receptor
|
Endocrinology
|
|
L-368,899 hydrochloride is a potent, selective, orally bioavailable, non-peptide oxytocin receptor antagonist, with IC50s of 8.9 nM and 26 nM for rat uterus and human uterus oxytocin receptor, respectively. L-368,899 hydrochloride used as a tocolytic agent .
|
-
- HY-160001
-
-
- HY-N10887
-
|
|
GABA Receptor
|
Neurological Disease
|
|
Withasomniferolide B is a withanolide. Withasomniferolide B can be isolated from a GABAA receptor positive activator methanol extract of the roots of Withania somnifera .
|
-
- HY-137279
-
|
|
Opioid Receptor
|
Inflammation/Immunology
|
|
Naloxone methiodide is a peripherally restricted, nonselective, and competitive opioid receptor antagonist. Naloxone methiodide does not penetrate the blood-brain barrier .
|
-
- HY-W502657
-
-
- HY-B1067A
-
|
Phenazoline
|
Histamine Receptor
|
Neurological Disease
|
|
Antazoline (Phenazoline) is an H1 receptor antagonist that affects the activity of the central nervous system, has a potent antiarrhythmic effect .
|
-
- HY-123813
-
|
|
Arrestin
|
Cancer
|
|
CCX-777 is a partial agonist of β-arrestin-2 recruitment to ACKR3 (atypical chemokine receptor 3) .
|
-
- HY-D2201
-
|
|
Fluorescent Dye
|
Cancer
|
|
Fluorescent ACKR3 antagonist 1(compound 18a) is a atypical chemokine receptor 3 antagonist .
|
-
- HY-124947
-
|
|
5-HT Receptor
|
Neurological Disease
|
|
PF-4522654 is a potent, selective and brain-permeable 5-HT2C receptor agonist with an EC50 of 16 nM and a Ki of 8 nM. PF-4522654 shows no measurable functional agonism at no 5-HT2A and 5-HT2B receptors. PF-4522654 can be used for the study of stress urinary incontinence (SUI) .
|
-
- HY-101588A
-
|
MK-7264 citrate; AF-219 citrate
|
P2X Receptor
|
Inflammation/Immunology
|
|
Gefapixant citrate is an orally active and potent purinergic P2X3 receptor (P2X3R) antagonist, with IC50 values of ~30 nM versus recombinant hP2X3 homotrimers and 100-250 nM at hP2X2/3 heterotrimeric receptors. Gefapixant citrate can be used for the research of chronic cough and knee osteoarthritis .
|
-
- HY-103090
-
|
|
5-HT Receptor
|
Neurological Disease
|
|
NPS ALX Compound 4a is a potent and selective 5-hydroxytryptamine6 (5-HT6) receptor antagonist, with an IC50 of 7.2 nM and a Ki of 0.2 nM .
|
-
- HY-169127
-
|
|
5-HT Receptor
|
Neurological Disease
|
|
Seganserin is an orally active 5-HT receptor antagonist with a plasma half-life of 26.1 ± 12.9 (S.D.) h. Seganserin can be utilized in neurological research .
|
-
- HY-136896
-
-
- HY-160856
-
|
TOP05300
|
Estrogen Receptor/ERR
|
Endocrinology
|
|
TOP5300 is an orally active follicle-stimulating hormone receptor allosteric agonist. TOP5300 can induce the production of testosterone in stromal cells and promote follicular genesis and superovulation in rats .
|
-
- HY-105699
-
|
|
Adrenergic Receptor
|
Neurological Disease
|
Napamezole is an α2A adrenergic receptor antagonist and a serotonin/norepinephrine uptake inhibitor. Napamezole increases the levels of monoamines in the brain by blocking monoamine uptake, which gives it antidepressant activity .
|
-
- HY-107560
-
|
|
Histamine Receptor
|
Cancer
|
|
4-Methylhistamine (dihydrochloride) is the potent agonist of histamine 4 receptor (H4R). 4-Methylhistamine (dihydrochloride) has the potential for the research of immune-related diseases such as cancer and autoimmune disorders .
|
-
- HY-160857
-
|
|
Estrogen Receptor/ERR
|
Endocrinology
|
|
TOP5668 is an orally active follicle-stimulating hormone receptor allosteric agonist. TOP5668 can induce the production of testosterone in stromal cells and promote follicular genesis and superovulation in rats .
|
-
- HY-119389
-
-
- HY-103090A
-
|
|
5-HT Receptor
|
Neurological Disease
|
|
NPS ALX Compound 4a dihydrochloride is a potent and selective 5-hydroxytryptamine6 (5-HT6) receptor antagonist, with an IC50 of 7.2 nM and a Ki of 0.2 nM .
|
-
- HY-111006
-
|
UH 232
|
Dopamine Receptor
|
Neurological Disease
|
|
(+)-UH 232 is a partially selective agonist of the D3 receptor with an intrinsic activity of 0.2-0.4. (+)-UH 232 antagonized quinpirole-induced mitogenesis with a Ki value of 9.4 nM .
|
-
- HY-123856
-
|
|
Phosphatase
|
Neurological Disease
|
|
MY10 is a potent and orally active receptor protein tyrosine phosphatase (RPTPβ/ζ) inhibitor. MY10 attenuates binge-like ethanol consumption and ethanol reward .
|
-
- HY-14157
-
|
|
Opioid Receptor
|
Inflammation/Immunology
|
|
ADL-5747 is a selective and orally active agonist of the δ-opioid receptor (DOR). By binding to the δ-opioid receptors, ADL-5747 activates these receptors, thereby playing a role in pain management pathways. ADL-5747 can be used for research into pain management mechanisms .
|
-
- HY-14157A
-
|
|
Opioid Receptor
|
Inflammation/Immunology
|
|
ADL-5747 hydrochloride is a selective and orally active agonist of the δ-opioid receptor (DOR). By binding to the δ-opioid receptors, ADL-5747 hydrochloride activates these receptors, thereby playing a role in pain management pathways. ADL-5747 hydrochloride can be used for research into pain management mechanisms .
|
-
- HY-15541A
-
|
CP-5736 dihydrochloride
|
Histamine Receptor
|
Endocrinology
|
|
Zaltidine (CP-5736) dihydrochloride is a highly specific H2 receptor antagonist with antisecretion activity. Zaltidine dihydrochloride reduces the stimulant effect of histamine on gastric acid secretion by binding to histamine H2 receptors on gastric parietal cells, thus reducing gastric acid production. Zaltidine dihydrochloride can be used in the study of gastric acid-related diseases such as duodenal ulcers .
|
-
- HY-100369A
-
|
|
GABA Receptor
|
Neurological Disease
|
|
DMCM hydrochloride is a nonselective full inverse agonist of benzodiazepine. DMCM shows bnding afinity at human recombinant GABAA αxβ3γ2 receptor subtypes with Kis of 10 nM, 13 nM, 7.5 nM, 2.2 nM for α1, α2, α3, and α5 ?receptors, respectively .
|
-
- HY-15541
-
|
CP-57361
|
Histamine Receptor
|
Endocrinology
|
|
Zaltidine dihydrochloride (CP-5736 dihydrochloride) is a highly specific H2 receptor antagonist with antisecretion activity. Zaltidine dihydrochloride reduces the stimulant effect of histamine on gastric acid secretion by binding to histamine H2 receptors on gastric parietal cells, thus reducing gastric acid production. Zaltidine dihydrochloride can be used in the study of gastric acid-related diseases such as duodenal ulcers .
|
-
- HY-120531
-
|
|
Histamine Receptor
|
Neurological Disease
|
|
UR-PI376 is a potent and selective histamine H4 receptor (H4R) agonist with a pEC50 value of 7.47. UR-PI376 shows negligible hH1R and hH2R activities and moderate inverse agonistic activity at the hH3R .
|
-
- HY-131954
-
|
|
5-HT Receptor
|
Neurological Disease
|
|
5-HT3 antagonist 4 is a 5-HT3 receptor (5HT3R) antagonist. 5-HT3 antagonist 4 prevents diabetes-induced depressive phenotypes in mice .
|
-
- HY-111044
-
|
|
Androgen Receptor
|
Cancer
|
|
(+)-JNJ-37654032 is an orally active and selective androgen receptor modulator. (+)-JNJ-37654032 can be used in the study of muscle-wasting diseases .
|
-
- HY-132294
-
|
|
Estrogen Receptor/ERR
|
Cancer
|
|
GNE-502 is an orally active and potent degrader for estrogen receptor (ER). GNE-502 can be used for the research of breast cancer .
|
-
- HY-163171
-
|
|
Chloride Channel
|
Neurological Disease
|
|
ARN 11391 is a selective enhancer of inositol triphosphate receptor type 1 (ITPR1). ARN 11391 can be used in the study of spinocerebellar ataxia .
|
-
- HY-111232
-
|
|
GHSR
|
Metabolic Disease
|
|
GSK894281 is an orally active and highly potent ghrelin receptor full agonist with a pEC50 of <4.9 at the human motilin receptor. GSK894281 effectively enters the CNS. GSK894281 has the potential for constipation or to assist in emptying the colon prior to colonoscopy or colon surgery research .
|
-
- HY-P10395
-
-
- HY-103162
-
|
|
Adenosine Receptor
|
Neurological Disease
|
|
ANR94 is a potent and selective adenosine A2A receptor (AA2AR) antagonist with an Ki of 46 nM for hAA2AR. ANR94 has the potential for the research of Parkinson's disease .
|
-
- HY-12200
-
|
GSK189254
|
Histamine Receptor
|
Neurological Disease
|
|
GSK189254A hydrochloride is a novel, potent and selective histamine H3 receptor antagonist with pKi values of 9.59-9.90 and 8.51-9.17 for human and rat H3, respectively .
|
-
- HY-146110
-
|
|
Parasite
|
Infection
|
|
RyRs activator 2 (compound 7o) is a potent activator of ryanodine receptors (RyRs). RyRs activator 2 is 30% larvicidal activity, comparable to chlorantraniliprole (30%) and better than cyantraniliprole (10%) .
|
-
- HY-116586
-
|
|
Sigma Receptor
|
Neurological Disease
|
|
AF710B is a highly potent and selective allosteric M1 muscarinic and σ1 receptor agonist. AF710B can be used for the research of Alzheimer’s disease .
|
-
- HY-100552
-
|
|
5-HT Receptor
|
Neurological Disease
|
|
VUF10166 is a potent and high-affinity 5-HT3 receptor antagonist, with Ki values of 0.04 nM (5-HT3A) and 22 nM (5-HT3AB). VUF10166 inhibits 5-HT-induced responses at 5-HT3A and 5-HT3AB receptors at nanomolar concentrations. At 5-HT3 receptor, VUF10166 at higher concentrations also acts as a partial agonist, with an EC50 of 5.2 μM .
|
-
- HY-P1345
-
|
|
Complement System
|
Neurological Disease
Endocrinology
|
|
TLQP-21, a VGF-derived peptide endowed of endocrine and extraendocrine properties, is a potent G-protein-coupled receptor complement-3a receptor 1 (C3aR1) agonist (EC50: mouse TLQP-21=10.3 μM; human TLQP-21=68.8 μM). TLQP-21 activates C3aR1 to induce an increase of intracellular Ca 2+. TLQP-21 is used for the research in regulation of nociception and other relevant physiologic functions .
|
-
- HY-109106A
-
|
|
CaSR
|
Endocrinology
|
|
Upacicalcet sodium is an intravenous calcimimetic agent. Upacicalcet suppresses excessive parathyroid hormone (PTH) secretion, thereby lowering blood PTH levels, by acting directly on parathyroid cell membrane calcium-sensing receptors. Upacicalcet can be used for researching the disease of secondary hyperparathyroidism (SHPT) .
|
-
- HY-109106
-
|
|
CaSR
|
Endocrinology
|
|
Upacicalcet is an intravenous calcimimetic agent. Upacicalcet suppresses excessive parathyroid hormone (PTH) secretion, thereby lowering blood PTH levels, by acting directly on parathyroid cell membrane calcium-sensing receptors. Upacicalcet can be used for researching the disease of secondary hyperparathyroidism (SHPT) .
|
-
- HY-118463
-
|
|
Neurokinin Receptor
|
Neurological Disease
|
|
Benzomalvin A is a potent antagonist of neurokinin receptor isolated from Penicillium sp. Benzomalvin A shows inhibitory activity against substance P with Ki values of 12, 42 and 43 μM at the guinea pig, rat and human neurokinin NK1 receptors, respectively .
|
-
- HY-B2089R
-
|
|
5-HT Receptor
Dopamine Receptor
|
Neurological Disease
Metabolic Disease
|
|
Cinitapride (Standard) is the analytical standard of Cinitapride. This product is intended for research and analytical applications. Cinitapride is a nonselective 5-HT1 and 5-HT4 receptors agonist and a 5-HT2 and D2 antagonist. Cinitapride can be used in functional dyspepsia (FD) and gastroesophageal reflux disease (GERD) research .
|
-
- HY-12560
-
|
|
nAChR
5-HT Receptor
|
Neurological Disease
|
|
PNU-282987 (free base) is a potent α7 nicotinic acetylcholine receptor (nAChR) agonist with an EC50 of 154 nM. PNU-282987 (free base) is also a functional antagonist of the 5-HT3 receptor with an IC50 of 4541 nM. PNU-282987 (free base) can be used for the research of central and peripheral nervous systems .
|
-
- HY-12959A
-
|
BAY x 3702
|
5-HT Receptor
|
Neurological Disease
|
|
Repinotan hydrochloride (BAY x 3702) is a potent, selective, brain-penetrant and orally active 5-HT1A receptor agonist, with Ki values of 0.19 nM (calf hippocampus), 0.25 nM (rat and human cortex), and 0.59 nM (rat hippocampus Repinotan hydrochloride has a weak affinity for other related receptors. Repinotan hydrochloride has pronounced neuroprotective effects .
|
-
- HY-137225
-
-
- HY-119943A
-
|
|
Dopamine Receptor
|
Neurological Disease
|
|
(Rac)-PF-06256142 is the less effective enantiomer of PF-06256142 (HY-119943). (Rac)-PF-06256142 is an agonist of D1 receptor, with an EC50 of 107 nM. (Rac)-PF-06256142 can be used for the research of schizophrenia and Parkinson's disease .
|
-
- HY-133014
-
|
|
RIP kinase
|
Inflammation/Immunology
|
|
RIP2 kinase inhibitor 1 (compound 11) is a potent and selective receptor interacting protein 2 (RIP2) kinase inhibitor with an IC50 of 0.03 μM for RIP2 FP. RIP2 kinase inhibitor 1 is used for autoinflammatory disorders .
|
-
- HY-W414823
-
|
|
LXR
HMG-CoA Reductase (HMGCR)
|
Metabolic Disease
|
|
24,25-Epoxycholesterol is an oxysterol agonist of the liver X receptor that can inhibit the activity of 3-hydroxy-3-methylglutaryl-CoA reductase (HMG-CoA reductase) in liver cells. 24,25-Epoxycholesterol regulates cholesterol metabolism in the liver .
|
-
- HY-101327
-
|
Corwin; ICI 118587
|
Adrenergic Receptor
|
Cardiovascular Disease
|
|
Xamoterol is a selective and potent agonist of beta1-adrenergic receptor. Xamoterol has the potential for the research of arrhythmogenesis. Xamoterol has the potential for the investigating the relationship between β1-adrenergic stimulation and IKr .
|
-
- HY-167674
-
|
|
Endogenous Metabolite
|
Neurological Disease
|
|
Bmapn is a synthetic cathinone. Bmapn has rewarding and reinforcing properties, decreases dopamine transporter and increases dopamine receptor D2 gene expression in the striatum .
|
-
- HY-122164
-
|
|
iGluR
|
Neurological Disease
|
|
LY-503430 is an orally active AMPA receptor positive allosteric modulator (PAM). LY-503430 can be used for the study of Parkinson's disease .
|
-
- HY-P2497
-
|
|
GCGR
|
Neurological Disease
|
|
Exendin (5-39) is a potent glucagon-like peptide 1 (GLP-1) receptor antagonist. Exendin (5-39) improves memory impairment in β-amyloid protein-treated rats .
|
-
- HY-133113
-
|
|
5-HT Receptor
|
Neurological Disease
|
|
7-Desmethyl-agomelatine is a metabolite of Agomelatine. Agomelatineis a potent agonist at melatonin receptors (MT1 and MT2), and also is an antagonist of 5-HT2C .
|
-
- HY-W062700
-
|
|
JAK
|
Neurological Disease
|
|
STS-E412 is a selective activator of tissue-protective EPO receptor (including EPOR and CD131). STS-E412 can be used for research of neurodegenerative diseases and organ protection .
|
-
- HY-B1337
-
|
|
nAChR
Endogenous Metabolite
|
Cancer
|
|
Choline chloride is an essential nutrient that activates alpha7 nicotinic receptors and has analgesic and anti-inflammatory activity. Glycerophosphoinositol choline can affect diseases such as liver disease, atherosclerosis and neurological disorders .
|
-
- HY-49382
-
|
|
Target Protein Ligand-Linker Conjugates
|
Others
|
|
Fluocinolone acetonide 3-benzylaniline (Precursor Example 1) is a glucocorticoid receptor agonist-linker conjugate, which can be used for the synthesis of anti-CD40 antibody-drug conjugates (ADCs) .
|
-
- HY-107010A
-
|
|
Adrenergic Receptor
|
Cardiovascular Disease
|
|
Esprolol hydrochloride is an orally active and potent β-adrenergic receptor antagonist. Esprolol hydrochloride undergoes rapid metabolism by blood and tissue esterases to form an active metabolite, amoxolol. Esprolol hydrochloride is promising for research of exertional angina .
|
-
- HY-103182A
-
|
|
Adenosine Receptor
|
Others
|
|
PSB-1115 potassium salt is a selective A2B Adenosine Receptor antagonist. PSB-1115 potassium salt inhibits the 2,4,6-trinitrobenzenesulfonic acid (TNBS)-induced contraction inhibition of acetylcholine (ACh) .
|
-
- HY-116524
-
|
|
5-HT Receptor
|
Neurological Disease
|
|
PF-04781340 is a potent and selective 5-HT2C receptor agonist. PF-04781340 is orally available and have central nervous system penetrant profile .
|
-
- HY-N12605
-
|
|
TRP Channel
|
Neurological Disease
|
|
hTRPA1-IN-1 (19), a norsesterterpenoid that can be isolated from the Marine Sponge Diacarnus spinipoculum, is an inhibitor of transient receptor potential Ankyrin 1 (TRPA1), with an IC50 of 2 μM .
|
-
- HY-105672
-
|
|
Adrenergic Receptor
|
Cancer
|
|
Cafaminol (Methylcoffanolamine) is a vasoconstrictor and anticatarrhal that selectively binds to alpha-1 receptors, causing blood vessels to constrict. Cafaminol is an xanthine derivative which can be utilized in decongestant and antitumor research .
|
-
- HY-147337
-
MeTC7
1 Publications Verification
|
VD/VDR
|
Cancer
|
|
MeTC7 is a Vitamin-D receptor (VDR) antagonist. MeTC7 has potent VDR inhibition activity with an IC50 value of 2.9 μM. MeTC7 shows good antitumor effects .
|
-
- HY-147276
-
|
JW1601
|
Histamine Receptor
|
Inflammation/Immunology
|
|
Izuforant (JW1601) (Compound 24) is an orally active histamine H4 receptor (H4R) antagonist with an IC50 of 36 nM against human H4R. Izuforant also shows binding affinity of human serotonin 3 receptor (h5-HT3R) with an IC50 of 9.1 μM. Izuforant exhibits strong anti-pruritic and anti-inflammatory efficacies .
|
-
- HY-106874A
-
|
RS-15385-197 hydrochloride
|
Adrenergic Receptor
|
Neurological Disease
|
|
Delequamine (RS-15385-197) hydrochloride is an orally active and selective α2-adrenergic receptor antagonist with a pKi of 9.5 for α2-adrenoceptors in rat cortex. Delequamine hydrochloride shows >1000 fold selectivity against 5-HT1A receptors and α1-adrenoceptors. Delequamine hydrochloride can be used for the study of erectile dysfunction .
|
-
- HY-106874
-
|
RS-15385-197
|
Adrenergic Receptor
|
Neurological Disease
|
|
Delequamine (RS-15385-197) is an orally active and selective α2-adrenergic receptor antagonist with a pKi of 9.5 for α2-adrenoceptors in rat cortex. Delequamine shows >1000 fold selectivity against 5-HT1A receptors and α1-adrenoceptors. Delequamine can be used for the study of erectile dysfunction .
|
-
- HY-122422
-
|
|
5-HT Receptor
|
Others
|
|
Gepirone is a selective and affinitive 5-HT1A agonist. Gepirone binds selectively to 5-HT1A receptor binding site. Gepirone acts as an antidepressant agent can be used for anxiety and major depressive disorder research .
|
-
- HY-128469
-
|
|
GABA Receptor
|
Neurological Disease
|
|
Inaperisone is a centrally acting muscle relaxant. Inaperisone can inhibit the micturition reflex by acting indirectly on GABAB receptors in the brainstem .
|
-
- HY-155672
-
|
|
5-HT Receptor
|
Neurological Disease
|
|
JPC0323 is a dual 5-HT2C/5-HT2A receptor positive allosteric modulator. JPC0323 has on-target properties, acceptable plasma exposure and brain penetration. JPC0323 can be used for the research of neurological disease .
|
-
- HY-113516
-
-
- HY-107586
-
|
DAQ B1; L-783281; Dimethylasterriquinone
|
Insulin Receptor
Akt
|
Endocrinology
|
|
Demethylasterriquinone B1 is a selective insulin receptor activator. Demethylasterriquinone B1 stimulates tyrosine phosphorylation of the IR β subunit, and the activation of PIK3 and AKT .
|
-
- HY-148349
-
-
- HY-121392
-
|
|
5-HT Receptor
|
Cardiovascular Disease
Neurological Disease
|
|
GR 125743 is a selective 5-HT1B/1D receptor antagonist, with pKis of 8.85 and 8.31 for wild-type h5-HT1B and wild-type h5-HT1D, respectively. GR 125743 is used for the research of Parkinson's disease and cardiovascular diseases .
|
-
- HY-114586
-
|
|
Angiotensin Receptor
|
Cancer
|
|
L-158809 is an angiotensin type 1 (AT1) receptor antagonist that prevents or ameliorates fractionated whole-brain irradiation-induced cognitive impairment. L-158809 is promising for research of brain tumor .
|
-
- HY-103568
-
|
|
mGluR
|
Neurological Disease
|
|
YM-298198 hydrochloride is a high-affinity, selective, orally active, and non-competitive antagonist of metabotropic glutamate receptor type 1 (mGluR1). YM-298198 hydrochloride can be used for the research of neurological disorders .
|
-
- HY-B1337B
-
-
- HY-107010
-
|
|
Adrenergic Receptor
|
Cardiovascular Disease
|
|
Esprolol is an orally active and potent β-adrenergic receptor antagonist. Esprolol is rapidly metabolized by blood and tissue esterases to form the active metabolite amoxolol. Esprolol holds potential for research in exercise-induced angina .
