Search Result
Results for "
antagonist
" in MedChemExpress (MCE) Product Catalog:
6201
Inhibitors & Agonists
11
Biochemical Assay Reagents
474
Isotope-Labeled Compounds
| Cat. No. |
Product Name |
Target |
Research Areas |
Chemical Structure |
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- HY-P1185
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- HY-155352
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mGluR
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Neurological Disease
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mGluR5 antagonist-1 is an orally active mGluR5 antagonist with an IC50 value of 11.5 nM. mGluR5 antagonist-1 has anti-depressant effect. mGluR5 antagonist-1 can be used for the study of depressive disorder .
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- HY-P1185A
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Vasopressin Receptor
Apoptosis
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Cancer
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Antagonist G TFA is a potent vasopressin antagonist. Antagonist G is also a weak antagonist of GRP and Bradykinin. Antagonist G induces AP-1 transcription and sensitizes cells to chemotherapy .
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- HY-128229
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- HY-149084
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- HY-157455
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Androgen Receptor
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Cancer
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AR antagonist 5 (compound 30a) is a selective androgen receptor (AR) antagonist with an IC50 value of 134.8 nM. AR antagonist 5 has favorable pharmacokinetic properties and shows a high skin exposure and low plasma exposure [1.
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- HY-157496
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Prostaglandin Receptor
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Others
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EP3 antagonist 7 (Compound II) is an EP3 receptor antagonist. EP3 antagonist 7 can be used in the study of itching, pain, dysuria or stress disorders .
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- HY-120652
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Adenosine Receptor
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Inflammation/Immunology
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A3AR antagonist 3 (compound 21) is a selective A3 adenosine receptor (A3AR) antagonist with a Ki of 37 nM. A3AR antagonist 3 shows >60-fold selectivity in comparison to A1 and A2A adenosine receptors .
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- HY-W037193
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- HY-170951
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Androgen Receptor
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Cancer
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AR antagonist 10 (Compound Y5) is potent and orally active androgen receptor (AR) antagonist with an IC50 of 0.04 μM. AR antagonist 10 demonstrates dual mechanisms of action, antagonizes AR by disrupting AR dimerization, and induces AR degradation via the ubiquitin-proteasome pathway. AR antagonist 10 exhibits excellent activity against variant drug-resistant AR mutants. AR antagonist 10 effectively suppresses the tumor growth of the LNCaP xenograft. AR antagonist 10 is potential to be used for drug-resistant prostate cancer .
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- HY-163504
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- HY-162070
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- HY-108513
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Sigma Receptor
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Neurological Disease
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σ1 Receptor antagonist 4 (compound TC1) is a selective sigma1 (σ1) receptor antagonist with a Ki of 10 nM. σ1 Receptor antagonist 4 is weakly active at σ2 receptor (Ki of 370 nM) and has no activity at dopamine (DAT), serotonin (SERT), and norepinephrine (NET) transporters .
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- HY-172226
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P2Y Receptor
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Inflammation/Immunology
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P2Y14R antagonist 3 (Compound A) is a potent and orally active P2Y14R antagonist with an IC50 value of 23.60 nM and a Kd value of 7.26 μM. P2Y14R antagonist 3 can reduce the degree of lung injury in the Lipopolysaccharides (LPS) (HY-D1056)-induced acute lung injury mice. P2Y14R antagonist 3 can be used for inflammatory diseases .
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- HY-147544
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- HY-147543
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- HY-147545
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- HY-170654
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Opioid Receptor
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Neurological Disease
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Opioid receptor antagonist 1 (Compound 10) is an Orvinol (HY-D0168)-based opioid receptor antagonist. Opioid receptor antagonist 1 has antagonistic activity to the analgesic properties of Morphine .
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- HY-149274
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Sigma Receptor
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Neurological Disease
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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 .
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- HY-144733
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Estrogen Receptor/ERR
Apoptosis
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Cancer
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ERα antagonist 1 (Compound 19d) is a potent, selective, covalent estrogen receptor α (ERα) antagonist. ERα antagonist 1 induces apoptosis and cell cycle G0/G1 phase arrest in MCF-7 cells .
