Search Result
Results for "
receptor
" in MedChemExpress (MCE) Product Catalog:
6904
Inhibitors & Agonists
53
Biochemical Assay Reagents
608
Isotope-Labeled Compounds
| Cat. No. |
Product Name |
Target |
Research Areas |
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- HY-14234
-
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Glucocorticoid Receptor
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Endocrinology
Metabolic Disease
Inflammation/Immunology
|
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
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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-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-156751
-
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Androgen Receptor
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Cancer
|
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Androgen receptor degrader-3 is an androgen receptor degrader. Androgen receptor degrader-3 blocks the process of androgen receptor transduction and also degrades the receptor itself. Androgen receptor degrader-3 can be used for prostate cancer research.
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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-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-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-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-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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Cancer
Endocrinology
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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
|
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-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-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-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-120273
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- HY-145250
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- HY-145775
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Others
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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-153477
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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-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-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-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-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-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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Apelin Receptor (APJ)
Arrestin
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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-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-138761
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Prostaglandin Receptor
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Cancer
Inflammation/Immunology
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EP4 receptor antagonist 3 is a potent EP4 receptor antagonist, example 3,extracted from patent WO2010019796 A1. EP4 receptor antagonist 3 can be used for the reseacrh of EP4 receptor-mediated diseases, such as acute and chronic pain, osteoarthritis, rheumatoid arthritis and cancer.
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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-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-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-144607
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Opioid Receptor
|
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-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-153458
-
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Orexin Receptor (OX Receptor)
|
Metabolic Disease
Neurological Disease
|
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Orexin receptor modulator-1 is an orexin receptor modulator. Orexin receptor modulator-1 can be used for the research of substance addiction, panic disorder, anxiety, post-traumatic stress disorder, pain, depression, seasonal affective disorder, an eating disorder, or hypertension.
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- HY-P0078
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TRAP-6
2 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-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-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 TARPγ2 dependent AMPA receptor. pIC50 = -lgIC50.
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- HY-P0283
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- HY-W584986
-
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Androgen Receptor
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Cancer
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Androgen receptor degrader-2 (compound 9) is a potent androgen receptor degrader. Androgen receptor degrader-2 can be used in research of cancer.
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- HY-W248665A
-
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Androgen Receptor
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Cancer
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Androgen receptor degrader-1 (compound 18) is a potent androgen receptor degrader. Androgen receptor degrader-1 can be used in research of cancer.
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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
|
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-139627
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- HY-W681071
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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-P0317
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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-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-W063197
-
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Adenosine Receptor
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Cancer
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Adenosine receptor antagonist 4 (compound 2) is an adenosine A1 receptor antagonist with a Ki of 101 nM for human A1 receptor.
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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-75502
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N-0923; (-)-N 0437
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Dopamine Receptor
Adrenergic Receptor
5-HT Receptor
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Neurological Disease
Endocrinology
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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.
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- HY-112689
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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-143314
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Protease Activated Receptor (PAR)
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Cardiovascular Disease
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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.
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- HY-155478
-
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Androgen Receptor
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Cancer
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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-P1840
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Neuropeptide Y Receptor
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Neurological Disease
Endocrinology
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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.
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- HY-U00339
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-
- HY-118259
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- HY-153276
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Androgen Receptor
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Cancer
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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).
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- HY-145364
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- HY-110047
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- HY-147736
-
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GABA Receptor
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Neurological Disease
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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.
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- HY-147735
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GABA Receptor
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Neurological Disease
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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.
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- HY-128781
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GCGR
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Metabolic Disease
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Glucagon receptor antagonists-5 (compound 13K) is a potent and orally bioavailable indazole-based glucagon receptor antagonist (Ki=32 nM). Glucagon receptor antagonists-5 has potential for the treatment of type 2 diabetes mellitus (T2DM).
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- HY-156522
-
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CFTR
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Endocrinology
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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).
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- HY-153478
-
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Estrogen Receptor/ERR
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Cancer
|
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Estrogen receptor modulator 7 is a potent estrogen receptor modulator. Estrogen receptor modulator 7 can be used in research of cancer.
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-
- HY-131974
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-
- HY-112189
-
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IFNAR
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Inflammation/Immunology
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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.
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- HY-142941
-
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Glucocorticoid Receptor
MMP
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Inflammation/Immunology
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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.
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- HY-121488
-
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Interleukin Related
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Neurological Disease
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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.
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-
- HY-145684
-
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Prostaglandin Receptor
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Inflammation/Immunology
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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.
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- HY-142942
-
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Glucocorticoid Receptor
MMP
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Inflammation/Immunology
|
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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.
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- HY-143390
-
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iGluR
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Neurological Disease
|
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NMDA receptor modulator 2 (Compound 1) is a potent NMDA receptor modulator. NMDA receptor modulator 2 can be used for neurological disorder research.
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- HY-143396
-
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iGluR
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Neurological Disease
|
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NMDA receptor modulator 5 (Compound 195) is a potent NMDA receptor modulator. NMDA receptor modulator 5 can be used for neurological disorder research.