|
-
- HY-158179
-
|
|
Adenosine Receptor
|
Neurological Disease
|
|
A3AR agonist 3 (Compound 15A) is a A3 adenosine receptor (A3AR) agonist, with Ki and EC50 values of 2.27 and 0.20 nM for hA3 and cAMP, respectivelly. A3AR agonist 3 can be used for the research of neuroinflammation .
|
-
- HY-P1345A
-
|
|
Complement System
|
Neurological Disease
Endocrinology
|
|
TLQP-21 TFA, a VGF-derived peptide endowed of endocrine and extraendocrine properties, is a potent G-protein-coupled receptor complement-3a receptor1 (C3aR1) agonist (EC50: mouse TLQP-21=10.3 μM; human TLQP-21=68.8μM). TLQP-21 TFA activates C3aR1 to induce an increase of intracellular Ca 2+. TLQP-21 TFA is used for the research in regulation of nociception and other relevant physiologic functions .
|
-
- HY-10121
-
-
- HY-101588R
-
|
|
P2X Receptor
|
Inflammation/Immunology
|
|
Gefapixant (Standard) is the analytical standard of Gefapixant. This product is intended for research and analytical applications. Gefapixant is an orally active and potent purinergic P2X3 receptor (P2X3R) antagonist, with IC50 values of ~30 nM versus recombinant hP2X3 homotrimers and 100-250 nM at hP2X2/3 heterotrimeric receptors. Gefapixant can be used for the research of chronic cough and knee osteoarthritis .
|
-
- HY-124097
-
|
|
Insulin Receptor
|
Metabolic Disease
|
|
HNMPA-(AM)3 is a cell-permeable and selective insulin receptor tyrosine kinase inhibitor analog of HNMPA. HNMPA-(AM)3 greatly inhibits the ability of prothoracicotropic hormone (PTTH) to activate ERK phosphorylation and stimulate ecdysteroidogenesis. HNMPA-(AM)3 is also effective in inhibiting ecdysteroid production (IC50=14.2 μM) and insulin receptor activity (IC50 is 14.2 μM and 200 μM in mosquitoes and mammals, respectively) .
|
-
- HY-116281
-
|
|
Prostaglandin Receptor
|
Cardiovascular Disease
|
|
ICI D1542 is a selective and potent inhibitor of thromboxane A2 (TXA2) synthase and the thromboxane A2 receptor (TP-receptor). ICI D1542 is effective at preventing thrombus formation by redirection of arachidonic acid metabolism .
|
-
- HY-131502
-
|
|
P2X Receptor
|
Inflammation/Immunology
|
|
Taspine is a natural product with anti-inflammatory activity. Taspine suppresses P2X4 receptor activity via PI3K inhibition. Taspine inhibits pro-inflammatory signalling via inhibition of P2X4 receptors in macrophage .
|
-
- HY-148088
-
|
|
Adenosine Receptor
|
Cancer
|
|
M1069 is a selective and orall active, dual A2A/A2B adenosine receptor antagonist with a selectivity of >100 fold against the A1 and A3 receptors. M1069 counteracts immune-suppressive mechanisms of adenosine, and exhibits anti-tumor activity .
|
-
- HY-A0158R
-
|
|
Glucocorticoid Receptor
|
Inflammation/Immunology
|
|
Diflorasone (Standard) is the analytical standard of Diflorasone. This product is intended for research and analytical applications. Diflorasone act as a corticosteroid hormone receptor agonist with anti-inflammatory and immunosuppressive properties. Diflorasone enters the cell by diffusion across the cell membrane and binds to the glucocorticoid receptor (GR) in the cytoplasm. Diflorasone is used for the research of skin diseases such as eczema or psoriasis .
|
-
- HY-109106B
-
|
|
CaSR
|
Endocrinology
|
|
(Rac)-Upacicalcet is the racemate of Upacicalcet.Upacicalcet is an intravenous calcimimetic agent. Upacicalcet suppresses excessive parathyroid hormone (PTH) secretion, thereby lowering blood PTH levels, by acting directly on parathyroid cell membrane calcium-sensing receptors. Upacicalcet can be used for researching the disease of secondary hyperparathyroidism (SHPT) .
|
-
- HY-101327A
-
|
Corwin hemifumarate; ICI 118587 hemifumarate
|
Adrenergic Receptor
|
Cardiovascular Disease
|
|
Xamoterol hemifumarate is a selective and potent agonist of beta1-adrenergic receptor. Xamoterol hemifumarate has the potential for the research of arrhythmogenesis. Xamoterol hemifumarate has the potential for the investigating the relationship between β1-adrenergic stimulation and IKr .
|
-
- HY-157220
-
|
|
Vasopressin Receptor
|
Cardiovascular Disease
|
|
Tolvaptan phosphate ester sodium, a prodrug of Tolvaptan (HY-17000), can be used in the study of cardiac edema. Tolvaptan is a selective, competitive and orally active vasopressin receptor 2 (V2R) antagonist with an IC50 of 1.28 μM for the inhibition of arginine vasopressin (AVP)-induced platelet aggregation .
|
-
- HY-139690
-
|
|
Opioid Receptor
|
Cardiovascular Disease
|
|
CCG258747 is a selective GRK2 inhibitor (IC50=18 nM) with high selectivity over GRK1, GRK5, PKA, and ROCK1 (518, 83, >5500, and >550–fold, respectively).CCG258747 also blocks the internalization of the µ-opioid receptor. G protein-coupled receptor (GPCR) kinases (GRKs) are attractive targets for the research of heart failure .
|
-
- HY-103413
-
|
|
Dopamine Receptor
|
Neurological Disease
|
|
Eticlopride hydrochloride, a selective dopamine D2‐like receptor antagonist, exhibits high affinity for dopamine D2, α1‐adrenergic, α2‐adrenergic, 5HT1, 5HT2 receptors with Kis of 0.09, 112, 699, 6220, and 830 nM, respectively. Eticlopride hydrochloride is an antipsychotic agent .
|
-
- HY-14111
-
-
- HY-P1313A
-
|
GYPGQV TFA
|
Protease Activated Receptor (PAR)
|
Others
|
|
PAR 4 (1-6) TFA (GYPGQV TFA), a hexapeptide, is a fragment of protease-activated receptor 4 (PAR4). PAR 4 (1-6) TFA acts as a PAR4-specific agonist .
|
-
- HY-107579
-
|
AY 25712
|
GPR109A
|
Cardiovascular Disease
|
|
Acifran (AY 25712), an antihyperlipidemic agent, is an orally active agonist of GPR109A (HM74A) and GPR109B, the high and low affinity receptors for Niacin .
|
-
- HY-147367
-
-
- HY-111051
-
|
|
nAChR
|
Neurological Disease
|
|
JN403 is an orally active and selective α7 nicotinic acetylcholine receptor agonist. JN403 can be used in the study of central nervous system disorders .
|
-
- HY-122495
-
|
rel-LY 171555 dihydrochloride; rel-LY 141865 dihydrochloride
|
Dopamine Receptor
|
Neurological Disease
|
|
rel-Quinpirole (rel-LY 171555) dihydrochloride, an ergot compound, is a selective dopamine (DA) D2 receptor agonist. rel-Quinpirole dihydrochloride can be used for research on neurological diseases .
|
-
- HY-133858
-
|
|
5-HT Receptor
|
Neurological Disease
|
|
25N-NBOMe hydrochloride, a 2C-N derivative, is a 5-HT2A and 5-HT2C receptors agonist with Ki values of 0.144 nM and 1.06 nM, respectively. 25N-NBOMe hydrochloride has little to no efficacy at inducing release of preloaded neurotransmitter from recombinant dopamine, serotonin and norepinephrine transporters .
|
-
- HY-13222
-
|
|
Opioid Receptor
|
Neurological Disease
Cancer
|
|
BAN ORL 24 is a nociceptin/orphanin FQ (N/OFQ) peptide receptor (NOP) antagonist. BAN ORL 24 has antagonistic effect for nociceptin (NOP) receptor with KI value of 0.24 nM in CHO cell. BAN ORL 24 can be used for the research of cancer and analgesic .
|
-
- HY-N8376
-
|
(±)-Fustin; 3,7,3',4'-Tetrahydroxyflavanone
|
Amyloid-β
mAChR
Cholinesterase (ChE)
|
Neurological Disease
|
|
Fustinis ((±)-Fustin; 3,7,3',4'-Tetrahydroxyflavanone) is a potent amyloid β (Aβ) inhibitor. Fustinis ((±)-Fustin; 3,7,3',4'-Tetrahydroxyflavanone) increases the expression of acetylcholine (ACh) levels, choline acetyltransferase (ChAT) activity, and ChAT gene induced by Aβ (1-42). Fustinis ((±)-Fustin; 3,7,3',4'-Tetrahydroxyflavanone) decreases in acetyl cholinesterase (AChE) activity and AChE gene expression induced by Aβ (1-42). Fustinis ((±)-Fustin; 3,7,3',4'-Tetrahydroxyflavanone) increases muscarinic M1 receptor gene expression and muscarinic M1 receptor binding activity. Fustinis ((±)-Fustin; 3,7,3',4'-Tetrahydroxyflavanone) can be used for Alzheimer's disease research .
|
-
- HY-150067
-
|
|
Cannabinoid Receptor
|
Metabolic Disease
|
|
CB1R Allosteric modulator 5, a selective cannabinoid-1 receptor (CB1R) inverse agonist with an IC50 value of 4.2 μM and EC50 value of ＞10 μM. CB1R Allosteric modulator 5 can be used for the research of metabolic and obesity .
|
-
- HY-15522
-
|
|
Oxytocin Receptor
|
Neurological Disease
|
|
WAY-267464 is a non-peptide oxytocin receptor (OTR) agonist. WAY-267464 can impair social recognition memory in rats through a vasopressin 1A receptor antagonist action. WAY-267464 can be used for the research of psychiatric disorders, such disorders include autism spectrum disorder, schizophrenia, and social anxiety disorder .
|
-
- HY-111269
-
-
- HY-159695A
-
-
- HY-159695
-
-
- HY-139413
-
|
|
Toll-like Receptor (TLR)
|
Cancer
|
|
β-D-glucan is a natural non-digestible polysaccharide and high biocompatibility that can be selectively recognized by recognition receptors such as Dectin-1 and Toll-like receptors as well as being easily internalized by murine or human macrophages, which is likely to attribute to a target delivery . β-d-glucan is an enteric delivery vehicle for probiotics .
|
-
- HY-106039
-
|
|
iGluR
|
Neurological Disease
|
|
LY 215490 is a selective, competitive AMPA receptor antagonist against AMPA, CGSl9755 and kainate with IC50 values of 4.8, 26.4 and 247 μM, respectively. LY 215490 shows neuroprotective effects in focal ischaemia .
|
-
- HY-P0003A
-
|
Brain Natriuretic Peptide-32 human acetate; BNP-32 acetate
|
Natriuretic Peptide Receptor (NPR)
|
Cardiovascular Disease
Cancer
|
|
Nesiritide (Brain Natriuretic Peptide-32 human) acetate is an agonist of natriuretic peptide receptors (NPRs), with Kd values of 7.3 and 13 pM for NPR-A and NPR-C, respectively. Nesiritide acetate can be used for the research of heart failure .
|
-
- HY-133898
-
|
TAK-925
|
Orexin Receptor (OX Receptor)
|
Others
|
|
Danavorexton (TAK-925) is an orexin receptor agonist with brain permeability. Danavorexton induces a physiological pattern of OX2R activation in vitro to wake up sleepy mice and improve sleepiness symptoms .
|
-
- HY-P0003
-
|
Brain Natriuretic Peptide-32 human; BNP-32
|
Natriuretic Peptide Receptor (NPR)
|
Cardiovascular Disease
Cancer
|
|
Nesiritide (Brain Natriuretic Peptide-32 human) is an agonist of natriuretic peptide receptors (NPRs), with Kd values of 7.3 and 13 pM for NPR-A and NPR-C, respectively. Nesiritide can be used for the research of heart failure .
|
-
- HY-115462
-
|
|
Prostaglandin Receptor
|
Inflammation/Immunology
|
|
PGN-9856 is a selective and high affinity (pKi ≥ 8.3) ligand at EP2 receptor. PGN-9856 is a potetn and non-prostanoid EP2 receptor agonist (pEC50 ≥ 8.5). PGN-9856 shows anti-inflammatory and anti-glaucoma activities .
|
-
- HY-158882
-
|
|
Biochemical Assay Reagents
Adenosine Receptor
|
Others
|
|
FLAC6 is a potent fluorinated detergent that can be used to solubilize membrane proteins (the native adenosine receptor A2AR, a G protein-coupled receptor, and two native transporters AcrB and BmrA). FLAC6 can maintain the structural and functional integrity of different membrane proteins .
|
-
- HY-132811
-
-
- HY-P99104
-
|
COVI-AMG; STI-2020
|
SARS-CoV
|
Infection
|
|
Plutavimab a human IgG1-κ anti-SARS-CoV-2 antibody, targeting to Spike (S) glycoprotein receptor binding domain (RBD) .
|
-
- HY-N7587
-
|
|
Melanocortin Receptor
|
Metabolic Disease
|
|
Chlorophorin is a inhibitor of Melanocortin Receptor. Chlorophorin reduces tyrosinase activity and inhibits a-melanocyte-stimulating hormone-induced melanin production in B16F10 melanoma cells .
|
-
- HY-P1471
-
|
22-52-Adrenomedullin (human)
|
CGRP Receptor
|
Cardiovascular Disease
|
|
Adrenomedullin (AM) (22-52), human, an NH2 terminal truncated adrenomedullin analogue, is an adrenomedullin receptor antagonist, and also antagonizes the calcitonin generelated peptide (CGRP) receptor in the hindlimb vascular bed of the cat .
|
-
- HY-139970
-
|
|
Androgen Receptor
|
Endocrinology
Cancer
|
|
VPC-13789 is a potent, selective, and orally bioavailable antiandrogen. VPC-13789 can be used for the research of castration-resistant prostate cancer (CRPC) therapeutics. VPC-13789 inhibits androgen receptor (AR) transcriptional activity in LNCaP cells (IC50=0.19 μM) .
|
-
- HY-10121R
-
|
|
5-HT Receptor
Adrenergic Receptor
Dopamine Receptor
Histamine Receptor
|
Neurological Disease
Endocrinology
|
|
Asenapine (Standard) is the analytical standard of Asenapine. This product is intended for research and analytical applications. Asenapine (Org 5222), an atypical antipsychotic, is an antagonist of serotonin receptors (pKi: 8.4-10.5), adrenoceptors (pKi: 8.9-9.5), dopamine receptors (pKi: 8.9-9.4) and histamine receptors (pKi: 8.2-9.0). Asenapine can be used in the research of schizophrenia and bipolar disorder .
|
-
- HY-138067
-
|
|
SARS-CoV
|
Inflammation/Immunology
|
|
SSAA09E2 is an inhibitor of SARS-CoV (Severe acute respiratory syndrome-Coronavirus) replication, acting by blocking early interactions of SARS-S with the receptor for SARS-CoV, Angiotensin Converting Enzyme-2 (ACE2) .
|
-
- HY-106347
-
|
CR 2945
|
Cholecystokinin Receptor
|
Inflammation/Immunology
|
|
Itriglumide (CR 2945) is an anthranilic acid derivative. Itriglumide is a potent and selective CCKB receptor antagonist, with an IC50 of 2.3 nM. Itriglumide antagonizes the response to gastrin in a dose-dependent manner with an IC50 of 5.9 nM. Itriglumide shows antisecretory and antiulcer activity .
|
-
- HY-136702
-
|
|
Adenosine Receptor
|
Inflammation/Immunology
|
|
L-97-1 is a A1 adenosine receptor (A1AR) antagonist. L-97-1 is a water-soluble small molecule compound with high affinity and high selectivity against human A1 adenosine receptors. L-97-1 works by blocking A1 adenosine receptors. In patients with asthma, adenosine is an important signaling molecule capable of causing bronchoconstriction by activating A1AR. L-97-1 reduces airway hyperreactivity (BHR) by competitively binding to A1AR, thereby alleviating or blocking adenosine-induced bronchoconstriction and inflammation .
|
-
- HY-108514
-
|
|
Sigma Receptor
|
Neurological Disease
Cancer
|
|
(±)-PPCC hemioxalate is a compound that has the ability to regulate the activity of the sigma-1 receptor. (±)-PPCC hemioxalate can selectively bind sigma-1 protein (s1), and then activate s1 receptor leading to dissociation of s1-BIP complex to regulate ER-mitochondrial calcium signaling, which plays an important role in cell bioenergy and cell survival. (±)-PPCC hemioxalate can be used to study sigma-1 receptors in cocaine addiction, forgetting, pain, depression, Alzheimer's disease, stroke, and cancer .
|
-
- HY-17417A
-
|
|
Opioid Receptor
|
Neurological Disease
Cancer
|
|
Naloxone is an antagonist of Opioid receptor. Naloxone alleviates opioid-overdose-induced respiratory depression. Naloxone may cause pulmonary edema and cardiac arrhythmias .
|
-
- HY-P3530
-
|
|
Integrin
|
Others
|
|
G-{d-Arg}-GDSP is an RGD peptide analogue that binds to the adhesion receptor of integrins and inhibits cellular fibronectin attachment as well as osteoclast resorption .
|
-
- HY-122221
-
-
- HY-117379
-
|
|
Adrenergic Receptor
|
Others
|
|
CHIR-2279 is a high-affinity ligand (Ki=5 nM) for the α1-adrenergic receptor and can be further studied as a drug lead compound .
|
-
- HY-168033
-
-
- HY-116560
-
-
- HY-107497
-
|
|
Biochemical Assay Reagents
|
Cancer
|
|
1-Methyl-3-amino-4-cyanopyrazole (compound 3) is a molecular compound that can be used in the synthesis of adenosine A3 receptor antagonists. 1-Methyl-3-amino-4-cyanopyrazole can be utilized in cancer research .
|
-
- HY-120820
-
|
|
5-HT Receptor
|
Neurological Disease
|
|
LY320954 is a selective 5-HT2A receptor antagonist, with a Ki of 96 nM. LY320954 potently inhibits Ca 2+ influx in the functional assay (EC50 of 35.5 nM). LY320954 inhibits 5-HT-induced paw swelling in rats, with ED50 of 4.8 mg/kg .
|
-
- HY-100672B
-
|
|
Adrenergic Receptor
|
Cardiovascular Disease
Metabolic Disease
|
|
(2R)-SR59230A is the isomer of SR59230A (HY-100672), and can be used as an experimental control. SR59230A is a potent, selective, and blood-brain barrier penetrating β3-adrenergic receptor antagonist with IC50s of 40, 408, and 648 nM for β3, β1, and β2 receptors, respectively .
|
-
- HY-P99171
-
|
|
Interleukin Related
|
Inflammation/Immunology
Cancer
|
|
Gevokizumab is a potent anti-IL-1β antibody, negatively modulates IL-1β signaling through an allosteric mechanism. Gevokizumab selectively decreases the binding affinity of IL-1β for the IL-1 receptor type I (IL-1RI) signaling receptor instead of IL-1 counter-regulatory decoy receptor (IL-1 receptor type II) .
|
-
- HY-138642
-
|
ARV-471
|
PROTACs
Estrogen Receptor/ERR
|
Cancer
|
|
Vepdegestrant (ARV-471) is an orally active PROTAC estrogen receptor degrader against breast cancer. Vepdegestrant is a hetero-bifunctional molecule that facilitates the interactions between estrogen receptor alpha and an intracellular E3 ligase complex. Vepdegestrant leads to the ubiquitylation and subsequent degradation of estrogen receptors via the proteasome. Vepdegestrant robustly degrades ER in ER-positive breast cancer cell lines with a half-maximal degradation concentration (DC50) of about 2 nM .
|
-
- HY-12206
-
|
MR-12842
|
Histamine Receptor
|
Neurological Disease
|
|
Thioperamide (MR-12842) is a potent, orally available, brain penetrant and selective H3 receptor antagonist with a Ki of 4.3 nM for inhibition of [ 3H]histamine release. Thioperamide inhibits [ 3H]histamine synthesis with a Ki of 31 nM .
|
-
- HY-144116
-
|
|
Adenosine Receptor
|
Neurological Disease
|
|
A1AR antagonist 2 (compound 18h) is a potent A1 adenosine receptor (AR) antagonist with Kis of 1.49, 10.2, and 50.1 nM for hA1, hA2A and hA2B, respectively .
|
-
- HY-124962
-
|
(1R,2R)-B13
|
iGluR
|
Neurological Disease
Cancer
|
|
D-NMAPPD ((1R,2R)-B13) is an acid ceramidase inhibitor. D-NMAPPD regulates NMDA receptor properties by enhancing endogenous production of ceramides. D-NMAPPD has anticancer effecs .
|
-
- HY-144115
-
|
|
Adenosine Receptor
|
Neurological Disease
|
|
A1AR antagonist 1 (compound 18g) is a potent A1 adenosine receptor (AR) antagonist with Kis of 2.08, 6.91, and 31.2 nM for hA1, hA2A and hA2B, respectively .
|
-
- HY-W001909R
-
|
|
nAChR
|
Metabolic Disease
|
|
Myosmine (Standard) is the analytical standard of Myosmine. This product is intended for research and analytical applications. Myosmine, a specific tobacco alkaloid in nuts and nut products, has low affinity for a4b2 nicotinic acetylcholinergic receptors (nAChR) with a Ki of 3300 nM .
|
-
- HY-106103A
-
|
MK 678 acetate; L 36358 acetate
|
Somatostatin Receptor
|
Cardiovascular Disease
Neurological Disease
Metabolic Disease
|
|
Seglitide acetate (MK 678; L 36358 acetate) is a potent, orally active somatostatin receptor 2 (SSTR2) agonist, and also a competitive antagonist of SSTR14, SSTR25, and SSTR28. Seglitide acetate has antihypertensive effects and can inhibit plasma glucagon and growth hormone. Seglitide acetate can be used for research on diabetes .
|
-
- HY-106103
-
-
- HY-P2703
-
|
|
Neuropeptide Y Receptor
|
Metabolic Disease
Endocrinology
|
|
Peptide YY (pig) is a 36 amino acid gastrointestinal peptide, can be isolated from porcine duodenum. Peptide YY (pig) decreases appetite and food-intake by activation of the Y2 receptor. Peptide YY (pig) is present mainly in pancreatic endocrine cells with effect on both intestinal motility and the cardiovascular system .
|
-
- HY-164807
-
|
|
PROTACs
Androgen Receptor
|
Cancer
|
|
SARD279 is a potent and selective Androgen Receptor degrader with DC50 value of 1099 nM. SARD279 can be used in prostate cancer research .(Structure Note: Pink: target protein ligand (HY-117486); Blue,: Hyt (HY-W001578); Black: linker (HY-W004896))
|
-
- HY-151105
-
|
|
Cannabinoid Receptor
|
Neurological Disease
|
CBR Agonist-1 (27a-cis) is a cannabinoid receptor (CBR) agonist with the Ki values of 0.18 μM for CB1R and 1.22 μM for CB2R. CBR Agonist-1 (27a-cis) can be used in the study of endogenous cannabinoid system-related diseases .