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- HY-168098
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P2Y Receptor
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Inflammation/Immunology
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P2Y6R antagonist 1 (compound 5ab) is a selective, orally active P2Y6R antagonist with an IC50 value of 19.6 nM. P2Y6R antagonist 1 has anti-inflammatory activity .
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- HY-W278072
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Calcium Channel
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Neurological Disease
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Calcium Channel antagonist 1 is an antagonist of Calcium Channel Calcium Channel antagonist 1 has the potential for the research of neurology disease .
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- HY-139035
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CRFR
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Neurological Disease
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CRHR1 antagonist 1 (compound 10a) is a non-peptide corticotropin-releasing hormone type 1 receptor (CRHR1) antagonist. CRHR1 antagonist 1 can be utilized in mental disorders research .
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- HY-148650A
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Neurotensin Receptor
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Neurological Disease
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(R)-Sortilin antagonist 1 is a sortilin antagonist that blocks the sortilin mediated apoptosis pathway by interfering with the binding of sortilin to its ligand pro-neurotrophin. (R)-Sortilin antagonist 1 can be used in the study of hearing loss .
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- HY-W278072R
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Calcium Channel
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Neurological Disease
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Calcium Channel antagonist 1 (Standard) is the analytical standard of Calcium Channel antagonist 1. This product is intended for research and analytical applications. Calcium Channel antagonist 1 is an antagonist of Calcium Channel Calcium Channel antagonist 1 has the potential for the research of neurology disease .
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- HY-147226
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Prostaglandin Receptor
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Neurological Disease
Endocrinology
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EP3 antagonist 3 (compound 2) is an orally active, potent and selective EP3 antagonist, with a pKi of 8.3. EP3 antagonist 3 shows excellent pharmacokinetic properties. EP3 antagonist 3 can be used for overactive bladder (OAB) research .
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- HY-155300
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Leukotriene Receptor
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Inflammation/Immunology
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BLT2 antagonist-1 (compound 15b) is a selective BLT2 antagonist that inhibits the chemotaxis of CHO-BLT2 cells with an IC50 of 224 nM. BLT2 antagonist-1 does not inhibits the chemotaxis of CHO-BLT1 cells. BLT2 antagonist-1 also inhibits the binding of LTB4 and BLT2 with a Ki value of 132 nM. BLT2 antagonist-1 can be used for the research of the inflammatory airway diseases such as asthma and chronic obstructive pulmonary disease .
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- HY-171235
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5-HT Receptor
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Neurological Disease
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5-HT2A antagonist 3 (Formula (III)) is a 5-HT2A receptor antagonist and inverse agonist with a pIC50 of 8.7 and a pKi of 9. 5-HT2A antagonist 3 can be utilized in neurological reesearch .
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- HY-112628
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AHR antagonist 7
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Aryl Hydrocarbon Receptor
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Cancer
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CAY10464 (AHR antagonist 7; compound 4j) is a selective and high-affinity aryl hydrocarbon receptor (AhR) antagonist with a Ki of 1.4 nM .
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- HY-P10204
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Wnt
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Cancer
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FZD7 antagonist 1 (peptide 34) is a dFz7-21 analogue. FZD7 antagonist 1 is an FZD7 antagonist that inhibits the wnt3a with IC50 value of 9.2 nM. FZD7 antagonist 1 blocks TcdB−FZD interaction via targeting FZD receptors .
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- HY-155490
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Nuclear Hormone Receptor 4A/NR4A
Apoptosis
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Cancer
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Nur77 antagonist 1(Compound ja) is a selective Nur77 antagonist(KD SPRNur77 = 91 nM). Nur77 antagonist 1 induces cancer cell apoptosis. ja displays excellent antitumor against triple-negative breast cancer (TNBC) cells .
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- HY-156293
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Formyl Peptide Receptor (FPR)
Apoptosis
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Cancer
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FPR1 antagonist 1 (compound 24a) is a formyl peptide receptor 1 (FPR1) antagonist with an IC50 of 25 nM. FPR1 antagonist 1 inhibits cell growth through a combined effect on cell proliferation and apoptosis and reduces cell migration, while inducing an increase in angiogenesis .