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- HY-143393
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iGluR
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Neurological Disease
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NMDA receptor modulator 4 (Compound 169) is a potent NMDA receptor modulator. NMDA receptor modulator 4 can be used for neurological disorder research.
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- HY-143391
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iGluR
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Neurological Disease
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NMDA receptor modulator 3 (Compound 99) is a potent NMDA receptor modulator. NMDA receptor modulator 3 can be used for neurological disorder research.
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- HY-143397
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iGluR
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Neurological Disease
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NMDA receptor modulator 6 (Compound 183) is a potent NMDA receptor modulator. NMDA receptor modulator 6 can be used for neurological disorder research.
|
-
- 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-150601
-
-
- 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-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-18076
-
-
- HY-P1840A
-
|
|
Neuropeptide Y Receptor
|
Endocrinology
Neurological Disease
|
|
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-156541
-
-
- HY-156536
-
-
- HY-156538
-
-
- HY-156537
-
-
- HY-136922
-
-
- HY-150205
-
|
|
Others
|
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-156543
-
-
- HY-156539
-
-
- HY-156540
-
-
- HY-156542
-
-
- 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-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-100113
-
-
- 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-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-133123
-
|
|
Prostaglandin Receptor
|
Cancer
Inflammation/Immunology
|
|
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-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 can induce apoptosis. Estrogen receptor modulator 10 can block cells at the G1/G0 phase. Estrogen receptor modulator 10 can be used in cancer studies.
|
-
- HY-139876
-
-
- HY-133486
-
-
- 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-P1868A
-
|
|
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-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-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-129636
-
|
|
GABA Receptor
|
Neurological Disease
|
|
(E)-GABAB receptor antagonist 1 is a trans-GABAB receptor antagonist 1. GABAB receptor antagonist 1 (compound 14) is a selective and negative allosteric modulator of GABAB (γ-Aminobutyric acid) receptors. (E)-GABAB receptor antagonist 1 decreases GABA-induced IP3 (inositol trisphosphate) production with IC50 of 37.9 μM.
|
-
- 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-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-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-110161
-
|
|
Somatostatin Receptor
|
Endocrinology
Cardiovascular Disease
|
|
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-139709
-
-
- HY-139710
-
-
- HY-10658
-
-
- 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-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-U00429
-
|
|
Others
|
Neurological Disease
|
|
NOT Receptor Modulator 1 is a nuclear receptor NOT modulator extracted from patent WO 2008034974 A1, Example 39 in table1.
|
-
- HY-U00387
-
-
- 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-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-129636A
-
|
|
GABA Receptor
|
Neurological Disease
|
|
GABAB receptor antagonist 1 (compound 14) is a selective and negative allosteric modulator of GABAB (γ-Aminobutyric acid) receptors. (E)-GABAB receptor antagonist 1 decreases GABA-induced IP3 (inositol trisphosphate) production with IC50 of 37.9 μM.
|
-
- 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-U00420
-
-
- HY-145611
-
-
- 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-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
-
|
|
Others
|
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-19733
-
|
ITI-007 tosylate
|
5-HT Receptor
Dopamine Receptor
|
Neurological Disease
|
|
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-17637
-
|
ITI-007
|
Dopamine Receptor
5-HT Receptor
|
Neurological Disease
|
|
Lumateperone (ITI-007) 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 has anticancer activity and can also be used in studies of psychiatric disorders such as schizophrenia.
|
-
- HY-137093
-
-
- HY-P1308
-
-
- HY-145610
-
-
- HY-121867
-
-
- HY-111194
-
|
|
Others
|
Others
|
|
Ro 22-8515 is a ligand of Benzodiazepine receptor.
|
-
- HY-147907
-
|
|
Adenosine Receptor
|
Cancer
Inflammation/Immunology
Neurological Disease
|
|
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-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-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-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-145553
-
-
- HY-100966
-
-
- 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-145106
-
-
- 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-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-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-114025
-
-
- HY-156830
-
|
|
Others
|
Metabolic Disease
|
|
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 plays important roles in hypoglycemic and weight loss.
|
-
- 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-129946
-
-
- HY-114017
-
-
- HY-148179
-
-
- 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-150068
-
-
- HY-10018
-
-
- 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-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-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-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-154980
-
|
|
Others
|
Neurological Disease
|
|
GPR52 receptor modulator 1 (Procedure 1) is a GPR52 receptor modulator with the potential to study neuropsychiatric diseases.
|
-
- 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-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-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-112679
-
|
|
GCGR
|
Others
|
|
GLP-1 receptor agonist 2 is a glucagon-like peptide-1 receptor (GLP-1R) agonist.
|
-
- 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-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-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-112451
-
-
- HY-112455
-
-
- HY-123829
-
-
- HY-13724
-
-
- 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-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
|
Cancer
Neurological Disease
|
|
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-106199
-
|
|
Adenosine Receptor
|
Inflammation/Immunology
Neurological Disease
|
|
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-155147
-
-
- 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-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).