|
-
- HY-118821
-
|
|
CRFR
|
Metabolic Disease
|
|
JTC-017, a specific corticotropin-releasing hormone receptor 1 antagonist, attenuates hippocampal noradrenaline release, visceral perception, adrenocorticotropic hormone release, and anxiety after acute colorectal distention in rats. JTC-017 blocks stress-induced changes in colonic motility after chronic colorectal distention in rats .
|
-
- HY-19755
-
|
|
Prostaglandin Receptor
|
Inflammation/Immunology
|
|
S-5751 is an orally active prostaglandin DP receptor antagonist. S-5751 inhibits cAMP generation in platelet-rich plasma induced by PGD2 with IC50 0.12 μM. S-5751 has anti-inflammatory activity. S-5751 can be used in asthma research .
|
-
- HY-157956
-
|
|
mAChR
|
Neurological Disease
|
|
LASSBio-873 is an orally active muscarinic cholinergic receptor (mAChR) agonist that crosses the blood-brain barrier. LASSBio-873 has potent analgesic effects on acute and inflammatory pain. The analgesic effect of LASSBio-873 can be inhibited by intrathecal injection of the M2 receptor antagonist methoctramine .
|
-
- HY-14249
-
|
|
Androgen Receptor
Autophagy
|
Cancer
|
|
Bicalutamide is an orally active non-steroidal androgen receptor (AR) antagonist. Bicalutamide can be used for the research of prostate cancer .
|
-
- HY-110278
-
|
|
mGluR
|
Neurological Disease
|
|
ADX71743 is a highly selective, noncompetitive and brain-penetrant metabotropic glutamate receptor 7 negative allosteric modulator (mGlu7 NAM). ADX71743 has anxiolytic-like activity .
|
-
- HY-10933
-
CX516
2 Publications Verification
BDP 12
|
iGluR
|
Neurological Disease
|
|
CX516 (BDP 12) is an ampakine and acts as an AMPA receptor positive allosteric modulator for the research of Alzheimer's disease, schizophrenia and mild cognitive impairment (MCI) .
|
-
- HY-12723
-
|
(-)-Apomorphine
|
Dopamine Receptor
5-HT Receptor
|
Neurological Disease
|
|
Apomorphine is an orally active agonist of Dopamine receptor. Apomorphine can be used in study Parkinson, biphasic dyskinesias, urinary dysfunction,,dystonia, dyspnoea, anismus and belching .
|
-
- HY-111615
-
|
|
Somatostatin Receptor
|
Neurological Disease
|
|
J-2156 is a high potent, selective somatostatin receptor type 4 (SST4 receptor) agonist with IC50s of 0.05 nM and 0.07 nM for human and rat SST4 receptors, respectively. J-2156 is used for the relief of mechanical allodynia and mechanical hyperalgesia in the ipsilateral hindpaws in rats .
|
-
- HY-161914
-
|
|
P2X Receptor
|
Neurological Disease
|
|
P2X3 antagonist 39 (compound 26a) is a selective P2X3 receptor antagonist with an IC50 value of 54.9 nM. P2X3 antagonist 39 can be used in the study of neuropathic pain model .
|
-
- HY-148118A
-
|
|
LYTACs
|
Cancer
|
|
Tri-GalNAc(OAc)3 TFA is a tri-GalNAc ligand that can be used for the synthesis of GalNAc-LYTAC. GalNAc-LYTAC engages the asialoglycoprotein receptor for targeted protein degradation. tri-GalNAc: triantenerrary N-acetylgalactosamine; LYTAC: lysosome-targeting chimera .
|
-
- HY-103211
-
L748337
1 Publications Verification
|
Adrenergic Receptor
|
Cardiovascular Disease
Metabolic Disease
Cancer
|
|
L748337 is a potent β3-adrenergic receptor antagonist and displays selectivity over β1 and β2 receptors. The Ki values of L748337 for β3-, β2- and β1-adrenoceptors are 4.0 nM, 204 nM and 390 nM, respectively . L748337 couples predominantly to Gi to activate MAPK signaling and increases phosphorylation of Erk1/2 with pEC50 value of 11.6 . L748337 can be used for the research of cancer, nonalcoholic fatty liver disease (NAFLD), and cardiovascular related diseases .
|
-
- HY-19927A
-
|
|
5-HT Receptor
|
Neurological Disease
Endocrinology
|
|
DA-6886 is a 5-Hydroxytryptamine receptor 4 (5-HT4) agonist. DA-6886 induces relaxation of the rat oesophagus preparation in a 5-HT4 receptor antagonist-sensitive manner. The evaluation of DA-6886 in CHO cells expressing hERG channels reveals that it inhibits hERG channel current with an pIC50 value of 4.3, indicating that the compound is 1000-fold more selective for the 5-HT4 receptor over hERG channels. DA-6886 can be used in the study of constipated irritable bowel syndrome .
|
-
- HY-P3099
-
|
|
Guanylate Cyclase
|
Cancer
|
|
Uroguanylin (human) is a natural ligand for the Guanylyl Cyclase (GCC) receptor expressed in metastatic colorectal cancer tumors. Uroguanylin (human) has anti-tumor actions in an animal model for human colon cancer .
|
-
- HY-P3891
-
-
- HY-N9329
-
|
|
Monoamine Oxidase
Estrogen Receptor/ERR
|
Metabolic Disease
|
|
Glicoricone, a phenolic compound, is isolated from a species of licorice. Glicoricone is an inhibitor of monoamine oxidase (MAO), with an IC50 of 140 μM. Glicoricone binds to estrogen receptor (ER) and shows estrogen antagonist activity .
|
-
- HY-145640
-
|
AZD4721; RIST4721
|
CXCR
|
Inflammation/Immunology
|
|
Vimnerixin (AZD4721) is the potent and orally active antagonist of acidic CXC chemokine receptor 2 (CXCR2). Vimnerixin has the potential for the research of inflammatory disease .
|
-
- HY-156831
-
|
AEF0117
|
Cannabinoid Receptor
|
Neurological Disease
|
|
Lixosicone is a signaling-specific inhibitor of the cannabinoid receptor 1 (CB1-SSi). Lixosicone plays an important role in Cannabis use disorder (CUD) .
|
-
- HY-108520
-
|
|
RAR/RXR
Apoptosis
|
Cancer
|
|
HX630 is a potent retinoic acid X receptor (RXR) agonist, can induce apoptosis, has anti-tumor effect, and can be used in Cushing's disease research .
|
-
- HY-P4895
-
|
|
Oxytocin Receptor
|
Neurological Disease
|
|
(d(CH2)51,Tyr(Me)2,Orn8)-Oxytocin (OVT) is an oxytocin receptor antagonist. (d(CH2)51,Tyr(Me)2,Orn8)-Oxytocin can be used for the research of neurological disease .
|
-
- HY-100449A
-
|
|
Prostaglandin Receptor
|
Endocrinology
|
|
(S)-AL 8810 is an 11β-fluoro analog of PGF2α that acts as a potent and selective antagonist at the FP receptor. (S)-AL 8810 is the C-15 epimer of AL 8810, having the
inverse, (S), or "natural" configuration at C-15 relative to AL 8810, which is 15-(R) .
|
-
- HY-13418A
-
|
Compound C; BML-275
|
Organoid
AMPK
TGF-β Receptor
Autophagy
|
Cancer
|
|
Dorsomorphin (Compound C) is a selective and ATP-competitive AMPK inhibitor (Ki=109 nM in the absence of AMP). Dorsomorphin (BML-275) selectively inhibits BMP type I receptors ALK2, ALK3, and ALK6. Dorsomorphin can reverse autophagy activation and anti-inflammatory effect of Urolithin A (HY-100599) .
|
-
- HY-103639
-
|
|
Toll-like Receptor (TLR)
|
Inflammation/Immunology
|
|
M62812 (free base) is a toll-like receptor 4 (TLR4) signal transduction inhibitor. M62812 can suppress endothelial cell and leukocyte activation and prevents lethal septic shock in mice. M62812 can be used for the research of sepsis .
|
-
- HY-147557
-
|
|
PACAP Receptor
|
Neurological Disease
|
|
PAC1R antagonist 1 (compound 3d) is a potent and orally active antagonist of PAC1 receptor. PAC1R antagonist 1 can inhibit pituitary adenylate cyclase-activating polypeptide (PACAP)- and nerve injury-induced allodynia .
|
-
- HY-A0261
-
|
ICI-50123
|
Cholecystokinin Receptor
|
Endocrinology
Cancer
|
|
Pentagastrin (ICI-50123) is a potent, selective Cholecystokinin B (CCKB) receptor antagonists with IC50 values of 11 nM and 1100 nM for CCKB and CCKA, respectively. Pentagastrin enhances gastric mucosal defense mechanisms against acid and protects the gastric mucosa from experimental injury . .
|
-
- HY-138642A
-
|
(Rac)-ARV-471
|
Estrogen Receptor/ERR
PROTACs
|
Cancer
|
|
(Rac)-Vepdegestrant is the isomer of Vepdegestrant (HY-138642). Vepdegestrant ((R)-Lavandulol) is an orally active PROTAC estrogen receptor degrader against breast cancer. Vepdegestrant is a hetero-bifunctional molecule that facilitates the interactions between estrogen receptor alpha and an intracellular E3 ligase complex. Vepdegestrant leads to the ubiquitylation and subsequent degradation of estrogen receptors via the proteasome. Vepdegestrant robustly degrades ER in ER-positive breast cancer cell lines with a half-maximal degradation concentration (DC50) of about 2 nM .
|
-
- HY-108662
-
|
2,2'-Pyridylisatogen tosylate
|
P2Y Receptor
|
Inflammation/Immunology
Cancer
|
|
PIT (2,2'-Pyridylisatogen tosylate) is a selective and non-competitive antagonist of P2Y1 receptor with an IC50 value of 0.14 μM for human P2Y1 receptor. PIT antagonizes P2Y1 receptor signaling without affecting nucleotide binding. PIT is an irreversible antagonist of responses to ATP at metabotropic purinoceptors (of the P2Y family) in some smooth muscles. PIT can be used for the research of chronic bronchitis and asthma .
|
-
- HY-B0160
-
|
FRG-8813
|
Histamine Receptor
|
Metabolic Disease
Endocrinology
|
|
Lafutidine (FRG-8813) is a histamine H2-receptor antagonist (H2RA), with proven gastric mucosal protective effects. Lafutidine can be used for the research of gastroesophageal reflux disease .
|
-
- HY-103164
-
|
|
Adenosine Receptor
Monoamine Oxidase
|
Neurological Disease
|
|
(E)-8-(3-Chlorostyryl)caffeine is a selective adenosine A2A receptor antagonist. (E)-8-(3-Chlorostyryl)caffeine inhibits monoamine oxidase B (MAO-B) with a Ki value of 70 nM by a pathway that is independent of its actions on the A2A receptor. (E)-8-(3-Chlorostyryl)caffeine has the potential for Parkinson's disease research .
|
-
- HY-121156
-
|
LF 16-0687; XY-2405
|
Bradykinin Receptor
|
Neurological Disease
|
|
Anatibant (LF 16-0687; XY-2405) is a selective non-peptide bradykinin B2 receptor antagonist. Anatibant binds to the human, rat and guinea-pig recombinant B2 receptor with Ki values of 0.67 nM, 1.74 nM and 1.37 nM, respectively. Anatibant crosses the blood-brain barrier (BBB). Anatibant can be used in research on brain damage diseases .
|
-
- HY-121156A
-
|
LF 16-0687 hydrochloride; XY-2405 hydrochloride
|
Bradykinin Receptor
|
Neurological Disease
|
|
Anatibant (LF 16-0687; XY-2405) hydrochloride is a selective non-peptide bradykinin B2 receptor antagonist. Anatibant hydrochloride binds to the human, rat and guinea-pig recombinant B2 receptor with Ki values of 0.67 nM, 1.74 nM and 1.37 nM, respectively. Anatibant hydrochloride crosses the blood-brain barrier (BBB). Anatibant hydrochloride can be used in research on brain damage diseases .
|
-
- HY-D2426
-
|
|
Fluorescent Dye
Transferrin Receptor
|
Cardiovascular Disease
|
|
Cy3-Transferrin is a fluorescent labeling reagent that combines Cy3 (HY-D0822) fluorescent dye and Transferrin (HY-P3267). The Cy3 fluorophore is commonly used in applications such as immunolabeling, nucleic acid labeling, fluorescence microscopy, and flow cytometry. Cy3 has an emission maximum around 562-570 nm. Transferrin, a blood-plasma glycoprotein, is a target ligand for transferrin receptor. Transferrin can bind to and mediate the transport of iron .
|
-
- HY-70081
-
|
PNU-95666E
|
Dopamine Receptor
|
Neurological Disease
|
|
Sumanirole (PNU-95666E) is a highly selective D2 receptor full agonist with an ED50 of about 46 nM. Sumanirole plays an important role in the research of Parkinson's disease and restless leg syndrome .
|
-
- HY-117436
-
|
|
Dopamine Receptor
|
Cardiovascular Disease
|
|
R(+)-6-Bromo-APB hydrobromide is a dopamine (DA) agonist. R(+)-6-Bromo-APB hydrobromide increased the expression of µ opioid receptor (MOR) mRNA in the nucleus accumbens .
|
-
- HY-B0781
-
|
|
Histamine Receptor
mAChR
Adrenergic Receptor
|
Neurological Disease
Endocrinology
|
Promethazine hydrochloride is an orally active phenothiazine derivative with antihistaminic (H1), sedative, antiemetic, anticholinergic, and antimotion sickness properties. Promethazine hydrochloride is a potent H1 receptor antagonist and a mAChR antagonist. It also has a certain affinity for 5-HT2A and 5-HT2C receptors .
|
-
- HY-P3209
-
-
![Des-Arg9-[Leu8]-Bradykinin acetate](//file.medchemexpress.com/product_pic/hy-p3209.gif)
- HY-149728
-
-
- HY-107722
-
|
|
Opioid Receptor
|
Neurological Disease
|
|
SCH 221510 is a potent, orally active and selective NOP (nociceptin opioid receptor) agonist, with an EC50 of 12 nM and Ki of 0.3 nM. SCH 221510 shows an anxiolytic-like effect .
|
-
- HY-157493
-
|
|
Progesterone Receptor
|
Endocrinology
|
|
PR antagonist 1 (compound 8) is a selective progesterone receptor (PR) antagonist, and can be used for the research of a variety of progesterone-related diseases and disorders such as endometriosis and uterine fibroids .
|
-
- HY-118410
-
|
|
Integrin
|
Cardiovascular Disease
|
|
L-738167 is an orally active fibrogen receptor antagonist that prevents the binding of fibrinogen to GP IIb/IIIa. L-738167 can be utilized in thrombus research .
|
-
- HY-113653
-
|
GSK706
|
GPR119
|
Metabolic Disease
|
|
GSK2041706A (GSK706) is a potent G protein-coupled receptor 119 (GPR119) agonist. GSK2041706A can be used for the research of type 2 diabetes .
|
-
- HY-108242
-
|
(-)-Apomorphine hydrochloride
|
Dopamine Receptor
5-HT Receptor
|
Neurological Disease
|
|
Apomorphine ((-)-Apomorphine) hydrochloride is an orally active agonist of Dopamine receptor. Apomorphine hydrochloride can be used in study Parkinson, biphasic dyskinesias, urinary dysfunction, dystonia, dyspnoea, anismus and belching .
|
-
- HY-122422R
-
|
|
5-HT Receptor
|
Others
|
|
Gepirone (Standard) is the analytical standard of Gepirone. This product is intended for research and analytical applications. Gepirone is a selective and affinitive 5-HT1A agonist. Gepirone binds selectively to 5-HT1A receptor binding site. Gepirone acts as an antidepressant agent can be used for anxiety and major depressive disorder research .
|
-
- HY-103112A
-
|
|
5-HT Receptor
|
Neurological Disease
|
|
SB 243213 dihydrochloride is an orally active, selective and high-affinity 5-HT2C receptor antagonist with a pKi of 9.37 and a pKb of 9.8 for human 5-HT2C receptor. SB 243213 dihydrochloride shows greater than a 100-fold selectivity over a wide range of neurotransmitter receptors, enzymes and ion channels. SB 243213 dihydrochloride has improved anxiolytic profile and has the potential for schizophrenia and motor disorders .
|
-
- HY-103112B
-
|
|
5-HT Receptor
|
Neurological Disease
|
|
SB 243213 is an orally active, selective and high-affinity 5-HT2C receptor antagonist with a pKi of 9.37 and a pKb of 9.8 for human 5-HT2C receptor. SB 243213 shows greater than a 100-fold selectivity over a wide range of neurotransmitter receptors, enzymes and ion channels. SB 243213 has improved anxiolytic profile and has the potential for schizophrenia and motor disorders .
|
-
- HY-103112
-
|
|
5-HT Receptor
|
Neurological Disease
|
|
SB 243213 hydrochloride is an orally active, selective and high-affinity 5-HT2C receptor antagonist with a pKi of 9.37 and a pKb of 9.8 for human 5-HT2C receptor. SB 243213 hydrochloride shows greater than a 100-fold selectivity over a wide range of neurotransmitter receptors, enzymes and ion channels. SB 243213 hydrochloride has improved anxiolytic profile and has the potential for schizophrenia and motor disorders .
|
-
- HY-142926
-
|
|
Estrogen Receptor/ERR
|
Cancer
|
|
ER degrader 2 is a potent degrader of estrogen receptor (ER). The estrogen signaling system plays an important role in regulating cell growth, differentiation and apoptosis. ER degrader 2 has the potential for the research of cancer diseases (extracted from patent CN112830919A, compound 1) .
|
-
- HY-143878
-
-
- HY-A0261A
-
|
ICI-50123 meglumine
|
Cholecystokinin Receptor
|
Endocrinology
Cancer
|
|
Pentagastrin (ICI-50123) meglumine is a potent, selective Cholecystokinin B (CCKB) receptor antagonists with IC50 values of 11 nM and 1100 nM for CCKB and CCKA, respectively. Pentagastrin meglumine enhances gastric mucosal defense mechanisms against acid and protects the gastric mucosa from experimental injury . .
|
-
- HY-163157
-
|
|
Parasite
|
Others
|
|
Insecticidal agent 7 (Compound 21m) is an insecticide that targets the insect ryanodine receptors (RyRs) with a LC50 of 0.0937 mg/L for the Plutella xylostella. Insecticidal agent 7 (Compound 21m) exhibits good selectivity and low toxicity towards non-target organisms .
|
-
- HY-P3634
-
|
|
Opioid Receptor
|
Neurological Disease
|
|
[DAla2] Dynorphin A (1-13), amide (porcine) is a petide. [DAla2] Dynorphin A (1-13), amide (porcine) might have the κ opioid receptor agonist effect. [DAla2] Dynorphin A (1-13), amide (porcine) can be used for the research of nervous system .
|
-
![[DAla2] Dynorphin A (1-13), amide (porcine)](//file.medchemexpress.com/product_pic/hy-p3634.gif)
- HY-B1067AR
-
|
|
Histamine Receptor
|
Neurological Disease
|
|
Antazoline (Standard) is the analytical standard of Antazoline. This product is intended for research and analytical applications. Antazoline (Phenazoline) is an H1 receptor antagonist that affects the activity of the central nervous system, has a potent antiarrhythmic effect .
|
-
- HY-P3913
-
|
|
Bacterial
|
Infection
|
|
Acetyl-Adhesin (1025-1044) amide is a 20-peptide fragment of Streptococcus pyogenes cell surface adhesin that acts as an antimicrobial peptide to specifically inhibit the binding of adhesin to salivary receptors and prevent recolonization of Streptococcus pyogenes .
|
-
- HY-P3629
-
|
Leumorphin (pig)
|
Opioid Receptor
|
Neurological Disease
Inflammation/Immunology
|
|
Dynorphin B 29 (Leumorphin) (pig) is a petide. Dynorphin B 29 (pig) can interact with multiple receptors in the brain, as well as in isolated tissue systems. Dynorphin B 29 (pig) can be used for the research of immunoreaction .
|
-
- HY-A0134
-
|
|
GABA Receptor
|
Neurological Disease
|
|
Isoflurane is a volatile general anaesthetic used for induction and maintenance of general anesthesia. Isoflurane binds to and enhances GABAA receptor. Isoflurane inhibits electron transfer in respiratory complex I .
|
-
- HY-145585
-
|
MIJ-821
|
iGluR
|
Neurological Disease
|
|
Onfasprodil is negative allosteric modulator of NR2B. Onfasprodil in combination with GABA receptor regulator has the potential for the research of Alzheimer's disease (extracted from patent CN111481543A) .
|
-
- HY-141495A
-
|
(-)-PW0464
|
Dopamine Receptor
|
Neurological Disease
|
|
Razpipadon ((-)-PW0464), an aromatic compound, is a dopamine receptor partial agonist. Razpipadon can be used in the study of dopamine D1 ligand-mediated related psychiatric disorders .
|
-
- HY-P2217
-
|
DSC-127; NorLeu3-A(1-7)
|
Angiotensin Receptor
|
Inflammation/Immunology
|
|
Aclerastide (DSC-127) is an angiotensin receptor agonist. Aclerastide also is a peptide analog of angiotensin II. Aclerastide can be used for the research of tissue regeneration in diabetic ulcers .
|
-
- HY-B1296
-
|
(±)-Promethazine
|
Histamine Receptor
|
Neurological Disease
Endocrinology
|
|
Promethazine is an orally active histamine receptor antagonist . Promethazine is first-generation antihistamine of the phenothiazine family, shows strong sedative and weak antipsychotic effects .
|
-
- HY-144291
-
|
|
Dopamine Receptor
|
Neurological Disease
|
|
LY3154885 is an orally active dopamine D1 receptor positive allosteric modulator (PAM). LY3154885 has an improved agent-agent interactions (DDI) risk profile .
|
-
- HY-108546
-
|
3-Phosphono-L-alanine
|
mGluR
|
Neurological Disease
|
|
L-AP3, metabotropic glutamate receptor (mGluR) antagonist, inhibits D-phosphoserine and L-phosphoserine with IC50s of 368 μM and 2087 μM, respectively .
|
-
- HY-15502
-
-
- HY-111615A
-
|
|
Somatostatin Receptor
|
Neurological Disease
Inflammation/Immunology
|
|
J-2156 TFA is a high potent, selective somatostatin receptor type 4 (SST4 receptor) agonist with IC50s of 0.05 nM and 0.07 nM for human and rat SST4 receptors, respectively. J-2156 TFA has anti-inflammatory activity and it is used for the relief of mechanical allodynia and mechanical hyperalgesia in the ipsilateral hindpaws in rats .