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- HY-156294
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Formyl Peptide Receptor (FPR)
Apoptosis
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Cancer
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FPR1 antagonist 2 (compound 25b) is a formyl peptide receptor 1 (FPR1) antagonist with an IC50 of 70 nM. FPR1 antagonist 2 inhibits cell growth through a combined effect on cell proliferation and apoptosis and reduces cell migration, while inducing an increase in angiogenesis .
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- HY-161914
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P2X Receptor
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Neurological Disease
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P2X3 antagonist 39 (compound 26a) is a selective P2X3 receptor antagonist with an IC50 value of 54.9 nM. P2X3 antagonist 39 can be used in the study of neuropathic pain model .
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- HY-157493
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Progesterone Receptor
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Endocrinology
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PR antagonist 1 (compound 8) is a selective progesterone receptor (PR) antagonist, and can be used for the research of a variety of progesterone-related diseases and disorders such as endometriosis and uterine fibroids .
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- HY-163895
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Fluorescent Dye
Opioid Receptor
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Neurological Disease
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δ opioid receptor antagonist 1 (compound 6-Cy3) is a fluorescent antagonist probe with high selectivity for δ opioid receptor (DOR) (Ki=1.7 nM). δ opioid receptor antagonist 1 can be used to study the mechanism of pain perception .
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- HY-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-129995A
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TSH Receptor
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Endocrinology
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TSHR antagonist S37a is a highly selective thyrotropin receptor (TSHR) antagonist, with potential for the treatment of Graves' orbitopathy .
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- HY-12908
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Bcl-2 Family
Apoptosis
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Cancer
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Bcl-xL antagonist 2 is a potent, selective, and orally active antagonist of BCL-XL with an IC50 and Ki of 0.091 μM and 65 nM, respectively. Bcl-xL antagonist 2 promotes the apoptosis of cancer cells. Bcl-xL antagonist 2 has the potential for the research of the chronic lymphocytic leukemia (CLL) and non-Hodgkin’s lymphoma (NHL) .
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- HY-160025
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- HY-158338
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MAGL
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Others
Neurological Disease
Inflammation/Immunology
Cancer
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ABHD antagonist 1 possesses ABHD6 (α/β-Hydrolase domain containing 6) inhibitory activity, involving the regulation of biochemical pathways involved in ABHD6, thereby affecting cell function and inflammatory response. ABHD antagonist 1 can be used in pain, neuropathic diseases, inflammatory diseases. Autoimmune diseases, metabolic diseases, and cancer research .
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- HY-147808
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CXCR
HIV
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Infection
Inflammation/Immunology
Cancer
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CXCR4 antagonist 7 (Compound PARA-B) is a CXCR4 antagonist with the IC50 of 9.3 nM. CXCR4 antagonist 7 can be used for the research of HIV infection, inflammatory diseases, cancer, and WHIM syndrome .
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- HY-155417
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ERK
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Neurological Disease
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GPR34 receptor antagonist 3 (Compound 5e) is a class of GRP34 antagonists, IC50 is 0.680?μM. GPR34 receptor antagonist 3 inhibited ERK1/2 phosphorylation induced by lysophosphatidylserine in a dose-dependent way without obvious cytotoxicity. GPR34 receptor antagonist 3 shows antisensory activity in mouse neuropathic pain model .
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- HY-162090
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TRP Channel
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Cancer
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TRPC antagonist 1 (compound 15g) is a potent TRP channel (TRPC) antagonist with IC50s of 2.4 μM, 12.2 μM, 7.6 μM, 2.9 μM, and 3.4 μM for TRPC3, TRPC4, TRPC5, TPRC6, and TRPC7, respectively. TRPC antagonist 1 displays noteworthy anti-glioblastoma efficacy in vitro against U87 cell lines .
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- HY-148038
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5-HT Receptor
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Neurological Disease
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5-HT3 antagonist 5 is a quinoxalin-2-carboxamide compound, a 5-HT3 receptor antagonist. 5-HT3 antagonist 5 exerts antagonism on 5-HT3 agonist and 2-methyl-5-HT, and shows anti-depressant effect in mice .