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-
- 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-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-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-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-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-P1308A
-
-
- HY-148198
-
-
- 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-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-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-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-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-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-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-12709
-
-
- HY-155417
-
|
|
Others
|
Neurological Disease
|
|
GPR34 receptor antagonist 3 (Compound 5e) is a class of GRP34 antagonists, with 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-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-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-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-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-148436
-
-
- 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-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-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-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-U00321
-
-
- 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-W095200
-
-
- 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-144672
-
-
- 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-P1536
-
-
- HY-P3852
-
|
SPR393-407
|
Neurokinin Receptor
|
Inflammation/Immunology
Neurological Disease
|
|
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-P5175
-
|
|
mAChR
|
Neurological Disease
|
|
Muscarinic toxin 7 is a peptide toxin with selective and noncompetitive antagonism at the muscarinic M1 receptor.
|
-
- HY-138695
-
-
- 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-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-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-102024
-
-
- HY-B1510S
-
-
- 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-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-50175A
-
-
- HY-50175
-
-
- HY-143267
-
-
- 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-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-101704
-
-
- 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-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-100920
-
-
- 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-149645
-
|
|
Others
|
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-145370
-
|
|
iGluR
|
Neurological Disease
|
|
GluN2B receptor modulator-1 is a selective GluN2B negative allosteric modulator with an IC50 value of 31 nM.
|
-
- 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-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 inhibits 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 for 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-50713
-
|
|
CaSR
|
Others
|
|
Calcium-Sensing Receptor Antagonists I is a click chemistry reagent, itcontains an Alkyne group and can undergo copper-catalyzed azide-alkyne cycloaddition (CuAAc) with molecules containing Azide groups.
|
-
- HY-144603
-
-
- 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-120633A
-
-
- HY-13715
-
-
- HY-P1818
-
-
- HY-13715A
-
-
- HY-P1266
-
|
|
nAChR
|
Neurological Disease
|
|
α-Conotoxin EI is a selective nicotinic acetylcholine α1β1γδ receptor (nAChR) antagonist (IC50=187 nM) and an α3β4 receptor inhibitor. α-Conotoxin EI can block muscle and ganglionic receptors.
|
-
- HY-111669
-
-
- HY-139436
-
-
- HY-13715B
-
-
- HY-125101A
-
-
- 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 inhibits for 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-155194
-
|
|
Others
|
Inflammation/Immunology
|
|
P2X7 receptor antagonist-4 (Compound 14a) is a P2X7R antagonist. The P2X7 receptor antagonist-4 values of P2X7R IC50 in human and mouse are 64.7 and 10.1 nM, respectively. P2X7 receptor antagonist-4 can inhibit the activation of NLRP3 inflammasome, thereby inhibiting the expression of caspase-1, gasdermin D, IL-1β and IL-18 in the damaged kidney of sepsis mice.
|
-
- HY-13715C
-
-
- HY-112185
-
|
LY3502970; GLP-1 receptor agonist 1
|
GCGR
|
Metabolic Disease
|
|
Orforglipron (LY3502970) (GLP-1 receptor agonist 1) is a GLP-1 receptor agonist extracted from patent WO2018056453A1, Compound 67.
|
-
- HY-152270
-
-
- HY-136969
-
-
- 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-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-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-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-148525
-
|
β2AR/M-receptor agonist-2
|
mAChR
Adrenergic Receptor
|
Inflammation/Immunology
Cardiovascular Disease
|
|
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-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-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-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.
|
-
- 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-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-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-P3450
-
-
- HY-P2355A
-
-
- 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-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-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-P2355
-
-
- 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-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-P1465
-
-
- HY-147279
-
|
|
LDLR
|
Others
|
|
Milpocitide is a low-density lipoprotein receptor (human LDL receptor, LDLR), (293-333)-peptide fragment (EGF-like domain 1).
|
-
- HY-154789
-
-
- 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-119482
-
|
|
Progesterone Receptor
|
Others
|
|
Cymipristone (ZXH-951), a progesterone receptor antagonist, is used potentially for termination of intrauterine pregnancy.
|
-
- HY-100842
-
-
- 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-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-P1465A
-
-
- HY-P1165
-
-
- 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-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-147421
-
-
- HY-109147A
-
-
- HY-N3398
-
-
- HY-111295
-
|
|
Adenosine Receptor
|
Others
|
LAS38096 is a potent, selective, and efficacious A2B Adenosine Receptor antagonist, with a Ki of 17 nM.
|
-
- HY-135436
-
|
|
IGF-1R
|
Cancer
|
|
AG 538 is a potent, competitive inhibitor of IGF-1 receptor kinase, with an IC50 of 400 nM.