|
-
- HY-119418
-
|
|
Estrogen Receptor/ERR
|
Cancer
|
|
Desketoraloxifene is an estrogen receptors alpha (ERα) activator at an AP-1 site. Desketoraloxifene can be used for the research of osteoporosis and breast cancer .
|
-
- HY-13418
-
|
Compound C dihydrochloride; BML-275 dihydrochloride
|
Organoid
AMPK
TGF-β Receptor
Autophagy
|
Cancer
|
|
Dorsomorphin (Compound C) dihydrochloride is a potent, selective and ATP-competitive AMPK inhibitor, with a Ki of 109 nM. Dorsomorphin dihydrochloride inhibits BMP pathway by targeting the type I receptors ALK2, ALK3, and ALK6. Dorsomorphin dihydrochloride can reverse autophagy activation and anti-inflammatory effect of Urolithin A (HY-100599).
|
-
- HY-B1337R
-
|
|
nAChR
Endogenous Metabolite
|
Cancer
|
|
Choline (chloride) (Standard) is the analytical standard of Choline (chloride). This product is intended for research and analytical applications. Choline chloride is an essential nutrient that activates alpha7 nicotinic receptors and has analgesic and anti-inflammatory activity. Glycerophosphoinositol choline can affect diseases such as liver disease, atherosclerosis and neurological disorders .
|
-
- HY-142925
-
|
|
Estrogen Receptor/ERR
|
Cancer
|
|
ER degrader 1 is a potent degrader of estrogen receptor (ER). The estrogen signaling system plays an important role in regulating cell growth, differentiation and apoptosis. ER degrader 1 has the potential for the research of cancer diseases (extracted from patent WO2021139756A1, compound 11) .
|
-
- HY-142927
-
|
|
Estrogen Receptor/ERR
|
Cancer
|
|
ER degrader 3 is a potent degrader of estrogen receptor (ER). The estrogen signaling system plays an important role in regulating cell growth, differentiation and apoptosis. ER degrader 3 has the potential for the research of cancer diseases (extracted from patent WO2018233591A1, compound 1) .
|
-
- HY-N7272
-
|
|
Phosphodiesterase (PDE)
|
Metabolic Disease
|
|
Cirsimarin is a potent antilipogenic flavonoid isolated from Microtea debilis. Cirsimarin exerts potent antilipogenic effect and decreases adipose tissue deposition in mice. The lipolytic activity of Cirsimarin resulting from both its antagonist activity on adenosin A1 receptor and its inhibitory effect on phosphodiesterase .
|
-
- HY-76570A
-
|
(Rac)-Desfesoterodine hydrochloride; (Rac)-PNU-200577 hydrochloride
|
mAChR
|
Neurological Disease
|
|
(Rac)-5-Hydroxymethyl Tolterodine ((Rac)-Desfesoterodine) hydrochloride, an active metabolite of Tolterodine, is a mAChR antagonist (Ki values of 2.3 nM, 2 nM, 2.5 nM, 2.8 nM, and 2.9 nM for M1, M2, M3, M4, and M5 receptors, respectively). (Rac)-5-Hydroxymethyl Tolterodine hydrochloride can be used for overactive bladder research .
|
-
- HY-157792
-
|
|
mAChR
|
Neurological Disease
|
Antidepressant agent 6 (S-3a) is a lead compound with potent and sustained antidepressant effects. Antidepressant agent 6 (S-3a) displays high cognitive safety margin.Antidepressant agent 6 (S-3a) antagonizes M1 receptors and elevates BDNF levels, suggesting its potential as an antidepressant for further exploration .
|
-
- HY-157491
-
-
- HY-109006
-
|
|
mAChR
|
Neurological Disease
|
|
Ilmetropium iodide is an anticholinergic agent. Ilmetropium iodide selectively blocks M-cholinergic receptors of bronchial muscle, reduces or prevents bronchoconstrictor response associated with both cholinergic stimulation, as well as the impact of the factors that provoke bronchospasm. Strength and selectivity of ilmetropium iodide action substantially exceeds Atropine sulfate (HY-B1205A) and Ipratropium bromide (HY-B0241) .
|
-
- HY-N8852
-
|
6-MeOF
|
GABA Receptor
|
Neurological Disease
|
|
6-Methoxyflavanone (6-MeOF) is an orally active flavonoid compound. 6-Methoxyflavanone has anxiolytic properties. 6-Methoxyflavanone targets unique sites on GABA-A receptors, different from traditional benzodiazepines. 6-Methoxyflavanone can be used to study anxiety disorders. 6-Methoxyflavanone readily crosses the blood brain barrier (BBB) .
|
-
- HY-76570
-
|
(Rac)-Desfesoterodine; (Rac)-PNU-200577
|
mAChR
|
Neurological Disease
|
|
(Rac)-5-Hydroxymethyl Tolterodine ((Rac)-Desfesoterodine), an active metabolite of Tolterodine, is a mAChR antagonist (Ki values of 2.3 nM, 2 nM, 2.5 nM, 2.8 nM, and 2.9 nM for M1, M2, M3, M4, and M5 receptors, respectively). (Rac)-5-Hydroxymethyl Tolterodine can be used for overactive bladder research .
|
-
- HY-12245
-
|
|
TRP Channel
|
Inflammation/Immunology
|
|
SB-366791 is a potent and selective vanilloid receptor (VR1/TRPV1) antagonist (IC50=5.7 nM). SB-366791 can be used for the research of inflammation .
|
-
- HY-106932
-
|
|
Integrin
|
Cardiovascular Disease
|
|
L-734217 is an orally active and potent fibrinogen receptor antagonist and an antithrombotic agent. L-734217 is excreted largely by the renal route and partly into the bile in dogs. L-734217 is promising for research of thrombotic disorders .
|
-
- HY-P99036
-
-
- HY-147293
-
|
|
Glucocorticoid Receptor
Apoptosis
Caspase
|
Cancer
|
|
Nenocorilantis a potent, orally activity glucocorticoid receptor (GR) antagonist with Ki value of 0.15 nM. Nenocorilant has pro-apoptotic effects and improves potency combined with cytotoxic agent. Nenocorilant can be used for cancer research .
|
-
- HY-10121S2
-
-
- HY-N2466A
-
|
MT-I acetate; [Nle4,D-Phe7]-α-MSH acetate
|
Melanocortin Receptor
|
Cancer
|
|
Melanotan I acetate is a potent non-selective melanocortin receptor (MCR) agonist. Melanotan I acetate is a synthetic analogue of α-melanocyte stimulating hormone (α-MSH) that stimulates melanogenesis. Melanotan I acetate can induce skin tanning by mimicking the actions of a-MSH on the melanocortin type 1 receptors (MC1R) of melanocytes. Melanotan I acetate can be used for sunlight-induced skin cancers research .
|
-
- HY-160221
-
|
|
PROTACs
Androgen Receptor
|
Cancer
|
|
PROTAC AR Degrader-7 (compound 99) is a PROTAC targeting androgen receptor with an IC50 value of 3 nM. PROTAC AR Degrader-7 is composed of PROTAC target protein ligand AR ligand-32 (HY-170303) (red part), E3 ligase ligand E3 ligase Ligand 44 (HY-170304) (blue part) and PROTAC Linker N-Boc-piperazine (HY-30105) (black part), among which the conjugate of E3 ubiquitin ligase ligand + Linker is E3 Ligase Ligand-linker Conjugate 145 (HY-170305) .
|
-
- HY-17497
-
-
- HY-B1216
-
-
- HY-116480
-
|
|
mAChR
|
Neurological Disease
|
|
LY593093 is a selective, orally active, and brain-penetrant muscarinic M1 receptor agonist with an EC50 of 22.8 nM. LY593093 can be utilized in Alzheimer’s disease research .
|
-
- HY-116586A
-
|
|
mAChR
Sigma Receptor
|
Neurological Disease
|
|
(Rac)-AF710B is the racemate of AF710B (HY-116586). AF710B is a highly potent and selective allosteric M1 muscarinic and σ1 receptor agonist. AF710B can be used for the research of Alzheimer’s disease .
|
-
- HY-119401
-
|
BML-241
|
LPL Receptor
|
Cancer
|
|
CAY10444 (BML-241) is a sphingosine-1-phosphate 3 (S1P3) antagonist. CAY10444 inhibits by 37% S1P-induced increases in Ca2+ in HeLa cells expressing S1P3 receptors .
|
-
- HY-106512
-
|
|
Prostaglandin Receptor
|
Others
|
|
Cianergoline is a ergoline derivative with the activity of reducing intraocular pressure (IOP). Its primary regulatory mechanism involves the inhibition of sympathetic nervous function, achieved through actions on both prejunctional (DA2) and postjunctional (α1) adrenergic receptors. Cianergoline can be used for research in the field of glaucoma .
|
-
- HY-103639A
-
|
|
Toll-like Receptor (TLR)
|
Infection
|
|
M62812 is a toll-like receptor 4 (TLR4) signaling inhibitor. M62812 inhibits endothelial and leukocyte activation and prevents lethal septic shock in mice. M62812 can reduces LPS-induced coagulation and inflammatory responses. M62812 can be used for the research of sepsis .
|
-
- HY-P3517
-
|
β-EP (6-31), human
|
Opioid Receptor
|
Neurological Disease
Endocrinology
|
|
β-Endorphin, an endogenous opioid neuropeptide, is an opioid receptor agonist. β-Endorphin binds preferentially to μ-opioid receptors and is produced in certain neurons of the central and peripheral nervous system and is one of three endorphins produced in humans. β-Endorphin can be used to reduce stress and maintain homeostasis in the body and is involved in neurological pain perception regulation .
|
-
- HY-163101
-
|
|
Platelet-activating Factor Receptor (PAFR)
Leukotriene Receptor
|
Inflammation/Immunology
|
|
CP-96021 is a potent and orally available leukotriene D4 (LTD4 Ki=34 μM) / platelet activating factor (PAF Ki=37 μM) receptor antagonist. CP-96021 has antagonist capable of simultaneously targeting two different inflammatory mediators, LTD4 and PAF. CP-96021 shows high specificity for α1, α2, β, dopamine-2, adenosine 1, 5-HT1, H1, muscarine, μ opioid, and GABA receptors, all expressing IC50 values greater than 10 μM. CP-96021 can be used to study the pathogenesis of many inflammatory diseases such as asthma .
|
-
- HY-18287A
-
|
|
Smo
|
Cancer
|
|
MRT-83 (hydrochloride) is the potent antagonist of Smoothened (Smo) receptor. MRT-83 (hydrochloride) inhibits the Hedgehog (Hh) signaling pathway and BODIPY-cyclopamine binding to human Smo. MRT-83 (hydrochloride) has the potential for researching cancer disease .
|
-
- HY-N7707
-
|
|
Apoptosis
|
Cancer
|
|
Sandacanol is a specific agonist of olfactory receptor (OR10H1). Sandacanol induces cell cycle arrest and some apoptosis in bladder cancer cells .
|
-
- HY-125265
-
|
|
Glucocorticoid Receptor
|
Metabolic Disease
|
|
JTP-117968, a novel selective glucocorticoid receptor modulator (a non-steroidal SGRM, IC50 of 6.8 nM), exhibits improved transrepression/transactivation dissociation .
|
-
- HY-126941
-
|
|
Opioid Receptor
|
Neurological Disease
|
|
Hecogenin acetate is a steroidal sapogenin-acetylated with anti-inflammatory and antinociceptive. Hecogenin acetate shows potential antihyperalgesic activity, inhibiting descending pain and acting in opioid receptors .
|
-
- HY-110206
-
|
|
Cannabinoid Receptor
|
Metabolic Disease
|
|
AM6545 is a highly selective, brain-free (peripherally active) CB1 receptor antagonist (Ki=1.7 nM). AM6545 inhibits endocannabinoid signaling by competitively antagonizing CB1 receptors, inhibiting CB1-mediated appetite stimulation and inflammatory responses without affecting cAMP levels. AM6545 significantly reduces food intake and body weight in mice, while improving metabolic syndrome-related renal impairment (such as proteinuria, fibrosis) and insulin resistance. AM6545 can be used in the study of obesity and its complications .
|
-
- HY-101100
-
|
D-16949 hydrochloride
|
5-HT Receptor
|
Neurological Disease
|
|
Anpirtoline (D-16949) hydrochloride is a centrally acting 5-HT1B receptor agonist, with Kis of 28 nM (5-HT1B), 150 nM (5-HT1A) and 1.49 μM (5-HT2). Anpirtoline hydrochloride has serotonergic, antinociceptive, antidepressant-like effects .
|
-
- HY-133189
-
|
|
PROTAC Linkers
|
Endocrinology
|
|
Bis-propargyl-PEG9 is a PEG-based PROTAC linker used in the synthesis of PROTACs. Bis-propargyl-PEG9 can be used to synthesize the bivalent estrogen receptor ligands . Bis-propargyl-PEG9 is a click chemistry reagent, it contains an Alkyne group and can undergo copper-catalyzed azide-alkyne cycloaddition (CuAAc) with molecules containing Azide groups.
|
-
- HY-B0121B
-
|
GR 43175 free base
|
5-HT Receptor
|
Neurological Disease
|
|
Sumatriptan (GR 43175) is an orally active 5-HT1 receptor agonist with IC50s of 7.3 nm, 9.3nm and 17.8 nm for 5-HT1D, 5-HT1B and 5-HT1F receptors, respectively. Sumatriptan can be used for migraine headache research .
|
-
- HY-B0121A
-
|
GR 43175 hydrochloride
|
5-HT Receptor
|
Neurological Disease
|
|
Sumatriptan hydrochloride (GR 43175) is an orally active 5-HT1 receptor agonist with IC50s of 7.3 nm, 9.3nm and 17.8 nm for 5-HT1D, 5-HT1B and 5-HT1F receptors, respectively. Sumatriptan hydrochloride can be used for migraine headache research .
|
-
- HY-N1064
-
|
|
nAChR
|
Neurological Disease
|
|
Xanthoplanine, isolated from theroot of Xylopia parviflora, fully inhibits the EC50 ACh responses of both alpha7 and alpha4beta2 nACh receptors with estimated IC50 values of 9 μM (alpha7) and 5 μM (alpha4beta2) .
|
-
- HY-124521
-
|
LY163502 free base
|
Dopamine Receptor
|
Neurological Disease
|
|
Quinelorane (LY163502 free base) is a dopamine D2 receptor agonist. Quinelorane promotes semen ejaculation but inhibits penile erection in rats. Quinelorane can be used in the study of sexual dysfunction .
|
-
- HY-P0120
-
|
LY2189265
|
GCGR
|
Metabolic Disease
|
|
Dulaglutide (LY2189265) is a glucagon-like peptide-1 (GLP-1) receptor agonist. Dulaglutide can be uesd for the research of type 2 diabetes (T2D) .
|
-
- HY-P2092
-
-
- HY-108531
-
|
|
RAR/RXR
|
Cancer
|
|
ER-50891 is a potent antagonist of retinoic acid receptor α(RARα). ER-50891 significantly attenuates ATRA's inhibitive effects on BMP 2-induced osteoblastogenesis .
|
-
- HY-108531A
-
|
|
RAR/RXR
|
Cancer
|
|
ER 50891 quarterhydrate is a potent antagonist of retinoic acid receptor α(RARα). ER 50891 quarterhydrate significantly attenuates ATRA's inhibitive effects on BMP 2-induced osteoblastogenesis .
|
-
- HY-B0802
-
|
Terbutaline hemisulfate
|
Adrenergic Receptor
Antibiotic
|
Endocrinology
|
|
Terbutaline sulfate is an orally active β2-adrenergic receptor agonist and an active metabolite of bambuterol . Terbutaline sulfate can be used in asthma symptom research .
|
-
- HY-19583
-
-
- HY-129710
-
|
|
GABA Receptor
|
Neurological Disease
|
|
CGP47656 is a potent GABAB receptor agonist that inhibits Forskolin (HY-15371)-stimulated adenylyl cyclase activity and augments noradrenaline-stimulated adenylyl cyclase activity. CGP47656 is promising for research of brain function-related diseases .
|
-
- HY-113414
-
|
|
Endogenous Metabolite
Mineralocorticoid Receptor
|
Others
Inflammation/Immunology
|
|
Deoxycorticosterone is a steroid hormone produced by the adrenal gland that possesses mineralocorticoid activity and acts as an aldosterone precursor. Deoxycorticosterone is an agonist for O. mykiss mineralocorticoid receptor (rtMR) transcription with EC50 of 0.16 nM . Deoxycorticosterone could acts as an immune stimulator in fish .
|
-
- HY-160979
-
|
DA-5047
|
Histamine Receptor
|
Others
Endocrinology
|
|
Bisfentidine is an H2 receptor antagonist, Bisfentidine can block the H2 receptor on the cells of the stomach wall, and reduce the secretion of stomach acid. Bisfentidine binds to cytochrome P-450 in liver microsomes and affects drug metabolism. Bisfentidine can be used in the study of metabolic processes of drugs, lipid peroxidation processes and peptic ulcers diseases .
|
-
- HY-P1471A
-
|
22-52-Adrenomedullin (human) (TFA)
|
CGRP Receptor
|
Cardiovascular Disease
|
|
Adrenomedullin (AM) (22-52), human (22-52-Adrenomedullin human) TFA, an NH2 terminal truncated adrenomedullin analogue, is an adrenomedullin receptor antagonist. Adrenomedullin (AM) (22-52), human also antagonizes the calcitonin generelated peptide (CGRP) receptor in the hindlimb vascular bed of the cat .
|
-
- HY-121313
-
|
BAY 10-6734
|
Angiotensin Receptor
|
Neurological Disease
Endocrinology
|
|
Embusartan (BAY 10-6734) is a brain-penetrant and effective AT1 receptor blocker. Embusartan inhibits Ang II binding to brain AT1 receptors in the nuclei of central nervous system (CNS) inside due to high lipophilic character. Embusartan is promising for research of sympathetic hyperactivity and hypertension .
|
-
- HY-P1389
-
|
|
Neuropeptide S Receptor
|
Neurological Disease
|
|
Neuropeptide S human, a neuropeptide, is a potent cognate neuropeptide S receptor (NPSR) agonist. Neuropeptide S human can be used for Alzheimer's disease (AD) research .
|
-
- HY-P3083
-
|
|
PKC
|
Inflammation/Immunology
|
|
N-Myristoyl-Lys-Arg-Thr-Leu-Arg is a protein kinase C (PKC) inhibitor with an IC50 value of 75 μM. N-Myristoyl-Lys-Arg-Thr-Leu-Arg inhibits IL-2 receptor induction and IL-2 production in the human leukemic cell line Jurkat .
|
-
- HY-B0121
-
|
GR 43175 succinate
|
5-HT Receptor
|
Neurological Disease
|
|
Sumatriptan succinate (GR 43175) is an orally active 5-HT1 receptor agonist with IC50s of 7.3 nm, 9.3nm and 17.8 nm for 5-HT1D, 5-HT1B and 5-HT1F receptors, respectively. Sumatriptan succinate can be used for migraine headache research .
|
-
- HY-111321
-
-
- HY-P99028
-
|
TMB-355; TNX-355
|
HIV
|
Infection
|
|
Ibalizumab (TMB-355) is a humanised IgG4 monoclonal antibody that prevents HIV cell entry by binding to CD4 receptor. Ibalizumab has the potential for HIV-1 infection research .
|
-
- HY-121539
-
|
|
TRP Channel
|
Neurological Disease
|
|
Supercinnamaldehyde is a potent transient receptor potential ankyrin 1 (TRPA1) activator with an EC50 value of 0.8 μM. Supercinnamaldehyde activates TRPA1 ion channels through covalent modification of cysteines .
|
-
- HY-169450
-
|
9-O-Desmethyl mitragynine
|
Opioid Receptor
|
Neurological Disease
|
|
(-)-9-Hydroxycorynantheidine (9-O-Desmethyl mitragynine), the 9-demethyl analogue of Mitragynine, is a selective and partial agonist of μ-opioid receptor. (-)-9-Hydroxycorynantheidine inhibits electrically stimulated twitch contraction in guinea-pig ileum .
|
-
- HY-70081A
-
|
U-95666E; PNU-95666
|
Dopamine Receptor
|
Neurological Disease
|
|
Sumanirole maleate (U-95666E; PNU-95666E) is a highly selective D2 receptor full agonist with an ED50 of about 46 nM. Sumanirole plays an important role in the research of Parkinson's disease and restless leg syndrome .
|
-
- HY-15682G
-
|
Ro 13-7410; Arotinoid acid; AGN191183
|
RAR/RXR
|
Cancer
|
|
TTNPB (Ro 13-7410) (GMP) is TTNPB (HY-15682) produced by using GMP guidelines. GMP small molecules work appropriately as an auxiliary reagent for cell therapy manufacture. TTNPB is a highly potent retinoic acid receptor (RAR) agonist .
|
-
- HY-19010
-
|
SKF 94482
|
Histamine Receptor
|
Neurological Disease
|
|
BMY-25368 (SKF 94482) is a histamine H2 receptor antagonist that acts as a gastric acid secretion inhibitor. BMY-25368 competitively antagonizes gastric secretion stimulated by histamine and also antagonizes gastric secretion stimulated by Pentagastrin (HY-A0261), Bethanechol (HY-B0406), and food .
|
-
- HY-124821
-
|
|
5-HT Receptor
|
Neurological Disease
Metabolic Disease
|
|
VA012 (compound 11) is a positive allosteric modulator (PAM) of the serotonin 5-HT2C receptor. VA012 reduces food intake and body weight gain without causing CNS-related malaise during subchronic administration. VA012 can be utilized in obesity research .
|
-
- HY-136208
-
|
|
Opioid Receptor
|
Neurological Disease
|
|
TAN-452 is an orally active, selective peripherally acting δ-opioid receptor (DOR) antagonist with a Ki of 0.47 nM and a Kb of 0.21 nM. TAN-452 is an antagonist for μ-opioid receptor (MOR; Ki=36.56 nM and Kb=9.43 nM) and κ-opioid receptor (KOR; Ki=5.31 nM and Kb=7.18 nM). TAN-452, a derivative of Naltrindole, demonstrates low brain penetrability and attenuates morphine-induced side effects without affecting pain control .
|
-
- HY-110080
-
|
|
Dopamine Receptor
|
Neurological Disease
|
|
Lisuride (maleate) is a potent agonist of dopamine with a probably direct action on dopaminergic receptors. Lisuride (maleate) is an ergot derivative. Lisuride (maleate) releases the premenstrual mastalgia without significant side effects .
|
-
- HY-130074
-
|
|
TRP Channel
|
Neurological Disease
|
|
FEMA 4809 is a TRPM8 receptor agonist (EC50=0.2 nM) for use as a cooling agent. TRPM8 is the ion channel responsible for the cool perception .