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- HY-147203
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5-HT Receptor
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Cardiovascular Disease
Metabolic Disease
Endocrinology
Cancer
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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 .
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- HY-139643A
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CXCR
Adrenergic Receptor
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Inflammation/Immunology
Cancer
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CXCR7 antagonist-1 hydrochloride is a CXCR7 antagonist that inhibits the binding of the SDF-1 chemokine (also known as the CXCL12 chemokine) or I-TAC (also known as CXCL11) to the chemokine receptor CXCR7. CXCR7 antagonist-1 hydrochloride is useful in preventing tumor cell proliferation, tumor formation, inflammatory diseases, and many other diseases .
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- HY-139643
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CXCR
Adrenergic Receptor
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Inflammation/Immunology
Cancer
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CXCR7 antagonist-1 is a CXCR7 antagonist that inhibits the binding of the SDF-1 chemokine (also known as the CXCL12 chemokine) or I-TAC (also known as CXCL11) to the chemokine receptor CXCR7. CXCR7 antagonist-1 is useful in preventing tumor cell proliferation, tumor formation, inflammatory diseases, and many other diseases .
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- HY-147222
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SAE-14
1 Publications Verification
GPR183 antagonist-1
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EBI2/GPR183
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Neurological Disease
Inflammation/Immunology
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SAE-14 (compound SAE-14) is a potent, specific GPR183 antagonist with an IC50 value of 28.5 nM, can antagonize 7α, 25-OHC–induced calcium mobilization with IC50 value below 50 nM in HL-60 cells. GPR183 antagonist-1 can reverse allodynia in mice .
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- HY-148533
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mAChR
Adrenergic Receptor
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Neurological Disease
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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) .
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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-162812
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Apoptosis
Cholinesterase (ChE)
Tau Protein
Ferroptosis
Histamine Receptor
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Neurological Disease
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H3R antagonist 4 (compound 11L) was a dual inhibitor of cholinesterase and histamine receptor (H3R), with corresponding IC50 of 7.04 μM (eeAChE), 9.73 μM (hAChE)(reversible) and 1.09 nM (H3R) , respectively. H3R antagonist 4 inhibited the aggregation of Aβ1-42 induced by itself and Cu 2+ (95.48% and 88.63%) , and degraded the Aβ1-42 fibrils induced by itself and Cu 2+ (80.16% and 89.30%) . H3R antagonist 4 chelate biometals such as Cu 2+, Zn 2+, Al 3+, and Fe 2+. H3R antagonist 4 significantly reduced tau protein hyperphosphorylation induced by Aβ1-42 and inhibited RSL-3-induced apoptosis and ferroptosis in PC12 cells. H3R antagonist 4 had the best blood-brain barrier permeability and intestinal absorption in hCMEC/D3 and hPepT1-MDCK cells.H3R antagonist 4 ameliorates learning and memory impairment in a mouse model of Alzheimer's disease induced by scopolamine (HY-N0296) .
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- HY-114945
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- HY-15015A
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- HY-162925
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CGRP Receptor
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Neurological Disease
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CGRP antagonist 6 (Compound 23) is a CGRP receptor antagonist (Ki: 0.84 nM). CGRP antagonist 6 can be used for research of migraine .
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- HY-103304
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CGRP Receptor
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Neurological Disease
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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 .
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- HY-162664
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STING
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Inflammation/Immunology
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STING antagonist 1 is an antagonist of STING with an IC50 of 3.8 nM. STING antagonist 1 can be used in the research of autoimmune diseases, inflammatory diseases, and others .
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- HY-15015
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Oxytocin receptor antagonist 1
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Oxytocin Receptor
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Endocrinology
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OT-R antagonist 1 is a new potent and selective nonpeptide low molecular weight OT-R antagonist.
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- HY-144377
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RAR/RXR
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Neurological Disease
Metabolic Disease
Cancer
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RXR antagonist 1 (compound 6a) is a retinoid X receptor (RXR) modulator. RXR antagonist 1 shows potent RXR-antagonistic activity, with a pA2 of 8.06. RXR antagonist 1 can be used for type 2 diabetes research .