|
-
- 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-P5506
-
|
|
Complement System
|
Others
|
|
C5a Receptor agonist, mouse, human is a biological active peptide. (This peptide is derived from the C-terminus of the chemokine, complement fragment 5 anaphylatoxin (C5a). This peptide functions as a C5a receptor agonist. C5a is a plasma protein involved in cellular inflammatory processes by inducing chemotaxis, degranulation of leukocytes, increased vascular permeability, and cytokine production. The cyclohexylalanine at position 5 is crucial to agonist function. Arg at the last position is of the d-isomer.)
|
-
- 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-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-155394
-
|
|
Others
|
Metabolic Disease
|
|
RyRs activator 5 (Compd A-1) is an active ryanodine receptor agonist against Spodoptera frugiperda.
|
-
- 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-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-B0098S
-
-
- 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-103407A
-
|
|
Dopamine Receptor
|
Cancer
Neurological Disease
|
|
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-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-103141
-
|
|
Others
|
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-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-128127
-
|
|
LPL Receptor
|
Others
|
|
NAEPA, a phosphate-mimetic derivative, is a lysophosphatidic acid (LPA) receptor agonist.
|
-
- 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-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-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-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-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-107218
-
|
|
RAR/RXR
VD/VDR
|
Infection
|
|
11-Hydroxysugiol regulates the SUMOylation of intracellular receptors by modulating RARα and vitamin D3 receptor (VDR).
|
-
- 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-W742957
-
|
|
iGluR
|
Neurological Disease
|
|
Pregnanolone sulfate pyridinium is an endogenous neurosteroid that inhibits NMDA receptors and is neuroprotective.
|
-
- HY-19320
-
-
- 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-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-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-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-123744
-
-
- HY-137883
-
|
|
ADC Linker
|
Cancer
|
|
Glucocorticoid receptor agonist-1 phosphate Gly-Glu-Br is an ADC linker 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-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-153958
-
|
|
Others
|
Cancer
|
|
PDS-MMAE (Compound 5’) is a modified MMAE (HY-15162). PDS-MMAE can be used for preparation of neurotensin receptor binding conjugates.
|
-
- 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-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-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-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-135270
-
-
- HY-19401
-
-
- HY-101747A
-
-
- 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/b> with IC50 values range from 5.2 μM to 106 μM. Picrotin can be used for the research of neurotransmission.
|
-
- HY-153345
-
-
- HY-P2000
-
-
- HY-P2572
-
-
- HY-107395
-
-
- 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-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-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-108483
-
|
|
Neurokinin Receptor
|
Inflammation/Immunology
Neurological Disease
|
|
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-107747
-
-
- 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-103246
-
|
|
Androgen Receptor
|
Cancer
|
|
TFM-4AS-1 is a selective androgen receptor modulator (SARM). TFM-4AS-1 is a potent androgen receptor (AR) ligand with an IC50 of 38 nm. TFM-4AS-1 is also a gene-selective agonist.
|
-
- 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-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-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-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.
|
-
- 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-132827
-
-
- HY-A0125
-
-
- HY-107704
-
-
- 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-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-116116
-
|
SIM010603
|
VEGFR
RET
c-Kit
|
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-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-153809
-
-
- HY-107747A
-
-
- HY-78168
-
-
- 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-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-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-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-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-114630
-
-
- HY-P990089
-
-
- HY-B1115
-
-
- HY-P4805
-
-
- 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-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-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
-
-
- 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-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-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-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-B1737
-
-
- 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-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-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-150790
-
-
- HY-148212
-
|
|
GCGR
|
Metabolic Disease
Cardiovascular 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-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-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-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-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-156994
-
|
|
Others
|
Others
|
|
ASGPR ligand-1 is an asialoglycoprotein receptor (ASGPR) ligand compound. ASGPR ligand-1 can be used for kinds of diseases research.
|
-
- 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-103304
-
|
|
Others
|
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-P1167A
-
-
- 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-18200
-
|
E5555; ER-172594-00
|
Protease Activated Receptor (PAR)
|
Cardiovascular Disease
|
|
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-107749
-
-
- HY-112736
-
-
- 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-P3546
-
-
- HY-15706
-
-
- 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-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-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-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-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-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-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-119802
-
-
- HY-103314
-
|
GdCl3
|
CaSR
|
Cardiovascular Disease
|
|
Gadolinium chloride is a specific calcium-sensing receptor (CaSR) agonist. Gadolinium chloride can be used for the research of cardiovascular disease.
|
-
- 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-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-18200B
-
|
E5555 hydrobromide; ER 172594-06
|
Protease Activated Receptor (PAR)
|
Cardiovascular Disease
|
|
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-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-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-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-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-P3891
-
-
- 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-103535
-
-
- 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-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-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-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-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-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-147544
-
-
- HY-147543
-
-
- 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-147545
-
-
- 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-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-B0649
-
-
- HY-122359B
-
|
L-Centchroman 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-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-145128
-
-
- 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-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-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-118497
-
|
|
Endothelin Receptor
|
Metabolic Disease
Cardiovascular 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-117824
-
|
|
Others
|
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-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
-
DAMGO
2 Publications Verification
|
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-121276
-
|
|
Others
|
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-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-155334
-
|
|
Others
|
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-143576
-
-
- 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-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-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-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-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-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-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-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-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-145700
-
-
- HY-131388
-
-
- HY-155316
-
|
|
Others
|
Others
|
|
5-HT6R antagonist 2 (compound 29) is a 5-HT6 receptor antagonist.