|
-
- HY-133552
-
|
|
ROR
|
Inflammation/Immunology
|
|
RORγt Inverse agonist 10 is a potent and orally bioavailable RORγt (retinoic acid receptor-related orphan nuclear receptor gamma t) inverse agonist, with an IC50 of 51 nM. RORγt is a major transcription factor of genes related to psoriasis pathogenesis such as IL-17A, IL-22, and IL-23R
|
-
- HY-149993
-
-
- HY-162118
-
|
|
Vasopressin Receptor
|
Neurological Disease
|
|
RGH-122 (compound 43) is an orally active, potent, selective, and hV1a receptor antagonist with Ki value of 0.3 nM and IC50 of 0.9 nM. RGH-122 showes microsomal stability with CLint value of 13/28/25 μL/min/mg .
|
-
- HY-104026CS
-
-
- HY-17498B
-
|
(RS)-Atenolol hydrochloride; Tenormin hydrochloride; ICI 66082 hydrochloride
|
Adrenergic Receptor
|
Cardiovascular Disease
Neurological Disease
Endocrinology
Cancer
|
|
Atenolol hydrochloride is a cardioselective β1-adrenergic receptor blocker, with a Ki of 697 nM at β1-adrenoceptor in guine pig left ventricle membrane. Atenolol hydrochloride can be used for the research of hypertension and angina pectoris .
|
-
- HY-B0203A
-
|
R 065824 hydrochloride
|
Adrenergic Receptor
|
Cardiovascular Disease
Endocrinology
Cancer
|
|
Nebivolol (R 065824) hydrochloride is an orally active beta receptor blocker and has the high beta(1)-receptor affinity.Nebivolol hydrochloride has direct vasodilator properties and adrenergic blocking characteristics. Nebivolol hydrochloride can be used for the research of kinds of diseases such as hypertension, coronary artery disease, congestive heart failure and ischemic heart disease .
|
-
- HY-B0203
-
|
R 065824
|
Adrenergic Receptor
|
Cardiovascular Disease
Endocrinology
Cancer
|
|
Nebivolol (R 065824) is an orally active beta receptor blocker and has the high beta(1)-receptor affinity. Nebivolol has direct vasodilator properties and adrenergic blocking characteristics. Nebivolol can be used for the research of kinds of diseases such as hypertension, coronary artery disease, congestive heart failure and ischemic heart disease .
|
-
- HY-19627A
-
|
S-297995 tosylate
|
Opioid Receptor
|
Neurological Disease
Metabolic Disease
|
|
Naldemedine (S-297995) tosylate is an orally active μ-opioid receptor antagonist (PAMORA) . Naldemedine tosylate shows potent binding affinities (Ki=0.34, 0.43, 0.94 nM, respectively) and antagonist activities (IC50=25.57, 7.09, 16.1 nM, respectively) for recombinant human μ-, δ-, and κ- opioid receptors . Naldemedine can be used in opioid-induced constipation (OIC) research . Naldemedine tosylate is predicted to bind to 3CL pro encoded by SARS-CoV2 genome .
|
-
- HY-19627
-
|
S-297995
|
Opioid Receptor
|
Neurological Disease
Metabolic Disease
|
|
Naldemedine (S-297995) is an orally active μ-opioid receptor antagonist (PAMORA) . Naldemedine shows potent binding affinities (Ki=0.34, 0.43, 0.94 nM, respectively) and antagonist activities (IC50=25.57, 7.09, 16.1 nM, respectively) for recombinant human μ-, δ-, and κ- opioid receptors . Naldemedine can be used in opioid-induced constipation (OIC) research . Naldemedine is predicted to bind to 3CL pro encoded by SARS-CoV2 genome .
|
-
- HY-135555
-
|
5-CT
|
5-HT Receptor
|
Neurological Disease
|
|
5-Carboxamidotryptamine (5-CT) is a 5-HT1A, 5-HT1B, 5-HT1D, 5-HT5A, 5-HT7 receptor agonist . 5-Carboxamidotryptamine has a Ki value of 4.6 nM for cloned human 5-HT5A receptor. 5-Carboxamidotryptamine causes a dose-dependent reduction in rectal temperature of mice .
|
-
- HY-P1329A
-
|
|
Opioid Receptor
|
Neurological Disease
|
|
CTOP TFA is a potent and highly selective μ-opioid receptor antagonist. CTOP TFA antagonizes the acute analgesic effect and hypermotility. CTOP TFA enhances extracellular dopamine levels in the nucleus accumbens. CTOP TFA dose-dependently enhances locomotor activity .
|
-
- HY-103053
-
|
|
VD/VDR
Apoptosis
|
Cancer
|
|
PS121912 is a selective vitamin D receptor (VDR)-coregulator inhibitor. PS121912 has acceptable metabolic stability in vivo. PS121912 can be used for the research of cancer .
|
-
- HY-P1389A
-
|
|
Neuropeptide S Receptor
|
Neurological Disease
|
|
Neuropeptide S human TFA, a neuropeptide, is a potent cognate neuropeptide S receptor (NPSR) agonist. Neuropeptide S human TFA can be used for Alzheimer's disease (AD) research .
|
-
- HY-134361
-
-
- HY-103187
-
|
|
Adenosine Receptor
|
Inflammation/Immunology
Cancer
|
|
HEMADO is a potent and selective adenosine A3 receptor agonist with a Ki of 1.1 nM at the human A3 subtype . HEMADO is a click chemistry reagent, it contains an Alkyne group and can undergo copper-catalyzed azide-alkyne cycloaddition (CuAAc) with molecules containing Azide groups.
|
-
- HY-P3785
-
|
|
PKA
|
Neurological Disease
|
|
PKI(5-22)amide is the active inhibitory fragment of the inhibitor of the cyclic AMP-dependent protein kinase (PKA). PKI(5-22)amide inhibits PKA activation, but fails to attenuate homologous desensitization of CRF1 receptors .
|
-
- HY-Z7721
-
|
(Rac)-TRK-100; (Rac)-ML 1129 sodium
|
Prostaglandin Receptor
|
Cardiovascular Disease
|
|
(Rac)-Beraprost ((Rac)-ML 1129) sodium is a racemic isomer of Beraprost sodium (HY-13569A). Beraprost sodium is an orally active prostacyclin analog that inhibits the release of Ca 2+ from intracellular storage sites by binding to prostacyclin membrane receptors (Prostaglandin Receptor), leading to relaxation of smooth muscle cells and vasodilation. Beraprost sodium has vasodilatory, antiplatelet, and cytoprotective effects, making it promising for research in the field of cardiovascular diseases, such as thromboangiitis obliterans and atherosclerosis .
|
-
- HY-B0781R
-
|
|
Histamine Receptor
mAChR
Adrenergic Receptor
|
Neurological Disease
Endocrinology
|
Promethazine (hydrochloride) (Standard) is the analytical standard of Promethazine (hydrochloride). This product is intended for research and analytical applications. Promethazine hydrochloride is an orally active phenothiazine derivative with antihistaminic (H1), sedative, antiemetic, anticholinergic, and antimotion sickness properties. Promethazine hydrochloride is a potent H1 receptor antagonist and a mAChR antagonist. It also has a certain affinity for 5-HT2A and 5-HT2C receptors .
|
-
- HY-P4874
-
|
|
Melanocortin Receptor
|
Metabolic Disease
|
|
ACTH (7-38) (human) is the 7-38 fragment of human ACTH (1-39). human ACTH (1-39), known as a corticotropin inhibitory peptide (CIP), is an antagonist of the ACTH receptor and has no any corticosteroid activity .
|
-
- HY-B0121R
-
|
GR 43175 succinate (Standard)
|
5-HT Receptor
|
Neurological Disease
|
|
Sumatriptan (succinate) (Standard) is the analytical standard of Sumatriptan (succinate). This product is intended for research and analytical applications. Sumatriptan succinate (GR 43175) is an orally active 5-HT1 receptor agonist with Kis of 17 nM, 27 nM and 100 nM for 5-HT1D, 5-HT1B and 5-HT1A receptors, respectively. Sumatriptan succinate can be used for migraine headache research .
|
-
- HY-147086
-
|
|
Leukotriene Receptor
G protein-coupled Bile Acid Receptor 1
TNF Receptor
|
Metabolic Disease
Inflammation/Immunology
|
|
CAY10789 (compound 6) is a potent CysLT1R (cysteinyl leukotriene receptor 1) antagonist (IC50=2.80 μM) and GPBAR1 (G-protein-coupled bile acid receptor 1) agonist (EC50=3 μM). CAY10789 significantly reduces the adhesion of U937 cells to HAEC, reduces the expression of TNF-α. CAY10789 shows very promising metabolic stability and excellent pharmacokinetics. CAY10789 can be used for the research of colitis, metabolic syndromes, and other GPBAR1/CysLT1R-related diseases .
|
-
- HY-18200A
-
|
E5555 hydrochloride; ER-172594-00 hydrochloride
|
Protease Activated Receptor (PAR)
JAK
Apoptosis
|
Cardiovascular Disease
Cancer
|
|
Atopaxar hydrochloride (E5555 hydrochloride) is the hydrochloride salt form of Atopaxar (HY-18200). Atopaxar hydrochloride is an orally active, selective and reversible antagonist for thrombin receptor protease-activated receptor-1 (PAR-1). Atopaxar hydrochloride is the inhibitor for Janus kinase 1 (JAK1) and JAK2, which inhibits the JAK-STAT with EC50 of 5.90 μM in A549. Atopaxar hydrochloride inhibits the cell viability of A549 (IC50=7.02 μM), arrests the cell cycle at G1 phase and induces apoptosis. Atopaxar hydrochloride exhibits antiplatelet and antitumor activities. Atopaxar hydrochloride can be used for the research of atherothrombotic disease .
|
-
- HY-110152
-
|
|
mGluR
|
Neurological Disease
|
|
LSN2463359 is positive allosteric modulator of metabotropic glutamate 5 (mGlu5). LSN2463359 attenuates aspects of the behavioral response to administration of the competitive NMDA receptor antagonist. LSN2463359 selectively attenuates reversal learning deficits observed in the neurodevelopmental MAM E17 model . LSN2463359 is a click chemistry reagent, it contains an Alkyne group and can undergo copper-catalyzed azide-alkyne cycloaddition (CuAAc) with molecules containing Azide groups.
|
-
- HY-133045
-
|
|
Ligands for E3 Ligase
|
Cancer
|
|
VHL Ligand 8 is a VHL ligand. VHL Ligand 8 can be used to synthesize ARD-266 (HY-133020), a highly potent and VHL E3 ligase-based androgen receptor (AR) PROTAC degrader. ARD-266 effectively induces degradation of AR protein in AR-positive LNCaP, VCaP, and 22Rv1 prostate cancer cell lines with DC50 values of 0.2-1 nM .
|
-
- HY-17498
-
-
- HY-16532
-
|
AEZS-108; AN-152
|
Peptide-Drug Conjugates (PDCs)
GnRH Receptor
|
Cancer
|
|
Zoptarelin doxorubicin (AEZS-108; AN-152) is a hybrid anticancer agent, containing Zoptarelin and Doxorubicin. Zoptarelin doxorubicin has been used to research targeting tumors expressing LHRH receptors. Zoptarelin doxorubicin abolishes tumor progression and induces remarkable apoptosis in vitro .
|
-
- HY-P2673
-
|
KRTLRR
|
EGFR
|
Others
|
|
Lys-Arg-Thr-Leu-Arg-Arg (KRTLRR) is a hexapeptide. Lys-Arg-Thr-Leu-Arg-Arg is a substrate of protein kinase C from EGF receptor. Lys-Arg-Thr-Leu-Arg-Arg can be used to determine the activity of protein kinase C .
|
-
- HY-106407
-
|
Org 4428; ADL 6906
|
Adrenergic Receptor
5-HT Receptor
|
Neurological Disease
|
|
Beloxepin (Org 4428) is an orally active synaptosomal noradrenalin reuptake inhibitor and a 5-HT2 receptor antagonist. Beloxepin shows about 100-fold less affine for other monoamine carriers. Beloxepin has antidepressant and pain-relieving effects .
|
-
- HY-B0160R
-
|
|
Histamine Receptor
|
Metabolic Disease
Endocrinology
|
|
Lafutidine (Standard) is the analytical standard of Lafutidine. This product is intended for research and analytical applications. Lafutidine (FRG-8813) is a histamine H2-receptor antagonist (H2RA), with proven gastric mucosal protective effects. Lafutidine can be used for the research of gastroesophageal reflux disease .
|
-
- HY-N3230
-
|
Murraxocin
|
TRP Channel
|
Inflammation/Immunology
|
|
Murpanicin (murraxocin) is a coumarin that is a thermosensitive transient receptor potential vanilloid 2 (TRPV2) channel inhibitor. Murpanicin has significant anti-inflammatory and insecticidal effects.
|
-
- HY-N3359
-
-
- HY-108250
-
|
|
Androgen Receptor
|
Cancer
|
|
(R)-Bicalutamide is the (R)-enantiomer of Bicalutamide (HY-14249). (R)-Bicalutamide is an androgen receptor (AR) antagonist, with antineoplastic activity. (R)-Bicalutamide is widely used for the research of prostate cancer .
|
-
- HY-N3359B
-
|
D-Lupanine hydrochloride
|
nAChR
|
Neurological Disease
|
|
Lupanine (D-Lupanine) hydrochloride is a natural ketonic derivative of Sparteine ((+)-Sparteine (HY-W008350)) with a ganglioplegic activity. Lupanine hydrochloride shows binding affinity for nicotinic receptor (nAChR) with a Ki value of 500 nM .
|
-
- HY-14407
-
-
- HY-145837
-
|
|
Neuropeptide Y Receptor
|
Cancer
|
|
Y1R probe-1 (Compound 39) is a high-affinity fluorescence probe for the Neuropeptide Y Y1 Receptor. Y1R probe-1 has the potential for the research of cancer disease .
|
-
- HY-170786
-
|
IRX4647F
|
RAR/RXR
|
Cancer
|
|
IRX5010 (IRX4647F), an analogue of IRX4647, is a highly selective RARγ nuclear receptor agonist. IRX5010 demonstrates inhibition of in vivo growth of EMT-6 triple negative breast cancer .
|
-
- HY-17417AR
-
|
|
Opioid Receptor
|
Neurological Disease
Cancer
|
|
Naloxone (Standard) is the analytical standard of Naloxone. This product is intended for research and analytical applications. Naloxone is an antagonist of Opioid receptor. Naloxone alleviates opioid-overdose-induced respiratory depression. Naloxone may cause pulmonary edema and cardiac arrhythmias .
|
-
- HY-116326
-
|
|
Leukotriene Receptor
|
Inflammation/Immunology
|
|
BayCysLT2, an isophthalic acid derivative, is a selective and potent cysteinyl leukotriene 2 (CysLT2) receptor antagonist with an IC50 value of 53 nM. BayCysLT2 inhibits calcium mobilization induced by leukotriene D4 in HEK293 cells expressing human CysLT2 receptors. BayCysLT2 reverses LTC4-induced increases in coronary artery perfusion pressure and decreases in contractility in isolated perfused guinea pig hearts .
|
-
- HY-150734A
-
|
|
Toll-like Receptor (TLR)
|
Infection
|
|
ODN 2007 sodium, a class B CpG ODN (oligodeoxynucleotide), is a Toll-like receptor (TLR) ligand. ODN 2007 sodium can be used as an immunomodulator, vaccine adjuvant, and enhance immune responses in mammals, fish, and humans. ODN 2007 sequence: 5'-TCGTCGTTGTCGTTTTGTCGTT-3' .
|
-
- HY-150734
-
|
|
Toll-like Receptor (TLR)
|
Infection
Inflammation/Immunology
|
|
ODN 2007, a class B CpG ODN (oligodeoxynucleotide), is a Toll-like receptor (TLR) ligand. ODN 2007 can be used as an immunomodulator, vaccine adjuvant, and enhance immune responses in mammals, fish, and humans. ODN 2007 sequence: 5'-TCGTCGTTGTCGTTTTGTCGTT-3' .
|
-
- HY-104026BS
-
-
- HY-163276
-
-
- HY-108670
-
|
|
P2X Receptor
|
Inflammation/Immunology
|
|
AZ11645373 is a highly selective and potent antagonist at human but not rat P2X7 receptors，AZ11645373 inhibits ATP-evoked IL-1β release from lipopolysaccharide-activated THP-1 cells , with an IC50 value of 90 nM .
|
-
- HY-114667
-
|
|
EGFR
|
Others
|
|
Lavendustin C6 is a specific inhibitor of tyrosine kinase. Lavendustin C6 inhibits epidermal growth factor (EGF) receptor tyrosine kinase with an EC50 value of 0.05 μg/mL. Lavendustin C6 inhibits platelet-derived growth factor (PDGF)-induced inositol phosphate formation .
|
-
- HY-151100
-
|
|
GPR84
|
Inflammation/Immunology
|
|
GPR84 antagonist 3 (compound 42) is a potent GPR84 (G-protein-coupled receptor 84) antagonist. GPR84 antagonist 3 inhibits GTPγS, with a pIC50 of 8.28. GPR84 antagonist 3 has a favorable pharmacokinetic profile suitable .
|
-
- HY-P99626
-
|
LY 3015014
|
PCSK9
|
Metabolic Disease
|
|
Frovocimab (LY 3015014) is a humanized IgG4 monoclonal antibody (mAb) that neutralizes PCSK9. Frovocimab inhibits PCSK9 binding to LDL receptor (LDLR) while permitting the normal proteolytic cleavage of the bound intact PCSK9 .
|
-
- HY-15078
-
|
(R)-SPD502
|
iGluR
|
Neurological Disease
|
|
NS1219 ((R)-SPD502) is the isomer of NS 1209 HY-15074. NS1209 is a selective AMPA receptor antagonist with neuroprotective activity. NS1209 can be used for the research of stroke, neuropathic pain and epilepsy .
|
-
- HY-114814
-
|
|
Adrenergic Receptor
|
Neurological Disease
|
|
ORM-10921 free base is a selective α-2C adrenergic receptor antagonist with a Ki of 1.4 nM. ORM-10921 free base displays potent antidepressant and antipsychotic-like effects .
|
-
- HY-P5558
-
|
|
VEGFR
|
Inflammation/Immunology
|
|
KLTWQELYQLKYKGI (QK) is a VEGF mimicking peptide, binds to the VEGF receptors and competes with VEGF. KLTWQELYQLKYKGI is active in gastric ulcer healing in rodents when administered either orally or systemically. KLTWQELYQLKYKGI shows the ability to induce capillary formation and organization in vitro .
|
-
- HY-P10379
-
|
|
Neuropeptide FF Receptor
|
Others
Neurological Disease
|
|
palm-PrRP31 is a potent dual receptor agonist for both GPR10 (EC50=72 pM) and NPFF-R2. palm-PrRP31 activates downstream signaling pathways through binding to its receptors, GPR10 and NPFF-R2, which results in reduced appetite and increased energy expenditure. Utilizing palm-PrRP31 facilitates the study of the mechanism of action in the nervous system, thereby elucidating the complex biological processes that regulate appetite and energy expenditure .
|
-
- HY-100991
-
|
ZK 39106; LSU-65
|
GABA Receptor
|
Neurological Disease
|
|
FG 7142 (ZK 39106; LSU-65), a non-selectively benzodiazepine inverse agonist, has high affinity for the α1 subunit-containing GABAA receptor (Ki=91 nM). FG 7142 (ZK 39106; LSU-65) also modulates GABA-induced chloride flux at GABAA receptors expressing the α1 subunit (EC50= 137 nM). FG 7142 (ZK 39106; LSU-65) can increase tyrosine hydroxylation and cause upregulation of?β-adrenoceptors in mouse cerebral cortex .
|
-
- HY-149504
-
|
|
Drug Metabolite
mAChR
|
Neurological Disease
|
|
3-Hydroxy darifenacin is a metabolite of Darifenacin (HY-A0033). 3-Hydroxy darifenacin is an antagonist of M1-5 muscarinic receptors with Kis values of 17.78, 79.43, 2.24, 36.31 and 6.17 nM, respectively in CHO cells .
|
-
- HY-P3561
-
|
|
Melanocortin Receptor
|
Neurological Disease
|
|
Agouti-related Protein (AGRP) (83-132) Amide (human) is a fragment of agouti-related protein (AGRP) which is a protein found in abundance in the arcuate nucleus of the hypothalamus. AgRP primarily acts as an inverse agonist for the melanocortin-4 receptor (MC4R) to increase food intake .
|
-
- HY-P1112
-
-
- HY-101250
-
|
MDL11939
|
Serotonin Transporter
|
Neurological Disease
|
|
Glemanserin (MDL11939) is a potent and selective antagonist for serotonin receptor 5-HT2A (Ki=2.89, 0.54 and 2.5 nM for rat 5-HT2A, rabbit 5-HT2A and human 5-HT2A, respectively) .
|
-
- HY-W009681
-
|
|
5-HT Receptor
Serotonin Transporter
Drug Intermediate
|
Infection
Neurological Disease
|
|
1-(2-Methoxyphenyl)piperazine hydrochloride is a key agent intermediate of antipsychotics with high affinity to the serotonin receptors and 5-HT, which can be used to synthesize the intestinal worm-repellent agents Piperazine phosphate (HY-B0912C) and Piperazine citrate (HY-17599), as well as Fluphenazine (HY-119980), dihydrochloride, Rifampicin (HY-B0272) .
|
-
- HY-145709
-
|
|
Androgen Receptor
|
Cancer
|
|
Ar-V7-IN-1 is a potent inhibitor of Ar-V7. AR-V7 is a hormone-independent splice variant of the androgen receptor. Ar-V7-IN-1 has the potential for the research of various indications, in particular cancers such as prostate cancer (extracted from patent WO2018114781A1, compound 43) .
|
-
- HY-N7272R
-
|
|
Phosphodiesterase (PDE)
|
Metabolic Disease
|
|
Cirsimarin (Standard) is the analytical standard of Cirsimarin. This product is intended for research and analytical applications. Cirsimarin is a potent antilipogenic flavonoid isolated from Microtea debilis. Cirsimarin exerts potent antilipogenic effect and decreases adipose tissue deposition in mice. The lipolytic activity of Cirsimarin resulting from both its antagonist activity on adenosin A1 receptor and its inhibitory effect on phosphodiesterase .
|
-
- HY-W007355
-
Skatole
5 Publications Verification
3-Methylindole; 3-Methyl-1H-indole
|
Aryl Hydrocarbon Receptor
p38 MAPK
Endogenous Metabolite
Apoptosis
|
Others
|
|
Skatole (3-methylindole) is a heterocyclic compound naturally found in the feces of vertebrates and can be found in certain plants. Skatole can be produced by intestinal bacteria, inducing apoptosis of intestinal epithelial cells through activating aryl hydrocarbon receptors (AhR) and p38. Skatole has been used in specific products of the perfume industry or as a flavor additive in ice cream .
|
-
- HY-130630
-
|
|
mGluR
|
Neurological Disease
|
|
mGluR2 modulator 1 (compound 95) is a potent and BBB-penetrated mGluR2 (metabotropic glutamate receptor-2) positive allosteric modulator, with an EC50 of 0.03 μM. mGluR2 modulator 1 can be used for psychosis research .