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- HY-111500
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iGluR
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Neurological Disease
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(Rac)-NMDAR antagonist 1 is the racemate of NMDAR antagonist 1. NMDAR antagonist 1 is a potent and orally bioavailable NR2B-selective NMDAR antagonist .
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- HY-162421
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Herbicide
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Others
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SL antagonist 1 (Compound D12) is strigolactones antagonists and can strongly interact with SL receptor proteins.SL antagonist 1 can combat root-parasitic weed infestations. SL antagonist 1 has no side effects on the germination or seedling growth .
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- HY-112264
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- HY-103650
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- HY-U00320
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- HY-U00330
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- HY-172612
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Androgen Receptor
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Cancer
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AR antagonist 13 (compound 19) is an androgen receptor antagonist with inhibition rates exceeding 71.5% at 10 μM. AR antagonist 13 inhibits prostate cancer cell growth .
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- HY-144383
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RAR/RXR
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Others
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RXR antagonist 2 (compound 6b) is a potent antagonist of RXR with a Ki and Kd of 0.391 and 0.281 μM. RXR antagonist 2 has the potential for the research of RXR related diseases .
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- HY-148874A
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FXR
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Metabolic Disease
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FXR antagonist 2 (compound A-26) hydrochloride is a diarylamide derivative, as well as a moderate FXR antagonist. FXR antagonist 2 hydrochloride can be used in the study of hyperlipidemia and type 2 diabetes .
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- HY-148874
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FXR
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Metabolic Disease
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FXR antagonist 2 (compound A-26) is a diarylamide derivative, as well as a moderate FXR antagonist. FXR antagonist 2 can be used in the study of hyperlipidemia and type 2 diabetes .
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- HY-148844
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GCGR
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Metabolic Disease
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GCGR antagonist 2, a Furan-2-carbohydrazide, is an orally active glucagon receptor antagonist. GCGR antagonist 2 binds to hGluR with an Kd value of 2.3 nM, and inhibits rat receptor with an IC50 value of 0.43 nM. GCGR antagonist 2 inhibits glucagon-stimulated glycogenolysis .
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- HY-103649
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- HY-136437
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CXCR
HIV
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Infection
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CXCR4 antagonist 1 is a potent CXCR4 antagonist. CXCR4 antagonist 1 has anti-HIV activity .
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- HY-144127
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Androgen Receptor
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Cancer
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AR antagonist 3 is a potent and selective androgen receptor (AR) antagonist with an IC50 of 0.47 µM. AR antagonist 3 exhibits a dose-dependent decrease of the FRET signal (IC50= 18.05 μM). AR antagonist 3 shows effective inhibition on tumor growth when administered intratumorally .
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- HY-163665
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Aryl Hydrocarbon Receptor
Dystrophin
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Others
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AHR antagonist 8 (compound SG-02) is a regulator of utrophin, a homolog of dystrophin, and an AhR antagonist (Kd: 41.68 nM). Studies have shown that 800 nM of AHR antagonist 8 can upregulate utrophin by 2.7 times. AHR antagonist 8 also stimulates increased MyHC expression, suggesting that it has the potential to enhance myogenesis. After ADME evaluation, AHR antagonist 8 also has a certain oral bioavailability .
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- HY-134864
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GnRH Receptor
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Endocrinology
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GnRH antagonist 2 (formula I) is a GnRH receptor antagonist that can be used for endometriosis research .
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- HY-173325
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LPL Receptor
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Cardiovascular Disease
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LPA2 antagonist 6 (example 2) is an antagonist of Lp(a). LPA2 antagonist 6 inhibits Lp(a) formation with an IC50 value of 2.33 nM. LPA2 antagonist 6 can be used in the research of cardiovascular disease .
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- HY-103651
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Oxytocin Receptor
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Endocrinology
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OT antagonist 1 demethyl derivative is the demethyl derivative of OT antagonist 1. OT antagonist 1 (Compound 4) is a potent, selective Oxytocin antagonist with a Ki of 50 nM.
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- HY-103652
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- HY-112562
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- HY-148650
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Neurotensin Receptor
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Neurological Disease
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Sortilin antagonist 1 (compound 44) is a sortilin antagonist with an IC50 value of 20 nM for inhibiting Neurotensin (NTS) binds to sortilin. Neurotensin is a sortilin ligand. Sortilin antagonist 1 can be used for the research of neurological disease .