|
-
- 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-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-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-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-B1115A
-
-
- 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-42849
-
-
- HY-42849A
-
-
- 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-101367A
-
-
- 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-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-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-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-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-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-109111
-
-
- 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-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-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-128469
-
|
|
GABA Receptor
|
Neurological Disease
|
|
Inaperisone is a centrally acting muscle relaxant. Inaperisone inhibits the micturition reflex by acting indirectly on GABAB receptors in the brainstem.
|
-
- 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-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-P1270
-
|
|
nAChR
|
Neurological Disease
|
|
α-Conotoxin Im-I is a selective α7/α9 nAChR antagonist, blocking α7 nicotinic receptors with the highest apparent affinity, while having an 8-fold lower affinity for homomeric α9 nicotinic receptors. α-Conotoxin Im-I is toxic and induces seizures in rodents. α-Conotoxin Im-I is a tool for studying neuronal nAChR.
|
-
- HY-19365
-
|
|
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-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-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-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-P2034
-
-
- HY-P99052
-
|
|
PD-1/PD-L1
|
Cancer
Inflammation/Immunology
|
|
Tislelizumab, a monoclonal antibody with high binding affinity to the PD-1 receptor, minimizes Fcγ receptor binding on macrophages, thereby abrogating antibody-dependent phagocytosis, a mechanism of T cell clearance and potential resistance to anti-PD-1 research. Tislelizumab can be used for the research of advanced squamous non-small-cell lung cancer.
|
-
- HY-12288
-
|
RPC-1063
|
LPL Receptor
|
Inflammation/Immunology
Neurological Disease
|
|
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
|
Inflammation/Immunology
Neurological Disease
|
|
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-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-115613
-
|
SR1848
|
Others
|
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-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-17497S
-
-
- HY-101106
-
AR7
5 Publications Verification
|
RAR/RXR
|
Cancer
Neurological Disease
|
|
AR7 is an atypical RARA/RARα (retinoic acid receptor, alpha) antagonist. AR7 specifically activates chaperone-mediated-autophagy (CMA) activity without affecting macroautophagy.
|
-
- 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-P0036B
-
|
SMS 201-995 pamoate
|
Somatostatin Receptor
Apoptosis
|
Cancer
Endocrinology
Inflammation/Immunology
Cardiovascular Disease
|
|
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
|
Cancer
Endocrinology
Inflammation/Immunology
Cardiovascular Disease
|
|
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-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-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-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-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-10419A
-
-
- HY-110206
-
|
|
Cannabinoid Receptor
|
Metabolic Disease
|
|
AM6545 is a peripherally active, cannabinoid receptor antagonist with limited brain penetration. AM6545 binds to CB1 and CB2 receptors with Kis of 1.7 nM and 523 nM, respectively. AM6545 is a neutral antagonist. AM6545 can be used for the research of obesity and its complications.
|
-
- 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-111258
-
-
- 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-B2089
-
-
- HY-P2537
-
|
|
Apelin Receptor (APJ)
HIV
|
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-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-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-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-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-119605
-
|
|
Others
|
Neurological Disease
|
|
DAA-1097 is an orally active and selective agonist for the peripheral benzodiazepine receptor (PBR). DAA-1097 has anxiolytic effects.
|
-
- 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-128128
-
|
|
Others
|
Neurological Disease
|
|
ASN04421891 is a potent GPR17 receptor modulator, with an EC50 of 3.67 nM in [35S]GTPγS binding assay. ASN04421891 can be used for neurodegenerative diseases research.
|
-
- HY-108972
-
-
- 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-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-156601
-
|
|
Others
|
Others
|
|
Bexicaserin (Compound 3) is a 5-HT2C receptor agonist with potential for studying obesity and psychiatric-related diseases.
|
-
- HY-122620
-
|
|
Thrombopoietin Receptor
|
Inflammation/Immunology
Cancer
|
|
Hetrombopag is a potent thrombopoietin receptor agonist. Hetrombopag is efficacious and well tolerated with a manageable safety profile. Hetrombopag has the potential for the research of immune thrombocytopenia.
|
-
- HY-150204
-
-
- 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-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-148531
-
|
|
CCR
|
Inflammation/Immunology
|
|
PF-07054894 is a potent CCR6 antagonist. PF-07054894 targets G protein-coupled receptor (GPCR). PF-07054894 can be used in research of inflammatory bowel disease.
|
-
- 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-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, itcontains an Alkyne group and can undergo copper-catalyzed azide-alkyne cycloaddition (CuAAc) with molecules containing Azide groups.