|
-
- HY-B1487
-
|
Tricyclamol hydrochloride; (±)-Procyclidine hydrochloride
|
iGluR
mAChR
|
Neurological Disease
|
|
Procyclidine (Tricyclamol, (±)-Procyclidine) hydrochloride , an anticholinergic agent, is a muscarinic receptor antagonist that also has the properties of an N-methyl-D-aspartate (NMDA) antagonist. Procyclidine hydrochloride can be used in studies of Parkinson's disease and related psychiatric disorders such as Soman-induced epilepsy .
|
-
- HY-119087
-
-
- HY-117378
-
|
KRP-204
|
Adrenergic Receptor
|
Inflammation/Immunology
Cancer
|
|
N-5984 (KRP-204) is a potent and selective agonist of β3-adrenergic receptor. N-5984 has the potential for developing as one of the clinically effective drugs for obesity and diabetes mellitus .
|
-
- HY-P99435
-
|
BRII-196
|
SARS-CoV
|
Infection
|
Amubarvimab (BRII-196) is a human IgG1 mAb that bind to non-competing epitopes on the receptor binding domain (RBD) of spike protein, with a KD of 5.88 nM. Amubarvimab can effectively neutralize SARS-CoV-2 variants .
|
-
- HY-B1487A
-
|
Tricyclamol; (±)-Procyclidine
|
mAChR
iGluR
|
Neurological Disease
|
|
Procyclidine (Tricyclamol; (±)-Procyclidine), an anticholinergic agent, is a muscarinic receptor antagonist that also has the properties of an N-methyl-D-aspartate (NMDA) antagonist. Procyclidine can be used in studies of Parkinson's disease and related psychiatric disorders such as Soman-induced epilepsy .
|
-
- HY-N3359A
-
|
D-Lupanine perchlorate
|
nAChR
|
Neurological Disease
|
|
Lupanine (D-Lupanine) perchlorate is a natural ketonic derivative of Sparteine ((+)-Sparteine (HY-W008350)) with a ganglioplegic activity. Lupanine perchlorate shows binding affinity for nicotinic receptor (nAChR) with a Ki value of 500 nM .
|
-
- HY-14249S1
-
-
- HY-14249R
-
|
|
Androgen Receptor
Autophagy
|
Cancer
|
|
Bicalutamide (Standard) is the analytical standard of Bicalutamide. This product is intended for research and analytical applications. Bicalutamide is an orally active non-steroidal androgen receptor (AR) antagonist. Bicalutamide can be used for the research of prostate cancer .
|
-
- HY-14407A
-
|
MK-0517; L785298
|
Neurokinin Receptor
|
Neurological Disease
Endocrinology
Cancer
|
|
Fosaprepitant dimeglumine (MK-0517) is a proagent of Aprepitant (HY-10052). Fosaprepitant dimeglumine is a neurokinin-1 receptor antagonist, which is development for the prevention of chemotherapy-induced nausea and vomiting (CINV) .
|
-
- HY-101108
-
|
AGN 190299
|
Drug Metabolite
|
Others
|
|
Tazarotenic acid is the metabolite of Tazarotene. Tazarotenic acid binding to retinoic acid receptors (RARs) is the probable molecular target of retinoid action. Tazarotenic acid has the potential for the research of warty dyskeratoma .
|
-
- HY-P3561A
-
|
|
Melanocortin Receptor
|
Neurological Disease
|
|
Agouti-related Protein (AGRP) (83-132) Amide (human) TFA is a fragment of agouti-related protein (AGRP) which is a protein found in abundance in the arcuate nucleus of the hypothalamus. AgRP primarily acts as an inverse agonist for the melanocortin-4 receptor (MC4R) to increase food intake .
|
-
- HY-129995
-
|
|
TSH Receptor
|
Endocrinology
|
|
TSHR antagonist S37b is the less effective enantiomer of TSHR antagonist S37a (HY-129995A). TSHR antagonist S37b shows only a minor effect for thyrotropin receptor (TSHR) inhibition. TSHR antagonist S37b can be used for the research of thyroid function .
|
-
- HY-118424
-
|
|
iGluR
|
Neurological Disease
|
|
JNJ-55511118 is a highly potent, reversible, and selective AMPA receptor inhibitor selective for TARP-γ8. JNJ-55511118 fully displaces the radioligand (20 nM) with the Ki of 26 nM in competition binding experiments. JNJ-55511118 is a tool molecule with potential therapeutic utility as an anticonvulsant or neuroprotectant .
|
-
- HY-107404
-
|
|
Orphan Receptor
|
Endocrinology
|
|
SID 7969543 is a selective SF-1 (steroidogenic factor 1, NR5A1) inhibitor with an IC50 of 760 nM. SID 7969543 inhibits SF-1-triggered luciferase expression with IC50 of 30 nM. SF-1 is a transcription factor belonging to the nuclear receptor superfamily .
|
-
- HY-153935
-
-
- HY-113802
-
|
|
Histamine Receptor
|
Neurological Disease
|
|
VUF 8328 is a potent histamine H(3) receptor agonist. VUF 8328 inhibits the electrically-evoked [ 3H]-no-radrenaline release from rat cortical slices. VUF 8328 is promising for research of central nervous system disorders .
|
-
- HY-19434A
-
|
|
iGluR
mGluR
|
Neurological Disease
|
|
cis-ACPD is a potent agonist of NMDA receptor, with an IC50 of 3.3 μM. cis-ACPD is also a selective agonist of group II mGluR, with EC50s of 13 μM and 50 μM for mGluR2 and mGluR4, respectively .
|
-
- HY-18963
-
|
RG-14355
|
EGFR
|
Cancer
|
|
Lavendustin A (RG-14355) is a potent, selective and ATP-competitive inhibitor of epidermal growth factor receptor (EGFR) tyrosine kinase, with an IC50 of 11 nM. Lavendustin A does not inhibit protein kinase A or C. Lavendustin A can suppress VEGF-induced angiogenesis .
|
-
- HY-19884
-
|
RM-131; BIM-28131
|
GHSR
|
Metabolic Disease
|
|
Relamorelin (RM-131), a pentapeptide ghrelin analog, is a selective ghrelin/growth hormone secretagogue receptor (GHSR) agonist with a Ki of 0.42 nM for GHS-1a receptor. Relamorelin is centrally penetrant. Relamorelin increases growth hormone levels and accelerates gastric emptying. Relamorelin has the potential for cachexia, gastroparesis, and gastric/intestinal dysmobility disorders research .
|
-
- HY-113689
-
|
|
Cannabinoid Receptor
|
Neurological Disease
|
|
GAT211 is a cannabinoid 1 receptor (CB1R) positive allosteric modulator (PAM). GAT211 activates cAMP and β-arrestin2 with EC50 values of 260 nM and 650 nM, respectively. GAT211 inhibits GAT211 can be used for neuropathic and/or inflammatory pain research .
|
-
- HY-N12744
-
|
|
Glucocorticoid Receptor
|
Metabolic Disease
|
|
2-O-trans-p-Coumaroylalphitolic acid (Zj7) is a triterpene which can be extracted from jujube plants. 2-O-trans-P-Coumaroyl alphitolic acid is a selective modulator of glucocorticoid receptor (GR). 2-O-trans-P-coumaroyl alphitolic acid can be used in the study of obesity .
|
-
- HY-P1112A
-
|
|
Endothelin Receptor
|
Cardiovascular Disease
Neurological Disease
|
|
Sarafotoxin S6a TFA , a sarafotoxin analogue, is a endothelin receptor agonist and has an ETA/ETB selectivity profile similar to that of Endothelin-3 (HY-P0204). Sarafotoxin S6a TFA elicits the pig coronary artery with an EC50 value of 7.5 nM .
|
-
- HY-168031
-
-
- HY-18314
-
-
- HY-120081A
-
|
|
mAChR
|
Neurological Disease
|
|
Metixene (Piperidine) hydrochloride hydrate is an anticholinergic and antiparkinsonian agent. Metixene hydrochloride hydrate potently inhibits binding of quinuclidinyl benzilate (QNB) with the muscarinic receptor, IC50 and Ki values of 55 nM and 15 nM, respectively. Metixene hydrochloride hydrate can be used for the research of parkinsonian .
|
-
- HY-120081
-
|
|
mAChR
|
Neurological Disease
|
|
Metixene (Piperidine) is an anticholinergic and antiparkinsonian agent. Metixene potently inhibits binding of quinuclidinyl benzilate (QNB) with the muscarinic receptor, IC50 and Ki values of 55 nM and 15 nM, respectively. Metixene can be used for the research of parkinsonian .
|
-
- HY-120081B
-
|
|
mAChR
|
Neurological Disease
|
|
Metixene (Piperidine) hydrochloride hydrate is an anticholinergic and antiparkinsonian agent. Metixene hydrochloride potently inhibits binding of quinuclidinyl benzilate (QNB) with the muscarinic receptor, IC50 and Ki values of 55 nM and 15 nM, respectively. Metixene hydrochloride can be used for the research of parkinsonian .
|
-
- HY-113044
-
|
|
Endogenous Metabolite
P2Y Receptor
|
Metabolic Disease
|
|
Uridine diphosphate glucose is the precursor of glucose-containing oligosaccharides, polysaccharides, glycoproteins, and glycolipids in animal tissues and in some microorganisms. Uridine diphosphate glucose is an agonist of the P2Y14 receptor, a neuroimmune system GPCR 1.
|
-
- HY-P10380
-
|
|
Neuropeptide FF Receptor
|
Neurological Disease
|
|
palm11-PrRP31 is a lipidized endogenous appetite inhibitory neuropeptide (PrRP) analogue. palm11-PrRP31 is GPR10 (EC50=39 pM) and NPFF-R2 effective dual agonists. palm11-PrRP31 is able to mimic the natural function of PrRP by binding to these receptors to reduce food intake. palm11-PrRP31 can be used as a potential anti-obesity agent and for the study of neuropeptide-receptor interaction .
|
-
- HY-B0121BS2
-
|
GR 43175 free base-d5
|
5-HT Receptor
Isotope-Labeled Compounds
|
Neurological Disease
|
|
Sumatriptan-d5 is deuterated labeled Sumatriptan (HY-B0121B). Sumatriptan (GR 43175) is an orally active 5-HT1 receptor agonist with IC50s of 7.3 nm, 9.3nm and 17.8 nm for 5-HT1D, 5-HT1B and 5-HT1F receptors, respectively. Sumatriptan can be used for migraine headache research .
|
-
- HY-N6070A
-
|
|
Prostaglandin Receptor
|
Inflammation/Immunology
|
|
Ricinoleic acid (purity≥99%), a hydroxy fatty acid, is an attractive feedstock for the production of high-performance lubricants, cosmetics, polymers, surfactants, and coatings. Ricinoleic acid is the main active ingredient of Castor oil (HY-107799). Ricinoleic acid is the agonist for prostaglandin EP3 receptor (EP3 receptor) (EC50 in MEG-01 is 0.5 μM), that causes laxative effects and uterine contraction. Ricinoleic acid exhibits antianxiety-like, anti-inflammatory and pro-inflammatory properties .
|
-
- HY-124146
-
|
|
Syk
|
Inflammation/Immunology
|
|
BI1002494 is an orally active, potent, and selective spleen tyrosine kinase (SYK) inhibitor. BI 1002494 exhibits an IC50 of 115 nM in inhibiting high-affinity IgE receptor-mediated mast cell and basophil degranulation. BI1002494 can be utilized in immunology reesearch .
|
-
- HY-107561
-
|
|
Histamine Receptor
|
Inflammation/Immunology
|
|
A-943931 (Compound 10) is a histamine H4 receptor antagonists. A-943931 has improved pharmacotropic and in vivo efficacy in models of pain and inflammation. A-943931 can be used in vivo anti-inflammatory and anti-nociception research .
|
-
- HY-156111
-
|
|
PROTACs
Androgen Receptor
|
Cancer
|
|
ARD-1676 is an orally available androgen receptor (AR) PROTAC degrader, consisting of AR ligand and cereblon ligand. ARD-1676 has AR-degrading activity in vitro and in vivo and inhibits VCaP tumor growth in mouse xenograft tumor models .
|
-
- HY-14756
-
|
|
Thrombopoietin Receptor
|
Others
|
|
Totrombopag is an orally effective thrombopoietin receptor (TpoR) agonist. By activating TpoR, Totrombopag initiates an intracellular signaling cascade mediated by JAK2 kinase and the transcription factor Stat5, a signaling process that is the primary mechanism regulating megakaryocyte growth and differentiation into platelets. Totrombopag can be used to study platelet production and megakaryocyte biology .
|
-
- HY-112741
-
|
|
Leukotriene Receptor
|
Inflammation/Immunology
|
|
SB-209247 is a selective, high affinity and orally active leukotriene B4 (LTB4) receptor antagonist with a Ki of 0.78 nM. SB-209247 blocks LTB4-induced Ca 2+ mobilization with an IC50 of 6.6 nM. SB-209247 shows a potent anti-inflammatory activity .
|
-
- HY-125314
-
|
|
Cholecystokinin Receptor
|
Endocrinology
Cancer
|
|
AG-041R is a potent and selective CCK2 Receptor/Gastrin antagonist. AG-041R inhibits gastrin-evoked secretion of pancreastatin with an IC50 of 2.2 nM. AG-041R inhibits cell growth of Mastomys ECL carcinoid tumor cells .
|
-
- HY-100234A
-
|
|
mAChR
|
Neurological Disease
|
|
DREADD agonist 21 dihydrochloride is a potent human muscarinic acetylcholine M3 receptors (hM3Dq) agonist (EC50=1.7 nM) .
|
-
- HY-100234
-
|
|
mAChR
|
Neurological Disease
|
|
DREADD agonist 21 is a potent human muscarinic acetylcholine M3 receptors (hM3Dq) agonist (EC50=1.7 nM) .
|
-
- HY-117820
-
-
- HY-19608
-
-
- HY-10315
-
|
RWJ-53308
|
Integrin
|
Cardiovascular Disease
|
|
Elarofiban (RWJ-53308) is a nonpeptide, orally active antagonist for fibrinogen receptor αIIbβ3 (GPIIb/IIIa), with an IC50 of 0.15 nM. Elarofiban has the potential for platelet mediated thrombotic disorders research .
|
-
- HY-19884A
-
|
RM-131 acetate; BIM-28131 acetate
|
GHSR
|
Metabolic Disease
|
|
Relamorelin (RM-131) acetate, a pentapeptide ghrelin analog, is a selective ghrelin/growth hormone secretagogue receptor (GHSR) agonist with a Ki of 0.42 nM for GHS-1a receptor. Relamorelin acetate is centrally penetrant. Relamorelin acetate increases growth hormone levels and accelerates gastric emptying. Relamorelin acetate has the potential for cachexia, gastroparesis, and gastric/intestinal dysmobility disorders research .
|
-
- HY-103178
-
|
|
Adenosine Receptor
|
Inflammation/Immunology
|
|
MRE3008F20 is a highly efficient, highly selective and radioactive adenosine A3 receptor (AA3R) antagonist (Ki=1.8 nM). MRE3008F20 effectively antagonises Cl-IB-MECA-induced cAMP production in resting lymphocytes with an IC50 value of 5 nM. MRE3008F20 can be used in the study of AA3R .
|
-
- HY-P3839
-
|
|
Opioid Receptor
|
Neurological Disease
|
|
Nocistatin, a neuropeptide, is an endogenous ligand for the orphan opioid receptor-like receptor. Nocistatin is also a functional antagonist of neuropeptide nociceptin or orphanin FQ (Noc/OFQ). Nocistatin inhibits 5-HT release via a Gi/o proteinmediated pathway. Nocistatin blocks Nociceptin (Nociceptin)-induced allodynia and hyperalgesia .
|
-
- HY-153437
-
|
|
RIP kinase
|
Cancer
|
|
RIP1 kinase inhibitor 7 (compound 41) is a potent receptor interacting protein 1 kinase (RIP1) Inhibitor with an IC50 of <100 nM for human RIP1. RIP1 kinase inhibitor 7 has an EC50 of 1-100 nM in the cell necrosis assay .
|
-
- HY-135882
-
-
- HY-156280
-
|
|
RAR/RXR
|
Endocrinology
|
|
RARα antagonist 1 (compound 21) is an orally active and selective retinoic acid receptor α(RARα) antagonist, with the IC50 of 4.6nM .
|
-
- HY-14824A
-
|
ABT 894 benzenesulfonate
|
nAChR
|
Neurological Disease
|
|
Sofinicline benzenesulfonate (ABT 894 benzenesulfonate) is a novel nicotinic acetylcholine receptor agonist, specifically acting on the α4β2 subtype of nAChR (IC50=0.1 nM). Sofinicline benzenesulfonate has the potential to improve cognitive function, including attention, memory and working memory. Sofinicline benzenesulfonate can be used in studies of attention deficit, hyperactivity disorder (ADHD) .
|
-
- HY-157303
-
|
|
Somatostatin Receptor
|
Cardiovascular Disease
|
|
SSTR5 antagonist 3 (Compound 23) is an orally active somatostatin receptor subtype 5 (SSTR5) antagonist with low hERG inhibition. SSTR5 antagonist 3 exhibits potency with IC50 values of 2.8 nM and 1.4 nM in human and mouse, respectively. SSTR5 antagonist 3 can be used for the research of anti-gallstone .
|
-
- HY-132935
-
|
|
c-Fms
|
Inflammation/Immunology
Cancer
|
|
BPR1R024 is an orally active and selective colony-stimulating factor-1 receptor (CSF1R) inhibitor. BPR1R024 has potent CSF1R inhibition activity with an IC50 value of 0.53 nM. BPR1R024 can be used for the research of immuno-oncology .
|
-
- HY-147357
-
|
|
TRP Channel
|
Cardiovascular Disease
|
|
TRPC3/6-IN-1 is a potent selectivity blocker of the canonical transient receptor channels (TRPC3/6), has block potency for hTRPC3 and hTRPC6 with IC50 values of 1260 nM and 500 nM, respectively. TRPC3/6-IN-1 can be used for the research of chronic models of heart failure .
|
-
- HY-119832B
-
|
(S)-EGIS-2062 free acid; (S)-EGYT-2062 free acid
|
Histamine Receptor
|
Inflammation/Immunology
|
|
(S)-Setastine ((S)-EGIS-2062 free acid) is a non-sedating, highly potent antagonist of H1 receptor-mediated responses. (S)-Setastine has a long-lasting antihistamine effect and good oral efficacy. (S)-Setastine can be used in the research of allergic diseases .
|
-
- HY-161273
-
|
|
TRP Channel
|
Neurological Disease
|
|
TRPV1 antagonist 6 (compound 51) is a mode-selective antagonist for transient receptor potential vanilloid member 1 (TRPV1), which shows antagonism with IC50 of 2.85 nM to capsaicin activation and 28.48 % inhibition against proton activation at a 3 µM concentration .
|
-
- HY-103522
-
|
|
GABA Receptor
|
Neurological Disease
|
|
AA29504 is a ethyl carbamate with γ-aminobutyric acid (GABAA(HY-L120) receptor activity. AA29504 inhibits the delivery of the neurotransmitter gamma-aminobutyric acid in the central nervous system. AA29504 can be used to research anxiety, insomnia and other neuropsychiatric diseases .
|
-
- HY-N6932
-
-
- HY-146288
-
|
|
LXR
|
Metabolic Disease
|
|
LXR agonist 2 (compound 18rr) is a potent LXR (liver X receptor) agonist. LXR agonist 2 can stabilize NCOA1 (co-activator), leading to LXR agonism .
|
-
- HY-107745
-
-
- HY-110050
-
-
- HY-111348
-
|
Ro 44-9883
|
Integrin
|
Cardiovascular Disease
|
|
Lamifiban is a nonpeptide glycoprotein IIb/IIIa receptor and platelet aggregation antagonist. Lamifiban in combination with thrombolytic therapy effectively restores coronary arterial patency. Lamifiban is promising for research of acute coronary syndromes .
|
-
- HY-13728
-
|
ZD 9331; BGC9331
|
Thymidylate Synthase
|
Cancer
|
|
Plevitrexed (ZD 9331; BGC 9331) is an orally active and potent thymidylate synthase (TS) inhibitor with a Ki of 0.44 nM. Plevitrexed is taken up via the α-folate receptor as well as the reduced folate carrier. Plevitrexed is used for gastric cancer in clinical . Plevitrexed is a click chemistry reagent, it contains an Alkyne group and can undergo copper-catalyzed azide-alkyne cycloaddition (CuAAc) with molecules containing Azide groups.
|
-
- HY-125641
-
|
|
5-HT Receptor
Adrenergic Receptor
|
Cardiovascular Disease
|
|
AL-34662 is a selective 5-HT2A receptoragonist (IC50: 0.77 nM and 1.5 nM for rat and human 5-HT2 receptor). AL-34662 is also a weak α-1D adrenergic agonist activity (EC50:0.4 μM). AL-34662 is an ocular hypotensive agent .
|
-
- HY-10711A
-
|
(R)-NFPS hydrochloride
|
GlyT
|
Neurological Disease
|
|
ALX-5407 ((R)-NFPS) hydrochloride is a selective and orally active glycine transporter GlyT1 inhibitor with an IC50 value of 3 nM. ALX-5407 hydrochloride can be used the research of N-methyl-D-aspartate-receptor function and schizophrenia .
|
-
- HY-116675
-
|
|
Adenosine Receptor
|
Cardiovascular Disease
|
|
Sulmazole is a cardiotonic agent. Sulmazole has competitive inhibitory for A1 adenosine receptor. Sulmazole can improve cardiac index and reduce pulmonary capillary wedge pressure .
|
-
- HY-134377
-
|
ASP0367; MA-0211
|
PPAR
|
Metabolic Disease
|
|
Bocidelpar is a modulator of peroxisome proliferator-activated receptor delta (PPAR-δ). Bocidelpar improves mitochondrial biogenesis and function in Duchenne Muscular Dystrophy (DMD) muscle cells .
|
-
- HY-167412
-
|
|
Biochemical Assay Reagents
|
Others
|
|
PLLA5000-PEG2000-FOL is a polylactic acid derivative. Polylactic acid derivatives have strong binding affinity to folate receptors and clear biodegradability. PLLA5000-PEG2000-FOL can be used in drug delivery research .
|
-
- HY-108683
-
|
|
Orexin Receptor (OX Receptor)
|
Neurological Disease
|
|
ACT-335827 is a selective, orally active, brain-penetrant orexin type 1 receptor antagonist. ACT-33582 acts on OXR1 and OXR2 with IC50 values of 6 nM and 417 nM, respectively. ACT-33582 can be used in studies related to neurological disorders .
|
-
- HY-B1296S1
-
-
- HY-14903
-
|
TZP-101
|
GHSR
Adrenergic Receptor
|
Metabolic Disease
|
|
Ulimorelin (TZP-101) is a ghrelin receptor (GRLN) agonist with an EC50 of 29 nM and a Ki of 16 nM. Ulimorelin is a prokinetic agent and causes vasorelaxation through competitive antagonist action at α1-adrenoceptors. Ulimorelin stimulates intestinal motility and is used for malnutrition .