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- HY-170589
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- HY-147392
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CXCR
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Metabolic Disease
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CXCR2 antagonist 8 is a potent and selective CXCR2 antagonist. CXCR2 antagonist 8 can be used for insulin resistance research .
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- HY-160692
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Androgen Receptor
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Others
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AR antagonist 7 (86) is an androgen receptor (AR) antagonist that can be used in the research of hair loss .
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- HY-169707
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GCGR
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Metabolic Disease
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GCGR antagonist 3 (example 1) is an antagonist of the glucagon receptor (GCGR) and can be used in diabetes research .
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- HY-W008038
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iGluR
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Others
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NMDAR antagonist 3 (Compound 2) is an antagonist of the NMDA receptor. NMDAR antagonist 3 has a certain but weak inhibitory activity against the NR1A/2B subtype of the NMDA receptor .
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- HY-159895
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Protease Activated Receptor (PAR)
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Cardiovascular Disease
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PAR4 antagonist 7 (Compound 20f) is selective PAR4 antagonist (IC50: 1.72 nM). PAR4 antagonist 7 inhibits PAR4 agonist-induced platelet aggregation. PAR4 antagonist 7 has good metabolic stability. PAR4 antagonist 7 does not show a bleeding tendency in mice .
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- HY-149823
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TRP Channel
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Neurological Disease
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TRPV4 antagonist 4 is a potent TRPV4 antagonist with an IC50 value of 22.65 nM. TRPV4 antagonist 4 inhibits TRPV4 current. TRPV4 antagonist 4 shows protective effects on acute lung injury .
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- HY-159972
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- HY-173409
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Androgen Receptor
Ser/Thr Protease
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Inflammation/Immunology
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AR antagonist 11 (Compound c2) is a selective AR antagonist with an IC50 of 0.019 μM. AR antagonist 11 is also effective against AR F877L/T878A mutant (IC50: 1.03 μM). AR antagonist 11 inhibits LNCaP cell proliferation and reduces PSA protein expression (IC50: 0.54 μM). AR antagonist 11 can be used for research of prostate cancer (PCa) .
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- HY-112265
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- HY-123301
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- HY-18075
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- HY-101536
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- HY-153772
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Androgen Receptor
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Cancer
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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 .
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- HY-111500A
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- HY-173398
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iGluR
Monoamine Transporter
Serotonin Transporter
Dopamine Transporter
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Neurological Disease
|
|
NMDAR antagonist 5 (Compound A17) is a multi-target antagonist against NMDAR and monoamine transporters (SERT、DAT and NET). NMDAR antagonist 5 shows good NMDAR antagonistic potency (IC50 = 0.3 μM) and monoamine transporter activities (SERT IC50 = 1.1 μM、DAT IC50 = 0.7 μM、NET IC50 = 2.7 μM). NMDAR antagonist 5 is highly safe and has low toxicity (hepatotoxicity and nephrotoxicity (IC50 > 100 μM); cardiotoxicity (IC50 = 24.5 μM)). NMDAR antagonist 5 has antidepressant effects and can be used in the study of depression .
|
-
- HY-146405
-
|
|
nAChR
|
Neurological Disease
Inflammation/Immunology
|
|
nAChR antagonist 1 (compound B15) is an excellent α7 nAChR antagonist with an IC50 value of 3.3 μM. nAChR antagonist 1 can be used for researching schizophrenia, Alzheimer’s disease and inflammatory disorders .
|
-
- HY-147762
-
-
- HY-160105
-
-
- HY-101264
-
-
- HY-112689
-
-
- HY-132936
-
|
|
CXCR
|
Others
|
|
CXCR4 antagonist 2 is a CXCR4 antagonist with an IC50 value of 47 nM.
|
-
- HY-160659
-
|
|
Androgen Receptor
|
Endocrinology
|
|
Androgen receptor antagonist 10 (compound 6h) is a androgen receptor antagonist. Androgen receptor antagonist 10 reduces the wax esters in the golden syrian hamster model .