|
-
- 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-17032A
-
|
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-147203
-
|
|
5-HT Receptor
|
Cancer
Endocrinology
Metabolic Disease
Cardiovascular Disease
|
|
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-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-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-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-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-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-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-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-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-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-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-103200
-
-
- HY-100672
-
-
- 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-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-90010
-
|
Kabi-2234; PNU-200583E
|
mAChR
|
Neurological Disease
|
|
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-A0158
-
|
|
Others
|
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-130842
-
|
β-NF-CH2-Br
|
Ligands for E3 Ligase
|
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-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-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-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-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-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-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-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-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-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-134801
-
-
- HY-103221
-
|
|
Aryl Hydrocarbon Receptor
GSK-3
CDK
|
Others
|
|
MeBIO is a potent AhR (aryl hydrocarbon receptor) agonist, with IC50 of 44 μM (GSK-3) and 55 μM (CDK1/cyclin B), respectively. MeBIO is inactive on GSK-3β.
|
-
- 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-123813
-
|
|
Arrestin
|
Cancer
|
|
CCX-777 is a partial agonist of β-arrestin-2 recruitment to ACKR3 (atypical chemokine receptor 3).
|
-
- 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-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-19627A
-
|
S-297995 tosylate
|
Opioid Receptor
|
Metabolic Disease
Neurological 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
|
Metabolic Disease
Neurological 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-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-160001
-
|
|
Others
|
Others
|
|
ZH8659 is a trace amine-associated receptor 1 (TAAR1) –Gq agonist. ZH8659 can be used for the research of schizophrenia.
|
-
- 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-W502657
-
|
|
Others
|
Neurological Disease
|
|
ZH8667 is a trace amine-associated receptor 1 (TAAR1) –Gs agonist. ZH8667 can be used for the research of schizophrenia.
|
-
- HY-P5896
-
-
- 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-136896
-
-
- 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-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-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-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-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-10121
-
-
- 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-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-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-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-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-121392
-
|
|
5-HT Receptor
|
Neurological Disease
Cardiovascular 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-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-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-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-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-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-P1345
-
|
|
Complement System
|
Endocrinology
Neurological Disease
|
|
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-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-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-118743
-
|
|
Prostaglandin Receptor
|
Metabolic Disease
|
|
KMN-80, a derivative of PGE1 (HY-B0131), is a selective and potent agonist of EP4 receptor with an IC50 and a Ki of 3 nM and 2.35 nM, respectively. KMN-80 is against EP3 receptor with an IC50 of 1.4 μM and >10 μM for all other prostanoid receptors. KMN-80 is a click chemistry reagent, itcontains an Alkyne group and can undergo copper-catalyzed azide-alkyne cycloaddition (CuAAc) with molecules containing Azide groups.
|
-
- 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-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-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
-
|
|
Others
|
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-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-147337
-
|
|
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-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-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-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. Antipsychotic agent.
|
-
- 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-P1345A
-
|
|
Complement System
|
Endocrinology
Neurological Disease
|
|
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-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-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-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-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-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-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-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-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-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-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-122495
-
|
rel-LY 141865 dihydrochloride
|
Dopamine Receptor
|
Neurological Disease
|
|
rel-Quinpirole (rel-LY 141865) dihydrochloride, an ergot compound, is a selective dopamine (DA) D2 receptor agonist. rel-Quinpirole dihydrochloride can be used for research on neurological diseases.
|
-
- HY-13222
-
|
|
Opioid Receptor
|
Cancer
Neurological Disease
|
|
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-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-133898
-
|
TAK-925
|
Orexin Receptor (OX Receptor)
|
Others
|
|
Danavorexton (TAK-925) is an orexin receptor agonist with brain permeability. Danavorexton induced a physiological pattern of OX2R activation in vitro to wake up sleepy mice and improve sleepiness symptoms..
|
-
- HY-139970
-
|
|
Androgen Receptor
|
Cancer
Endocrinology
|
|
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-P4032
-
|
|
HCV
|
Inflammation/Immunology
|
|
HCV Peptide (35-44), a HCV core protein at positions 35 to 44, is a HLA-A2-restricted CTL epitope. HCV Peptide (35-44) inhibits NK cell activity via two distinct mechanisms, directly via KIR2DL2/3, and synergistically via the CD94:NKG2A receptor.
|
-
- 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-132811
-
-
- HY-P99104
-
|
COVI-AMG; STI-2020
|
SARS-CoV
|
Infection
|
|
Plutavimab a humanized 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-111269
-
-
- HY-P2703
-
|
|
Neuropeptide Y Receptor
|
Endocrinology
Metabolic Disease
|
|
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-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-138642
-
|
ARV-471
|
Estrogen Receptor/ERR
PROTACs
|
Cancer
|
|
Vepdegestrant (ARV-471) is an oral estrogen receptor PROTAC protein degrader for 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 ~2 nM.