|
-
- HY-167415
-
|
|
Biochemical Assay Reagents
|
Others
|
|
PLLA10000-PEG5000-FOL is a polylactic acid derivative. Polylactic acid derivatives have strong binding affinity to folate receptors and clear biodegradability. PLLA10000-PEG5000-FOL can be used in drug delivery research .
|
-
- HY-110157
-
|
|
Estrogen Receptor/ERR
|
Neurological Disease
|
|
AC-186 is a selective non-steroidal estrogen receptor β (ERβ) agonist with EC50s of 6 nM and 5000 nM for ERβ and ERα, respectively. AC-186 shows gender selective neuroprotective effects in a male rat model of Parkinson's disease .
|
-
- HY-167413
-
|
|
Biochemical Assay Reagents
|
Others
|
|
PLLA20000-PEG5000-FOL is a polylactic acid derivative. Polylactic acid derivatives have strong binding affinity to folate receptors and clear biodegradability. PLLA20000-PEG5000-FOL can be used in drug delivery research .
|
-
- HY-167411
-
|
|
Biochemical Assay Reagents
|
Others
|
|
PLLA5000-PEG5000-FOL is a polylactic acid derivative. Polylactic acid derivatives have strong binding affinity to folate receptors and clear biodegradability. PLLA5000-PEG5000-FOL can be used in drug delivery research .
|
-
- HY-B1216R
-
|
|
Sigma Receptor
|
Cardiovascular Disease
Others
Neurological Disease
|
|
Oxeladin (citrate) (Standard) is the analytical standard of Oxeladin (citrate). This product is intended for research and analytical applications. Oxeladin citrate is an orally active and brain-penetrant cough suppressant as well as a selective sigma 1 receptor agonist (Ki = 25 nM). Oxeladin can be used for pulmonary diseases and stroke research .
|
-
- HY-167416
-
|
|
Biochemical Assay Reagents
|
Others
|
|
PLLA10000-PEG2000-FOL is a polylactic acid derivative. Polylactic acid derivatives have strong binding affinity to folate receptors and clear biodegradability. PLLA10000-PEG2000-FOL can be used in drug delivery research .
|
-
- HY-167414
-
|
|
Biochemical Assay Reagents
|
Others
|
|
PLLA20000-PEG2000-FOL is a polylactic acid derivative. Polylactic acid derivatives have strong binding affinity to folate receptors and clear biodegradability. PLLA20000-PEG2000-FOL can be used in drug delivery research .
|
-
- HY-147105
-
|
|
Orphan Receptor
|
Inflammation/Immunology
|
|
LRH-1 modulator-1 (compound 6N) is a potent LRH-1 (liver receptor homolog-1) modulator/agonist. LRH-1 modulator-1 shows anti-inflammatory effects in intestinal organoids. LRH-1 modulator-1 induces anti-inflammatory cytokine IL-10, and reduces inflammatory cytokine IL-1b and TNFa .
|
-
- HY-118301
-
|
|
GABA Receptor
|
Neurological Disease
|
|
ADX71441 is a potent and selective positive allosteric modulator of the GABAB receptor. ADX71441 is bioavailable after oral administration and is brain penetrant. ADX71441 has the potential for research of anxiety, pain and spasticity .
|
-
- HY-P2687
-
|
Urodilatin (human)
|
Natriuretic Peptide Receptor (NPR)
|
Cardiovascular Disease
|
|
Ularitide (Urodilatin), natriuretic peptide, is a vasodilator. Ularitide binds to and activates renal receptors. Ularitide also regulates renal dopamine metabolism Ularitide can be used in the research of heart failure .
|
-
- HY-156190
-
|
|
Orphan Receptor
|
Cancer
|
|
NR2F6 modulator-2 (CIA1) is a potent and selective orphan nuclear receptor COUP-TFII (NR2F2) inhibitor. NR2F6 modulator-2 substantially inhibits COUP-TFII–driven NGFIA reporter expression. NR2F6 modulator-2 directly binds to the COUP-TFII ligand-binding domain and disrupts COUP-TFII interaction with transcription regulators, including FOXA1, thus repressing COUP-TFII activity on target gene regulation .
|
-
- HY-19884B
-
|
RM-131 TFA; BIM-28131 TFA
|
GHSR
|
Metabolic Disease
|
|
Relamorelin (RM-131) TFA, a pentapeptide ghrelin analog, is a selective ghrelin/growth hormone secretagogue receptor (GHSR) agonist with a Ki of 0.42 nM for GHS-1a receptor. Relamorelin TFA is centrally penetrant. Relamorelin TFA increases growth hormone levels and accelerates gastric emptying. Relamorelin TFA has the potential for cachexia, gastroparesis, and gastric/intestinal dysmobility disorders research .
|
-
- HY-14915A
-
|
MN-221; KUR-1246
|
Adrenergic Receptor
|
Inflammation/Immunology
|
|
Bedoradrine (MN-221) sulfate is a highly selective β2-adrenergic receptor agonist. Bedoradrine sulfate can effectively relieve airway spasm in asthma patients, dilate airway smooth muscle cells, reduce airway inflammation, and thus improve respiratory function. Bedoradrine sulfate can be used in research on asthma treatment .
|
-
- HY-11051
-
|
|
Opioid Receptor
|
Inflammation/Immunology
|
|
JNJ-20788560 is a selective and orally active delta opioid receptor agonist with an affinity of 2.0 nM for DOR (rat brain cortex binding assay). JNJ-20788560 also is a potent and efficacious antihyperalgesic agent that does not produce respiratory depression, pharmacologic tolerance, or physical dependence. JNJ-20788560 can be used for the research of the relief of inflammatory hyperalgesia .
|
-
- HY-W019787
-
|
|
Opioid Receptor
CXCR
|
Neurological Disease
|
|
BAM-12P, an endogenous opioid peptide, is a novel pro-Met-enkephalin. BAM-12P can activate human κ-opioid receptor (hKOR) with an EC50 of 101 nM and a pEC50 of 6.99. BAM-12P is a ligand for CXCR7 with an EC50 of 175 nM .
|
-
- HY-107707
-
|
|
iGluR
|
Neurological Disease
|
|
TCS 46b (Compound 46b) is a potent, selective and orally active NMDA NR1A/2B receptor antagonist with an IC50 of 5.3 nM . TCS 46b is a click chemistry reagent, it contains an Alkyne group and can undergo copper-catalyzed azide-alkyne cycloaddition (CuAAc) with molecules containing Azide groups.
|
-
- HY-118901
-
|
Ensidon; G-33040
|
Sigma Receptor
|
Neurological Disease
|
|
Opipramol (Ensidon) is an atypical tricyclic antidepressant (TCA). Opipramol acts primarily as a sigma (σ) receptor agonist and can potently interact with sigma recognition sites with a Ki value of 50 nM. Opipramol can be used for the research of generalized anxiety disorder (GAD) .
|
-
- HY-P1338
-
|
|
Opioid Receptor
|
Neurological Disease
|
|
PL-017 is a potent and selective μ opioid receptor agonist with an IC50 of 5.5 nM for 125I-FK 33,824 binding to μ site. PL-017 produces long-lasting, reversible analgesia in rats .
|
-
- HY-105120A
-
|
GR 32191 hydrochloride
|
Prostaglandin Receptor
|
Others
|
|
Vapiprost hydrochloride (GR 32191 hydrochloride) is a thromboxane A2 receptor antagonist. Vapiprost hydrochloride (GR 32191 hydrochloride) inhibits the aggregation and ATP release stimulated with U-46619, collagen or arachidonic acid (AA) at an IC50 of less than 2.1×10 -8 M .
|
-
- HY-118901A
-
|
Ensidon dihydrochloride; G-33040 dihydrochloride
|
Sigma Receptor
|
Neurological Disease
|
|
Opipramol (Ensidon) is an atypical tricyclic antidepressant (TCA). Opipramol acts primarily as a sigma (σ) receptor agonist and can potently interact with sigma recognition sites with a Ki value of 50 nM. Opipramol can be used for the research of generalized anxiety disorder (GAD) .
|
-
- HY-112746
-
|
DPC974; GW5638
|
Estrogen Receptor/ERR
|
Cancer
|
|
Etacstil (GW5638) is a estrogen receptor antagonist that displays minimal uterotropic activity in ovariectomized rats and inhibits the agonist activity of Estradiol (HY-B0141), Tamoxifen (HY-13757A) and Raloxifene (HY-13738) in the environment. Etacstil is promising for research of breast cancer and bone protection .
|
-
- HY-124475
-
|
|
CRFR
|
Neurological Disease
|
|
Antalarmin is a selective nonpeptide corticotropin-releasing factor receptor 1 (CRHR1) antagonist with a Ki of 2.7 nM. Antalarmin can pass through the blood–brain barrier .
|
-
- HY-N10756
-
Hyp9
2 Publications Verification
|
TRP Channel
|
Neurological Disease
|
|
Hyp9 is a transient receptor potential canonical 6 (TRPC6)-specific agonist. Hyp9 can be used for the research of spinal cord injury (SCI) .
|
-
- HY-32067
-
|
Quinuclidin-3-yl acetate
|
mAChR
|
Cardiovascular Disease
Neurological Disease
|
|
Aceclidine (Quinuclidin-3-yl acetate) is a modulator of M3 muscarinic acetylcholine receptor and a M1 receptor agonist (EC50: 40 μM). Aceclidine is a cycloplegic agent, a surfactant, a tonicity adjustor and optionally a viscosity enhancer and an antioxidant. Aceclidine has the potential for the research of disorders such as refractive errors of the eye, xerostomia, Sjogren's syndrome, glaucoma, conjunctivitis, lacrimal gland disease, and esotropia .
|
-
- HY-32067A
-
|
Quinuclidin-3-yl acetate hydrochloride
|
mAChR
|
Neurological Disease
|
|
Aceclidine (Quinuclidin-3-yl acetate) hydrochloride is a modulator of M3 muscarinic acetylcholine receptor and a M1 receptor agonist (EC50: 40 μM). Aceclidine hydrochloride is a cycloplegic agent, a surfactant, a tonicity adjustor and optionally a viscosity enhancer and an antioxidant. Aceclidine hydrochloride has the potential for the research of disorders such as refractive errors of the eye, xerostomia, Sjogren's syndrome, glaucoma, conjunctivitis, lacrimal gland disease, and esotropia .
|
-
- HY-W062702
-
|
|
nAChR
|
Neurological Disease
|
|
BMS-933043 is a potent and selective α7 nACh receptor partial agonist. BMS-933043 attenuates the cognitive impairment in mice and can be utilized in research related to cognitive dysfunction in schizophrenia .
|
-
- HY-100961
-
|
1,3-Dipropyl-8-phenylxanthine
|
Adenosine Receptor
|
Inflammation/Immunology
|
|
NPC 200 is a potent and selective antagonist of Adenosine A1 Receptor. NPC 200 reverses NECA-induced left and right atrial depression with EC50s of 1.08 and 2.03 μM .
|
-
- HY-119806
-
|
|
5-HT Receptor
|
Neurological Disease
|
|
TMPPAA is an allosteric agonist and positive allosteric modulator of the 5-HT3 receptor. TMPPAA enhances 5-HT-mediated 5-HT3AR signaling .
|
-
- HY-12355A
-
|
BAF-312 hemifumarate
|
LPL Receptor
|
Neurological Disease
Inflammation/Immunology
|
|
Siponimod (BAF-312) hemifumarate is a potent and selective sphingosine-1-phosphate (S1P) receptor modulator. Siponimod hemifumarate is selective for S1P1 and S1P5 receptors over S1P2, S1P3, and S1P4 (EC50s of 0.39, 0.98, >10000, >1000, and 750 nM, respectively). Siponimod hemifumarate can be used for multiple sclerosis (MS) research .
|
-
- HY-103563
-
|
|
mGluR
|
Neurological Disease
|
|
3-MATIDA is a metabolic glutamate 1 (mGlu1) receptor antagonist. 3-MATIDA alleviates neuronal death in cerebral ischemia models. 3-MATIDA can be used in the study of neuronal injury and epileptiform activity after ischemia .
|
-
- HY-A0030
-
|
|
mAChR
|
Neurological Disease
Metabolic Disease
Cancer
|
|
Fesoterodine Fumarate is an orally active, nonsubtype selective, competitive muscarinic receptor (mAChR) antagonist with pKi values of 8.0, 7.7, 7.4, 7.3, 7.5 for M1, M2, M3, M4, M5 receptors, respectively. Fesoterodine Fumarate is used for the overactive bladder (OAB) .
|
-
- HY-70053
-
|
|
mAChR
|
Neurological Disease
Metabolic Disease
|
|
Fesoterodine is an orally active, nonsubtype selective, competitive muscarinic receptor (mAChR) antagonist with pKi values of 8.0, 7.7, 7.4, 7.3, 7.5 for M1, M2, M3, M4, M5 receptors, respectively. Fesoterodine is used for the overactive bladder (OAB) .
|
-
- HY-W007355R
-
|
|
Aryl Hydrocarbon Receptor
p38 MAPK
Endogenous Metabolite
Apoptosis
|
Others
|
|
Skatole (Standard) is the analytical standard of Skatole. This product is intended for research and analytical applications. Skatole (3-methylindole) is a heterocyclic compound naturally found in the feces of vertebrates and can be found in certain plants. Skatole can be produced by intestinal bacteria, inducing apoptosis of intestinal epithelial cells through activating aryl hydrocarbon receptors (AhR) and p38. Skatole has been used in specific products of the perfume industry or as a flavor additive in ice cream .
|
-
- HY-168869
-
|
|
PROTACs
Estrogen Receptor/ERR
|
Cancer
|
|
Tamoxifen-PEG-Clozapine is an estrogen receptor α (ERα) PROTAC degrader. Tamoxifen-PEG-Clozapine degrades ERα via a ubiquitin-proteasome system that uses the ubiquitin protein ligase E3 component N-recognin 5. Tamoxifen-PEG-Clozapine can be used for the research of cancer . (Pink: ERα inhibitor (HY-W271653); Black: linker (HY-168870); Blue: CRBN Ligand (HY-G0021))
|
-
- HY-135881
-
|
|
TRP Channel
Endogenous Metabolite
|
Neurological Disease
|
|
OMDM-5 is a selective inhibitor of anandamide cellular uptake (ACU), with a Ki of 4.8 μM. OMDM-5 is also a potent vanilloid receptor type 1 (VR1, TRPV1) agonist, with an EC50 of 75 nM, and shows weakly active as cannabinoid receptor type 1 (CB1) ligand (Ki=4.9 μM) .
|
-
- HY-N1919
-
|
Raubasine
|
Adrenergic Receptor
Cholinesterase (ChE)
|
Neurological Disease
Endocrinology
|
|
Ajmalicine (Raubasine) is a potent adrenolytic agent which preferentially blocks α1-adrenoceptor. Ajmalicine is an reversible but non-competitive nicotine receptor full inhibitor, with an IC50 of 72.3 μM. Ajmalicine also can be used as anti-hypertensive, and serpentine, with sedative activity .
|
-
- HY-N1919A
-
|
Raubasine hydrochloride
|
Adrenergic Receptor
Cholinesterase (ChE)
|
Neurological Disease
Endocrinology
|
|
Ajmalicine (Raubasine) hydrochloride is a potent adrenolytic agent which preferentially blocks α1-adrenoceptor. Ajmalicine hydrochloride is an reversible but non-competitive nicotine receptor full inhibitor, with an IC50 of 72.3 μM. Ajmalicine hydrochloride also can be used as anti-hypertensive, and serpentine, with sedative activity .
|
-
- HY-P1108
-
|
|
CFTR
|
Others
|
|
Astressin 2B is a potent and selective corticotropin-releasing factor receptor 2 (CRF2) antagonist, with the IC50 values of 1.3 nM and > 500 nM for CRF2 and CRF1, respectively. Astressin 2B antagonizes CRF2-mediated inhibition of gastric emptying .
|
-
- HY-123801
-
|
GL-II-93
|
GABA Receptor
|
Others
|
|
MIDD0301 (GL-II-93) is an orally effective, anti-asthmatic positive allosteric modulator of GABAA receptor. MIDD0301 had no significant adverse immune reactions at repeated doses and was better than Prednisone (HY-B0214). MIDD0301 relaxes histamine contractions in guinea pig and human tracheal smooth muscle for the study of bronchial systolic diseases .
|
-
- HY-105670A
-
|
|
nAChR
|
Neurological Disease
|
|
PHA-543613 hydrochloride is an oral or active α7 nAChR agonist with brain permeability, For α3β4, α1β1γδ, α4β2 and 5-HT3 receptors selective. PHA-543613 hydrochloride affects sensory gating and memory in an in vivo model of schizophrenia .
|
-
- HY-135041
-
|
SB-559448 choline
|
Thrombopoietin Receptor
|
Others
|
|
Totrombopag (SB-559448) choline is an orally effective thrombopoietin receptor (TpoR) agonist. By activating TpoR, Totrombopag choline initiates an intracellular signaling cascade mediated by JAK2 kinase and the transcription factor Stat5, a signaling process that is the primary mechanism regulating megakaryocyte growth and differentiation into platelets. Totrombopag choline can be used to study platelet production and megakaryocyte biology .
|
-
- HY-162897
-
|
|
mAChR
|
Cardiovascular Disease
|
|
BAY-2413555 is an orally active muscarinic acetylcholine receptor M2 modulator that protects the heart and improve cardiac function. BAY-2413555 is promising for research of heart failure .
|
-
- HY-105791
-
|
|
GABA Receptor
|
Inflammation/Immunology
|
|
Sulazepam, a benzodiazepine, is a selective ovarian cancer G protein-coupled receptor (OGR1) agonist. Sulazepam has anticonvulsive action and has the potential for airway hyperresponsiveness (AHR) research .
|
-
- HY-107481
-
|
NS 105
|
mGluR
|
Neurological Disease
|
|
Fasoracetam (NS 105) is the activator of metabotropic glutamate receptor (mGluR). Fasoracetam (NS 105) has the potential for the research of attention-deficit hyperactivity disorder (ADHD) and Alzheimer's disease (AD) .
|
-
- HY-P10032
-
-
- HY-111348A
-
|
|
Integrin
|
Cardiovascular Disease
|
|
Lamifiban TFA is a nonpeptide glycoprotein IIb/IIIa receptor and platelet aggregation antagonist. Lamifiban TFA in combination with thrombolytic therapy effectively restores coronary arterial patency. Lamifiban TFA is promising for research of acute coronary syndromes .
|
-
- HY-116144
-
|
Lcaridin
|
Parasite
Bacterial
Fungal
|
Infection
|
|
Picaridin (Lcaridin) is a broad spectrum arthropod repellent. Picaridin interacts with mosquito and tick olfactory receptor proteins. Picaridin repels Aedes aegypti. Picaridin exhibits considerable antibacterial, anticandidal and antifungal properties .
|
-
- HY-122066
-
|
|
Integrin
|
Infection
|
|
NSC47924 is a laminin receptor (LR) inhibitor. NSC47924 affects 37/67 kDa LR cell surface localization and interaction with the cellular prion protein. NSC47924 can be used for testing prion diseases .
|
-
- HY-B1481A
-
|
Isoetarine
|
Adrenergic Receptor
|
Cardiovascular Disease
Inflammation/Immunology
|
|
Isoetharine (Isoetarine) is an orally active selective agonist of β-adrenergic receptors. Isoetharine is a catechol-like agent and catechol O-methyltransferase (COMT) mediates its methylation. Isoetharine can promote the production of cAMP which stimulates the relaxation of smooth muscle cells and can be used as an emphysema, bronchitis and bronchodilator .
|
-
- HY-B1481
-
|
Isoetarine mesylate
|
Adrenergic Receptor
|
Cardiovascular Disease
Inflammation/Immunology
|
|
Isoetharine (Isoetarine) mesylate is an orally active selective agonist of β-adrenergic receptors. Isoetharine mesylate is a catechol-like agent and catechol O-methyltransferase (COMT) mediates its methylation. Isoetharine mesylate can promote the production of cAMP which stimulates the relaxation of smooth muscle cells and can be used as an emphysema, bronchitis and bronchodilator .
|
-
- HY-W014728
-
|
|
Dopamine Receptor
|
Cardiovascular Disease
Neurological Disease
|
|
N-Methyldopamine hydrochloride is a precursor of adrenaline in the adrenal medulla. N-Methyldopamine hydrochloride is a modification of the dopamine (DA), and retains agonist activity at the DA1 receptor. N-Methyldopamine hydrochloride remains capable of universal surface coating and secondary reactions using the surface catechols. N-Methyldopamine hydrochloride can be used for heart failure research .
|
-
- HY-P1338A
-
|
|
Opioid Receptor
|
Neurological Disease
|
|
PL-017 TFA is a potent and selective μ opioid receptor agonist with an IC50 of 5.5 nM for 125I-FK 33,824 binding to μ site. PL-017 TFA produces long-lasting, reversible analgesia in rats .
|
-
- HY-105182A
-
|
LY 246708 tartrate
|
mAChR
|
Neurological Disease
|
|
Xanomeline (LY 246708) is the potent agonist of muscarinic M1/M4 receptor with antipsychotic-like activity. Xanomeline (LY 246708) increases neuronal excitability. Xanomeline (LY 246708) can be used for the research of schizophrenia .
|
-
- HY-P4146
-
|
BI 456906
|
GLP Receptor
GCGR
|
Metabolic Disease
|
|
Survodutide (BI 456906) is a potent, selective glucagon receptor/GLP-1 receptor (GCGR/GLP-1R) dual agonist with EC50s of 0.52 nM and 0.33 nM in CHO-K1 cells, respectively. Survodutide, a 29-amino-acid peptide, is a potent acylated peptide containing a C18 fatty acid. Survodutide has robust anti-obesity efficacy achieved by increasing energy expenditure and decreasing food intake .
|
-
- HY-153342
-
|
ARV-766
|
PROTACs
Androgen Receptor
|
Cancer
|
|
Luxdegalutamide (ARV-766) is an orally active protein hydrolysis targeted chimeric (PROTAC) targeting androgen receptor (AR), which can degrade AR resistance related mutants, including T878/H875/L702 mutants. Luxdegalutamide has anti-tumor activity and can be used in the study of castration resistant prostate cancer .
|
-
- HY-14648
-
-
- HY-14648A
-
-
- HY-P1108A
-
|
|
CFTR
|
Others
|
|
Astressin 2B TFA is a potent and selective corticotropin-releasing factor receptor 2 (CRF2) antagonist, with the IC50 values of 1.3 nM and > 500 nM for CRF2 and CRF1, respectively. Astressin 2B TFA antagonizes CRF2-mediated inhibition of gastric emptying .
|
-
- HY-108847
-
|
|
TNF Receptor
Bacterial
|
Inflammation/Immunology
Cancer
|
|
Etanercept, a dimeric fusion protein that binds TNF, acts as a TNF inhibitor. Etanercept competitively inhibits the binding of both TNF-α and TNF-β to cell surface TNF receptors, rendering TNF biologically inactive. Etanercept shows efficacy against rheumatoid arthritis, juvenile idiopathic arthritis, and plaque psoriasis .
|
-
- HY-12598
-
|
|
mGluR
|
Neurological Disease
|
|
(S)-3,5-DHPG is a weak, but selective group I metabotropic glutamate receptors (mGluRs) agonist with Ki values of 0.9 μM and 3.9 μM for mGluR1a and mGluR5a, respectively . (S)-3,5-DHPG exhibits anxiolytic activity in rats subjected to hypoxia .
|
-
- HY-B1487R
-
|
|
iGluR
mAChR
|
Neurological Disease
|
|
Procyclidine (hydrochloride) (Standard) is the analytical standard of Procyclidine (hydrochloride). This product is intended for research and analytical applications. Procyclidine (Tricyclamol, (±)-Procyclidine) hydrochloride , an anticholinergic agent, is a muscarinic receptor antagonist that also has the properties of an N-methyl-D-aspartate (NMDA) antagonist. Procyclidine hydrochloride can be used in studies of Parkinson's disease and related psychiatric disorders such as Soman-induced epilepsy .
|
-
- HY-107320
-
|
|
Prostaglandin Receptor
COX
NO Synthase
|
Inflammation/Immunology
|
|
Amtolmetin guacil is an effective nonsteroidal anti-Inflammatory agent with pain-relieving effects. Amtolmetin guacil inhibits prostaglandin synthesis and cyclooxygenase (COX). Amtolmetin guacil can stimulate capsaicin receptors present on the gastrointestinal wall and also releases gastroprotective nitric oxide (NO). Amtolmetin guacil can be used to research knee osteoarthritis .