|
-
- HY-153165
-
|
|
RAR/RXR
|
Others
|
|
RXR antagonist 5 (compound 22) is a selective retinoic acid X receptor (RXR) antagonist with binding potential to RXR evaluated by modeling.
|
-
- HY-107705
-
|
|
iGluR
|
Neurological Disease
|
|
NMDAR antagonist 4 (Compound 8) is the antagonist for NMDA receptor that binds NMDA receptor on glycine site with Ki >100 μM .
|
-
- HY-160680
-
|
|
Androgen Receptor
|
Endocrinology
|
|
AR antagonist 6 (compound 6i) is a diphenyl ether androgen receptor (AR) antagonist that binds AR at a concentration of 120 nM. AR antagonist 6 exhibits low toxicity and in vitro activity against the golden Syrian hamster ear model .
|
-
- HY-160647
-
|
|
CCR
|
Inflammation/Immunology
|
|
CCR8 antagonist 3 (compound 2) is a CCR8 antagonist with an IC50 value of 0.062 µM. CCR8 antagonist 3 shows human microsomal stability .
|
-
- 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-14231
-
|
|
CCR
|
Infection
Inflammation/Immunology
|
|
CCR5 antagonist 5 (compound example 11) is a CCR5 antagonist. CCR5 antagonist 5 has the potential to study inflammation and immunity and viral (such as HIV) infection .
|
-
- HY-168095
-
|
|
CXCR
|
Cancer
|
|
CXCR4 antagonist 10 (compound 21) is a potent antagonist of CXCR4, with the IC50 of 7.8 nM. CXCR4 antagonist 10 plays an important role in cancer research .
|
-
- HY-136152
-
-
- HY-133034
-
|
|
Complement System
|
Cancer
|
|
NRP1 antagonist 1 (compound 12a) is a potent NRP1 antagonist with an IC50 of 19.1 μM. NRP1 antagonist 1 has the potential for cancer research .
|
-
- HY-142620
-
-
- HY-U00375
-
-
- HY-111218
-
-
- HY-124668A
-
|
|
CCR
|
Others
|
|
CCR1 antagonist 13 is a selective CCR1 small molecule antagonist .
|
-
- HY-112262
-
-
- 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-136922
-
-
- HY-158339
-
|
|
MAGL
|
Neurological Disease
|
|
ABHD antagonist 2 (Compound 9) is an antagonist for alpha/beta-Hydrolase domain containing 6 (ABHD6), with IC50 <0.001 μM. ABHD antagonist 2 exhibits good binding ability with ABHD6, with IC50 of 0.002 μM .
|
-
- HY-151481A
-
|
|
FXR
|
Neurological Disease
|
|
β-FXR antagonist 1 (C 12), an isomer of FXR antagonist 1 (HY-151481) is a FXR antagonist .
|
-
- HY-144286
-
|
|
CXCR
|
Infection
|
|
CXCR4 antagonist 3 (compound 12a) is a potent antagonist of CXCR4 with an IC50 of 11 nM. CXCR4 antagonist 3 is a congener of TIQ15. CXCR4 antagonist 3 demonstrates the best overall properties including CXCR4 antagonism, CYP 2D6 inhibition, metabolic stability, and permeability. CXCR4 antagonist 3 has the potential for the research of human immunodeficiency virus .
|
-
- HY-18668
-
|
|
Integrin
|
Cancer
|
|
Integrin antagonist 27 is a small molecule integrin αvβ3 antagonist with binding affinity of 18 nM, as s novel anticancer agent.
|
-
- HY-152132
-
|
|
CCR
HIV
|
Infection
|
|
CCR5 antagonist 3 (Compound 26) is a CCR5 antagonist with an IC50 of 15.90 nM. CCR5 antagonist 3 shows broad-spectrum anti-HIV-1 activities .
|
-
- HY-172908
-
|
|
Androgen Receptor
|
Cancer
|
|
Androgen receptor antagonist 13 (compound 8a) is an orally active Androgen receptor antagonist with an IC50 of 0.20 μM. Androgen receptor antagonist 13 can be used in the study of prostate cancer .