|
-
- 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-103211
-
|
|
Adrenergic Receptor
|
Cancer
Metabolic Disease
Cardiovascular Disease
|
|
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-148118
-
|
|
LYTACs
|
Cancer
|
|
Tri-GalNAc(OAc)3 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-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
|
Cancer
Neurological Disease
|
|
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-17417A
-
|
|
Opioid Receptor
|
Neurological Disease
|
|
Naloxone is an antagonist of Opioid receptor. Naloxone alleviates opioid-overdose-induced respiratory depression. Naloxone may cause pulmonary edema and cardiac arrhythmias.
|
-
- 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-13418A
-
|
Compound C; BML-275
|
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-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-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-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-100672B
-
|
|
Others
|
Metabolic Disease
Cardiovascular Disease
|
|
(2R)-SR59230A is the inactive 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-10933
-
CX516
1 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-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-108662
-
|
2,2'-Pyridylisatogen tosylate
|
P2Y Receptor
|
Inflammation/Immunology
|
|
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-P99171
-
|
|
Interleukin Related
|
Inflammation/Immunology
|
|
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-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
-
|
|
Others
|
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
|
Cancer
Endocrinology
|
|
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-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-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-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-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-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-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-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-P3209
-
-
- HY-149728
-
-
- HY-W420452
-
|
JSTX-3; Jorotoxin 3
|
Others
|
Neurological Disease
|
|
Joro spider toxin 3 is a GABA agonist. Joro spider
toxin 3 blocks the binding of muscle-stimulating diazepam. Joro spider toxin 3
can be used to study the inactivation mechanism of inhibitory GABA receptor
.
|
-
- 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-13418
-
|
Compound C dihydrochloride; BML-275 dihydrochloride
|
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-143878
-
|
|
Others
|
Neurological Disease
|
|
MRGPRX1 agonist 2 (compound 1a) is a potent Mas-related G protein-coupled receptor X1 (MRGPRX1) positive allosteric modulator with an EC50 value of 0.48 μM. MRGPRX1 agonist 2 can be used for researching neuropathic pain.
|
-
- 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-A0261A
-
|
ICI-50123 meglumine
|
Cholecystokinin Receptor
|
Cancer
Endocrinology
|
|
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-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.
|
-
- HY-101119
-
|
|
Estrogen Receptor/ERR
|
Cancer
|
|
GLL398, an orally active selective estrogen receptor degrader (SERD), competitively binds to the estrogen receptor with an IC50 value of 1.14 nM. GLL398 exhibits a strong dose-dependent binding profile for the ER with a Y537S point mutation (IC50= 29.5 nM). GLL398 blocks tumor growth in xenograft breast cancer models.
|
-
- 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-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-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-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 was developed for the treatment of Parkinson's disease and restless leg syndrome.
|
-
- 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-135147
-
|
|
Dopamine Receptor
|
Cancer
Neurological Disease
|
|
ONC206 is an analogue of TRAIL inducer ONC201. ONC206 is a selective antagonist of the D2-like dopamine receptors (DRD2/3/4) at nanomolar concentrations. ONC206 has broad-spectrum anti-tumor activity.
|
-
- HY-156831
-
-
- 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-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-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-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-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-P3517
-
|
β-EP (6-31), human
|
Opioid Receptor
|
Endocrinology
Neurological Disease
|
|
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-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-N2466
-
|
MT-I; [Nle4,D-Phe7]-α-MSH
|
Melanocortin Receptor
|
Cancer
|
|
Melanotan I is a potent non-selective melanocortin receptor (MCR) agonist. Melanotan I is a synthetic analogue of α-melanocyte stimulating hormone (α-MSH) that stimulates melanogenesis. Melanotan I can induce skin tanning by mimicking the actions of a-MSH on the melanocortin type 1 receptors (MC1R) of melanocytes. Melanotan I can be used for sunlight-induced skin cancers research.
|
-
- 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-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-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-111615A
-
|
|
Somatostatin Receptor
|
Inflammation/Immunology
Neurological Disease
|
|
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-147293
-
|
Relacorilant; CORT125134
|
Glucocorticoid Receptor
Apoptosis
Caspase
|
Cancer
|
|
Nenocorilant (Relacorilant) is 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-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-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-17497
-
-
- HY-145585
-
|
|
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-138641
-
|
ARV-110
|
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.
|
-
- 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.
|
-
- HY-19583
-
-
- 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-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-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-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-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-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-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-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-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-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-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-149993
-
-
- 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-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-B0203A
-
|
R 065824 hydrochloride
|
Adrenergic Receptor
|
Cardiovascular Disease
Endocrinology
|
|
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
|
|
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-103187
-
|
|
Adenosine Receptor
|
Cancer
Inflammation/Immunology
|
|
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, itcontains an Alkyne group and can undergo copper-catalyzed azide-alkyne cycloaddition (CuAAc) with molecules containing Azide groups.
|
-
- HY-145600
-
|
|
Opioid Receptor
Arrestin
|
Neurological Disease
|
|
Tegileridine is the potent agonist of opioid receptor (MOR). Tegileridine is an oxa spiro derivative which reduces the side effects mediated by β-arrestin. Tegileridine has the potential for the research of pains and pains-related diseases (extracted from patent WO2017063509A1).