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-
- HY-145308
-
-
- HY-136181
-
|
|
Orexin Receptor (OX Receptor)
|
Neurological Disease
|
|
YNT-185 dihydrochloride is a nonpeptide, selective orexin type-2 receptor (OX2R) agonist, with EC50s of 0.028 and 2.75 μM for OX2R and OX1R, respectively. YNT-185 dihydrochloride ameliorates narcolepsy-cataplexy symptoms in mouse models .
|
-
- HY-P10501
-
|
|
Antifolate
|
Cancer
|
|
FRα-targeting peptide C7 is a selective peptide ligand for folate receptor α (FRα) that has specific binding to FRα expressing cells and in vivo tumor targeting ability. FRα-targeting peptide C7 can be used in the research of tumor diagnosis and treatment .
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-
- HY-B0661R
-
|
|
Adrenergic Receptor
Endogenous Metabolite
|
Neurological Disease
Endocrinology
Cancer
|
|
Tamsulosin (Standard) is the analytical standard of Tamsulosin. This product is intended for research and analytical applications. Tamsulosin ((R)-(-)-YM12617 free base) is an inhibitor of α1-adrenergic receptor. Tamsulosin is used for the research of prostatic hyperplasia. Tamsulosin attenuates abdominal aortic aneurysm growth in animal models .
|
-
- HY-164506
-
|
|
FAAH
|
Neurological Disease
Cancer
|
|
NRMA-8 is a brain-penetrant small molecule nuclear receptor modulator. NRMA-8 is promising for research of central nervous system disorders, including Alzheimer's disease, Parkinson's disease, demylenation disorders and glioblastomas .
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-
- HY-19589
-
-
- HY-103570
-
|
|
mGluR
|
Neurological Disease
|
|
MCPG is a carboxylic phenyl glycine. MCPG can block metabotropic glutamate receptor (mGluR)(HY-15129) and has antagonistic activity of mGluR subtype. MCPG can be used to study the induction and maintenance of long-term potentiation (LTP) .
|
-
- HY-N2080
-
|
|
GABA Receptor
|
Cancer
|
|
Songorine is a diterpenoid alkaloid isolated from the genus Aconitum. Songorine is a GABAA receptor antagonist in rat brain and has anti cancer, antiarrhythmic and anti-inflammatory activities. Songorine has the potential for the treatment of Epithelial ovarian cancer (EOC) .
|
-
- HY-19374
-
|
|
GCGR
|
Metabolic Disease
|
|
BAY-27-9955 is an orally active non-peptide glucagon receptor antagonist. Bay 27-9955 competitively blocks the interaction of glucagon with the human glucagonreceptor at an IC50 value of 110 nM. BAY-27-9955 can be used for the study of type 2 diabetes .
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-
- HY-117088
-
|
|
Neurokinin Receptor
|
Neurological Disease
|
|
LM11A-31, a non-peptide p75 NTR (neurotrophin receptor p75) modulator, is an orally active and potent proNGF (nerve growth factor) antagonist. LM11A-31 is an amino acid derivative with high blood-brain barrier permeability and blocks p75-mediated cell death. LM11A-31 reverses cholinergic neurite dystrophy in Alzheimer's disease mouse models with mid- to late-stage disease progression .
|
-
- HY-156190A
-
|
|
Orphan Receptor
|
Cancer
|
|
NR2F2-IN-1 (free base) is a potent and selective orphan nuclear receptor COUP-TFII (NR2F2) inhibitor. NR2F2-IN-1 (free base) substantially inhibits COUP-TFII–driven NGFIA reporter expression. NR2F2-IN-1 (free base) directly binds to the COUP-TFII ligand-binding domain and disrupts COUP-TFII interaction with transcription regulators, including FOXA1, thus repressing COUP-TFII activity on target gene regulation .
|
-
- HY-169001
-
|
|
5-HT Receptor
|
Neurological Disease
|
|
5-HT2A/5-HT2C inverse agonist 1 is a potent and dual 5-HT2A and 5-HT2C receptor inverse agonist with a hERG inhibitions, thus avoiding cardiovascular risks. 5-HT2A/5-HT2C inverse agonist 1 shows significant antipsychotic efficacy in the MK-801 (HY-15084B)-induced mouse model. 5-HT2A/5-HT2C inverse agonist 1 is promising for research of psychosis .
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-
- HY-113313
-
|
|
Endogenous Metabolite
|
Cardiovascular Disease
|
|
Aldosterone is the primary mineralocorticoid. Aldosterone is a steroid hormone, and it is synthesized and secreted in response to renin-angiotensin system activation (RAS) or high dietary potassium by the zona glomerulosa (ZG) of the adrenal cortex. Aldosterone activity is dependent by the binding and activation of the cytoplasmic/nuclear mineralocorticoid receptor (MR) at cellular level .
|
-
- HY-W178327
-
|
|
Adenosine Receptor
|
Cancer
|
|
8-Chloro caffeine binds to adenosine receptors (Ki = 30 µM). 8-Chloro caffeine potentiates UV-induced chromosomal aberrations in Cl-I Chinese hamster embryonic lung cells. 8-Chloro caffeine is a derivative of the methylxanthine alkaloid caffeine .
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-
- HY-110237
-
|
|
P2X Receptor
Calcium Channel
|
Cardiovascular Disease
|
|
BX430 is a potent and selective noncompetitive allosteric human P2X4 receptor channels antagonist with an IC50 of 0.54 μM. BX430 has species specificity. BX430 is used for chronic pain and cardiovascular disease.
|
-
- HY-15319
-
|
|
CXCR
|
Inflammation/Immunology
Endocrinology
Cancer
|
|
AMG 487 is an orally active and selective antagonist of CXC chemokine receptor 3 (CXCR3) which inhibits the binding of CXCL10 and CXCL11 to CXCR3 with IC50s of 8.0 and 8.2 nM, respectively .
|
-
- HY-P99332
-
|
Anti-Human CD3E Recombinant Antibody; HuM291
|
Apoptosis
|
Inflammation/Immunology
Cancer
|
|
Visilizumab (Anti-Human CD3E Recombinant Antibody) is a humanized low-Fc receptor binding anti-CD3 monoclonal IgG2 antibody. Visilizumab can be used for ulcerative colitis and Crohn's disease research .
|
-
- HY-70053A
-
|
|
mAChR
|
Neurological Disease
Metabolic Disease
Cancer
|
|
Fesoterodine L-mandelate is an orally active, nonsubtype selective, competitive muscarinic receptor (mAChR) antagonist with pKi values of 8.0, 7.7, 7.4, 7.3, 7.5 for M1, M2, M3, M4, M5 receptors, respectively. Fesoterodine L-mandelate is used for the overactive bladder (OAB) .
|
-
- HY-15997
-
|
(-)-Trans-(1S,2S)-U-50488 hydrochloride
|
Opioid Receptor
|
Infection
Cancer
|
|
(-)-U-50488 hydrochloride ((-)-Trans-(1S,2S)-U-50488 hydrochloride) is a selective kappa-opioid receptor (KOR) agonist (b>Kd=2.2 nM) over μ-opioid receptor (MOR) (b>Kd=430 nM). (-)-U-50488 hydrochloride is a more active enantiomer than (+)?trans-(1R,2R) U-50488 (HY-15997A)?or the (±)?trans-racemic mixture U-50488 (HY-15997B). (-)-U-50488 hydrochloride has a potent and sustained anti-HIV effect in fected blood monocyte-derived macrophages (MDM) .
|
-
- HY-P3632
-
|
DADAD
|
Opioid Receptor
|
Neurological Disease
Metabolic Disease
|
|
[DAla2, DArg6] Dynorphin A, (1-13) (porcine) (DADAD) is an opioid peptide (dynorphinl-13, DYN) derivative found in porcine pituitary extracts. DYN is highly potent at the peripheral opioid receptors GPI and MVD, but is readily and rapidly degraded in vivo. [DAla2, DArg6] Dynorphin A, (1-13) (porcine) has some resistance to enzymatic cleavage and prevents peptide cleavage by enzymes .
|
-
![[DAla2, DArg6] Dynorphin A, (1-13) (porcine)](//file.medchemexpress.com/product_pic/hy-p3632.gif)
- HY-136696
-
|
|
Prostaglandin Receptor
|
Metabolic Disease
|
|
11-Deoxy-16,16-dimethyl-PGE2, a Prostaglandin E2 analog, is a EP2 and EP3 receptors agonist. 11-Deoxy-16,16-dimethyl-PGE2 protects proximal renal tubular epithelial cells from potent nephrotoxicity-induced cell damage by exerting anti-oxidative stress .
|
-
- HY-119442
-
|
|
Leukotriene Receptor
|
Cardiovascular Disease
|
|
Quininib is a cysteinyl leukotriene 1 and 2 receptor antagonist with IC50s of 1.2 and 52 μM for CysLT1R and CysLT2R, respectively. Quininib is a potent inhibitor of developmental angiogenesis in the zebrafish eye. Quininib can be used for the research of ocular neovascular pathologies and may complement current anti-VEGF biological agents .
|
-
- HY-120274
-
-
- HY-P4146A
-
|
BI 456906 TFA
|
GLP Receptor
GCGR
|
Metabolic Disease
|
|
Survodutide (BI 456906) TFA is a potent, selective glucagon receptor/GLP-1 receptor (GCGR/GLP-1R) dual agonist with EC50s of 0.52 nM and 0.33 nM in CHO-K1 cells, respectively. Survodutide TFA, a 29-amino-acid peptide, is a potent acylated peptide containing a C18 fatty acid. Survodutide TFA has robust anti-obesity efficacy achieved by increasing energy expenditure and decreasing food intake .
|
-
- HY-116144R
-
|
|
Parasite
|
Infection
|
|
Picaridin (Standard) is the analytical standard of Picaridin. This product is intended for research and analytical applications. Picaridin (Lcaridin) is a broad spectrum arthropod repellent. The repellent and deterrent activities of Picaridin involve olfactory sensing in mosquitoes, and ticks, via their interactions with odorant receptor proteins .
|
-
- HY-124733A
-
|
|
Oxytocin Receptor
|
Neurological Disease
|
|
LIT-001 is the first nonpeptide oxytocin receptor (OT-R) agonist (EC50=55 nM; Ki=226 nM). LIT-001 improves social interaction in a mouse model of autism .
|
-
- HY-N7491A
-
|
|
Calcium Channel
|
Cancer
|
|
ent-(+)-verticilide is a potent and selective inhibitor of cardiac ryanodine receptor (RyR2) calcium release channels with antiarrhythmic activity. ent-(+)-verticilide inhibits RyR2-mediated diastolic Ca 2+?leak and exhibits higher potency and a distinct mechanism of action compared with theDantrolene and Tetracaine.?ent-(+)-verticilide is a useful tool to investigate the therapeutic potential of targeting RyR2 hyperactivity in heart and brain pathologies .
|
-
- HY-110160
-
|
ABT-089 dihydrochloride
|
nAChR
|
Neurological Disease
|
|
Pozanicline dihydrochloride (ABT-089 dihydrochloride) is an orally bioavailable nicotinic acetylcholine receptor (nAChR) agonist with a Ki of 16.7 nM for binding to [ 3H]cytisine sites . Pozanicline is an α4β2-selective nAChR agonist, which binds to rat brain α4β2 nAChR with a Ki of 17 nM while binding to α7 nAChR is insignificant .
|
-
- HY-16950
-
|
(Z)-4-Hydroxytamoxifen; trans-4-Hydroxytamoxifen; (Z)-Afimoxifene
|
Estrogen Receptor/ERR
|
Cancer
|
|
4-Hydroxytamoxifen ((Z)-4-Hydroxytamoxifen) is an orally active, selective estrogen receptor modulator (SERM). 4-Hydroxytamoxifen ((Z)-4-Hydroxytamoxifen) induces CRISPR/Cas9 systems based on ER mediated nucleus translocation. 4-Hydroxytamoxifen ((Z)-4-Hydroxytamoxifen) is also the active metabolic form of Tamoxifen (HY-13757A) in vivo and can be used to induce gene knockout in transgenic mice expressing CreER .
|
-
- HY-147354
-
|
|
LYTACs
|
Cardiovascular Disease
|
TriGalNAc CBz is a GalNAc derivative and tri-GalNAc is an asialoglycoprotein receptor (ASGPR) ligand. TriGalNAc CBz can be used for mRNA drug delivery as well as lysosomal targeted chimerism (LYTAC) studies .
|
-
- HY-10315A
-
|
|
Integrin
|
Cardiovascular Disease
|
|
Elarofiban diTFA is the salt form of Elarofiban (HY-10315) with two TFA. Elarofiban diTFA is a nonpeptide, orally active antagonist for fibrinogen receptor αIIbβ3 (GPIIb/IIIa), with an IC50 of 0.15 nM. Elarofiban diTFA has the potential for platelet mediated thrombotic disorders research .
|
-
- HY-120081AR
-
|
|
mAChR
|
Neurological Disease
|
|
Metixene (hydrochloride hydrate) (Standard) is the analytical standard of Metixene (hydrochloride hydrate). This product is intended for research and analytical applications. Metixene (Piperidine) hydrochloride hydrate is an anticholinergic and antiparkinsonian agent. Metixene hydrochloride hydrate potently inhibits binding of quinuclidinyl benzilate (QNB) with the muscarinic receptor, IC50 and Ki values of 55 nM and 15 nM, respectively. Metixene hydrochloride hydrate can be used for the research of parkinsonian .
|
-
- HY-113820
-
|
|
PPAR
|
Metabolic Disease
|
|
AZD4619 is an orally active, selective peroxisome proliferator-activated receptor α (PPARα) agonist. AZD4619 increases alanine aminotransferase 1 (ALT1) protein expression in a dose-dependent manner in human, but not in rat primary hepatocytes. AZD4619 is a lipid-lowering drug .
|
-
- HY-N7748A
-
-
- HY-156082
-
|
|
Parasite
Calcium Channel
|
Others
|
|
RyRs activator 3 (compound A4) is an effective insecticide against diamondback moths (M. separata) and diamondback moths (P. xylostella). The LC50 value of RyRs activator 3 against diamondback moth is 3.27 mg/L. RyRs activator 3 can bind to ryanodine receptor, increase cytoplasmic Ca2+ concentration, and produce biological toxicity .
|
-
- HY-B0661
-
|
(R)-(-)-YM12617 free base; LY253351 free base
|
Adrenergic Receptor
Apoptosis
|
Neurological Disease
Endocrinology
Cancer
|
|
Tamsulosin ((R)-(-)-YM12617 free base) is an orally active antagonist of α1-adrenergic receptor. Tamsulosin induces Apoptosis. Tamsulosin is used for the research of prostatic hyperplasia. Tamsulosin attenuates abdominal aortic aneurysm growth and inhibits inflammation in animal models .
|
-
- HY-137602
-
|
Up2U
|
P2Y Receptor
|
Others
|
|
P1,P2-Diuridine-5’-diphosphate (Up2U) is a symmetrical dinucleoside polyphosphate containing two pyrimidine base moieties. P1,P2-Diuridine-5’-diphosphate is also an activator of purinergic P2Y receptor .
|
-
- HY-B0661A
-
|
(R)-(-)-YM12617; LY253351
|
Adrenergic Receptor
Apoptosis
|
Neurological Disease
Endocrinology
Cancer
|
|
Tamsulosin hydrochloride ((R)-(-)-YM12617 free base) is an orally active antagonist of α1-adrenergic receptor. Tamsulosin hydrochloride induces Apoptosis. Tamsulosin hydrochloride is used for the research of prostatic hyperplasia. Tamsulosin hydrochloride attenuates abdominal aortic aneurysm growth and inhibits inflammation in animal models .
|
-
- HY-163945
-
|
|
Thyroid Hormone Receptor
|
Metabolic Disease
|
|
ZTA-261 is a highly selective and low toxic thyroid hormone receptor β subtype (THR-β) agonist (IC50=6.3 nM) that reduces body weight and visceral fat through a liothyronine (HY-A0070A) mediated pathway. ZTA-261 can be used in the study of lipid metabolism and obesity prevalence .
|
-
- HY-138641
-
|
ARV-110
|
PROTACs
Androgen Receptor
|
Cancer
|
|
Bavdegalutamide (ARV-110) is an orally active, specific androgen receptor (AR) PROTAC degrader. Bavdegalutamide promotes ubiquitination and degradation of AR. Bavdegalutamide can be used for the research of prostate cancer (Pink: AR ligand (HY-168299); Blue: E3 ligase ligand (HY-W093272); Black: linker (HY-W091986)) .
|
-
- HY-117223
-
|
|
Potassium Channel
|
Neurological Disease
|
|
GEA 857 is a structural analog of the Serotonin (HY-B1473A) uptake blocker Alaproclate (HY-164011). GEA 857 enhances responses induced by muscarinic receptor agonists by inhibiting certain calcium-dependent potassium channels on membranes, a blockade that can enhance or prolong the muscarinic cholinergic effects. GEA 857 can be used in research on neurodegenerative diseases .
|
-
- HY-117851
-
|
|
CaSR
|
Metabolic Disease
Endocrinology
|
|
AC-265347 is a calcium-sensing receptor (CaSR) agonist and positive allosteric modulator (ago-PAM) with the functional affinity (pKB) of 5.1. AC-265347 can be used for the research of hyperparathyroidism and related diseases .
|
-
- HY-14132
-
|
|
CRFR
|
Neurological Disease
|
|
BMS-665053 is a corticotropin-releasing factor-1 (CRF1) receptor antagonist (IC50 = 1.0 nM). BMS-665053)11 is a potent inhibitor of CRF-stimulated cyclic adenosine monophosphate (cAMP) production in human Y-79 retinoblastoma cells (IC50 = 4.9 nM) .
|
-
- HY-W016868
-
|
|
Hydroxycarboxylic Acid Receptor (HCAR)
|
Metabolic Disease
|
|
3-Chloro-5-hydroxybenzoic acid is a potent, orally active and selective lactate receptor GPR81 agonist, with an EC50 of 16 μM for human GPR81. 3-Chloro-5-hydroxybenzoic acid exhibits favorable in vivo effects on lipolysis in a mouse model of obesity .
|
-
- HY-14407AR
-
|
|
Neurokinin Receptor
|
Neurological Disease
Endocrinology
Cancer
|
|
Fosaprepitant (dimeglumine) (Standard) is the analytical standard of Fosaprepitant (dimeglumine). This product is intended for research and analytical applications. Fosaprepitant dimeglumine (MK-0517) is a proagent of Aprepitant (HY-10052). Fosaprepitant dimeglumine is a neurokinin-1 receptor antagonist, which is development for the prevention of chemotherapy-induced nausea and vomiting (CINV) .
|
-
- HY-132935A
-
|
|
c-Fms
|
Inflammation/Immunology
Cancer
|
|
BPR1R024 mesylate is an orally active and selective colony-stimulating factor-1 receptor (CSF1R) inhibitor.
BPR1R024 mesylate is the equivalent of BPR1R024 (HY-132935). BPR1R024 has potent CSF1R inhibition activity with an IC50 value of 0.53 nM. BPR1R024 can be used for the research of immuno-oncology .
|
-
- HY-122171
-
|
|
Histamine Receptor
|
Neurological Disease
|
|
A-317920 is a selective and potent rat histamine H3 receptor (H3R) antagonist with pKi value of 9.2 and 7.0 for full-length rat and full-length human H3R, respectively. A-317920 exhibits over 130 fold selective affinity for the rat over the human H3R. A-317920 enhances cognition via H3R blockade .
|
-
- HY-141852
-
|
|
Deubiquitinase
|
Inflammation/Immunology
|
|
STAMBP-IN-1 is a small-molecule inhibitor of STAMBP deubiquitinase, and interrupts STAMBP-Ub-NALP7 interaction. STAMBP-IN-1 decreases protein level of its inflammasome substrate NALP7 and suppresses IL-1b release after Toll-like receptor (TLR) agonism. STAMBP-IN-1 inhibits the activity of STAMBP to cleave recombinant di-Ub with an IC50 value of 0.33 mM .
|
-
- HY-112739
-
![[pTyr1146][pTyr1150][pTyr1151]Insulin Receptor (1142-1153)](http://file.medchemexpress.com/product_pic/hy-p1776.gif)
![[D-Trp2,7,9] Substance P](http://file.medchemexpress.com/product_pic/hy-p3802.gif)
![[Orn5]-URP](http://file.medchemexpress.com/product_pic/hy-p1167.gif)
![[Orn5]-URP TFA](http://file.medchemexpress.com/product_pic/hy-p1167a.gif)
![[DPen2, Pen5] Enkephalin](http://file.medchemexpress.com/product_pic/hy-p3546.gif)
![N-Acetyl [Leu28, Leu31] neuropeptide Y (24–36)](http://file.medchemexpress.com/product_pic/hy-p10148.gif)
![Des-Arg9-[Leu8]-Bradykinin acetate](http://file.medchemexpress.com/product_pic/hy-p3209.gif)
![[DAla2] Dynorphin A (1-13), amide (porcine)](http://file.medchemexpress.com/product_pic/hy-p3634.gif)
![[DAla2, DArg6] Dynorphin A, (1-13) (porcine)](http://file.medchemexpress.com/product_pic/hy-p3632.gif)