|
-
- 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, itcontains 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-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-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-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-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-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-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-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-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-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-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-14407
-
-
- HY-B0661
-
-
- HY-P99626
-
|
LY 3015014
|
Ser/Thr Protease
|
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-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-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-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-N3359
-
-
- 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-116144
-
|
Lcaridin
|
Parasite
|
Infection
|
|
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-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
-
|
|
Others
|
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-P1112
-
-
- 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-117378
-
|
KRP-204
|
Adrenergic Receptor
|
Cancer
Inflammation/Immunology
|
|
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-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-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-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-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-P1112A
-
|
|
Endothelin Receptor
|
Neurological Disease
Cardiovascular 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-153935
-
-
- HY-107561
-
|
|
Others
|
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-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-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-18314
-
-
- HY-120081A
-
|
|
Others
|
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
-
|
|
Others
|
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-105120A
-
|
|
Others
|
Others
|
|
Vapiprost hydrochloride is a thromboxane A2 receptor antagonist. Vapiprost 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-120081B
-
|
|
Others
|
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-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-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-156111
-
|
|
Androgen Receptor
PROTACs
|
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-132935
-
|
|
c-Fms
|
Cancer
Inflammation/Immunology
|
|
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-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-19608
-
-
- 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-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-135882
-
-
- 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-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-156190
-
|
|
Others
|
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-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 specific neuroprotection in a Parkinson’s Disease rat model.
|
-
- 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
-
|
|
Adrenergic Receptor
5-HT 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-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-117820
-
-
- 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-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-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-110050
-
-
- HY-147105
-
|
|
Others
|
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-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-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-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-151744
-
|
|
ADC Linker
|
Others
|
|
N3-TFBA-O2Oc is a click chemistry reagent containing an azide group and an aryl group. Aryl azides are well-known precursors of nitrenes and have been introduced by Fleet et al. as versatile photoaffinity labeling agents to probe biological receptors. This type of compounds has been used as photo-cross linker (λmax=258 nm) in estrogen receptor studies and for direct surface coating of carbon and organic based polymers.
|
-
- HY-12355A
-
|
BAF-312 hemifumarate
|
LPL Receptor
|
Inflammation/Immunology
Neurological Disease
|
|
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-14648
-
-
- 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, itcontains an Alkyne group and can undergo copper-catalyzed azide-alkyne cycloaddition (CuAAc) with molecules containing Azide groups.
|
-
- 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-N6932
-
-
- 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-P4146A
-
|
BI 456906 TFA
|
GLP Receptor
|
Metabolic Disease
|
|
Survodutide (BI 456906) (TFA) is an glucagon and glucagon-like peptide 1 (GLP-1) receptor agonist Survodutide (TFA) is equivalent to Survodutide HY-P4146.
|
-
- 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-103563
-
|
|
Others
|
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-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-A0030
-
|
|
mAChR
|
Metabolic Disease
Neurological Disease
|
|
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
|
Metabolic Disease
Neurological 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-N1919
-
|
Raubasine
|
Adrenergic Receptor
Cholinesterase (ChE)
|
Endocrinology
Neurological Disease
|
|
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)
|
Endocrinology
Neurological Disease
|
|
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-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-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
-
|
|
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-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-14648A
-
-
- HY-B1481A
-
|
Isoetarine
|
Adrenergic Receptor
|
Inflammation/Immunology
Cardiovascular Disease
|
|
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
|
Inflammation/Immunology
Cardiovascular Disease
|
|
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-108847
-
|
|
TNF Receptor
Bacterial
|
Inflammation/Immunology
Cancer
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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.
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- HY-107320
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Prostaglandin Receptor
COX
NO Synthase
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Inflammation/Immunology
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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-W014728
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Dopamine Receptor
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Neurological Disease
Cardiovascular Disease
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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.
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- HY-136181
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Orexin Receptor (OX Receptor)
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Neurological Disease
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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.
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- HY-P1338A
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Opioid Receptor
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Neurological Disease
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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.
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- HY-105182A
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LY 246708 tartrate
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mAChR
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Neurological Disease
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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.
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- HY-14569
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mGluR
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Neurological Disease
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CDPPB is a potent, selective and brain penetrant positive allosteric modulator of the metabotropic glutamate receptor subtype 5 (mGluR5), with an EC50 of 27 nM in Chinese hamster ovary cells expressing human mGluR5. CDPPB may provide an approach for development of antipsychotic agents.
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- HY-103570
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mGluR
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Neurological Disease
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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) .
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- HY-122066
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Others
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Infection
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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.
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- HY-P3632
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DADAD
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Opioid Receptor
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Metabolic Disease
Neurological Disease
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[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.
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- HY-19589
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- HY-110237
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P2X Receptor
Calcium Channel
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Cardiovascular Disease
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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.
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- HY-N2080
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