|
-
- HY-149082
-
|
|
Leukotriene Receptor
|
Inflammation/Immunology
|
|
LTB4 antagonist 1, a carboxamide-acid compound, is a potent Leukotriene B4 (LTB4) antagonist with an IC50 of 288 nM. LTB4 antagonist 1 has significant anti-inflammatory properties .
|
-
- HY-160616
-
-
- HY-152131
-
|
|
CCR
HIV
|
Infection
|
|
CCR5 antagonist 2 (Compound 25) is a CCR5 antagonist with an IC50 of 8.34 nM. CCR5 antagonist 2 shows broad-spectrum anti-HIV-1 activities .
|
-
- 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-162267
-
|
|
LPL Receptor
|
Inflammation/Immunology
|
|
LPAR1 antagonist 1 (compound 18) is a potent, oral active and selective LPAR1 antagonist with the IC50 of 3.3 nM. LPAR1 antagonist 1 can be used for study of fibrosis .
|
-
- HY-131664
-
|
|
Prostaglandin Receptor
|
Others
|
|
EP3 antagonist 2 (Compound Exp 1) is a potent and selective EP3 receptor antagonist. EP3 antagonist 2 has a strong binding affinity for the human EP3 receptor (Ki: 3.3 nM) and significant antagonistic activity (IC50: 30.8 nM, determined by cellular cAMP levels) .
|
-
- HY-155542
-
|
|
ROR
|
Cancer
|
|
RORγ antagonist 1 (compound 22), a potent betulinic acid derivative, is an antagonist of RORγ (KD=0.18 μM). RORγ antagonist 1 exhibits anti-proliferative activity in HPAF-II pancreatic cancer xenograft model. RORγ antagonist 1 inhibits RAS/MAPK and AKT/mTORC1 pathway, and induces caspase-dependent apoptosis in pancreatic cancer cells .
|
-
- HY-151481
-
|
|
FXR
|
Metabolic Disease
|
|
FXR antagonist 1 (compound F6) is an orally active and selective intestinal FXR antagonist (IC50=2.1 μM). FXR antagonist 1 selectively inhibits intestinal FXR signalling through antagonism of intestinal FXR and feedback activation of hepatic FXR to improve hepatic steatosis, inflammation and fibrosis in NASH (nonalcoholic steatohepatitis) models. FXR antagonist 1 can be used in NASH studies .
|
-
- HY-115912
-
|
|
Glycoprotein VI
|
Cardiovascular Disease
|
|
GPVI antagonist 3 (Compound 2) is a potential antagonist of Glycoprotein VI (GPVI). IC50 values of GPVI antagonist 3 are, respectively, 1.01 μM for collagen, 1.92 μM for CRP, 7.24 μM for convulxin and 51.74 μM for thrombin. Glycoprotein VI (GPVI) is a platelet major collagen receptor and a target for potent and safe antithrombotic research. GPVI antagonist 3 is a promising antiplatelet agent .
|
-
- HY-115911
-
|
|
Glycoprotein VI
|
Cardiovascular Disease
|
|
GPVI antagonist 2 (Compound 1) is a potential antagonist of Glycoprotein VI (GPVI). IC50 values of GPVI antagonist 2 are, respectively, 0.35 μM for collagen, 0.80 μM for CRP, 195.2 μM for convulxin and 81.38 μM for thrombin. Glycoprotein VI (GPVI) is a platelet major collagen receptor and a target for potent and safe antithrombotic research. GPVI antagonist 2 is a promising antiplatelet agent .
|
-
- HY-147979
-
|
|
CXCR
|
Infection
Cancer
|
|
CXCR4 antagonist 9 (Compound 2) is a CXCR4 antagonist with an IC50 of 15 nM. CXCR4 antagonist 9 inhibits CXCL12 induced cytosolic calcium increase with an IC50 of 1.3 nM .
|
-
- HY-144419
-
|
|
Adenosine Receptor
|
Cancer
|
|
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) .
|
-
- HY-160176
-
|
|
Somatostatin Receptor
|
Metabolic Disease
|
|
SSTR5 antagonist 6 is an orally active somatostatin receptor subtype 5 (SSTR5) antagonist with an IC50 of 24 nM. SSTR5 antagonist 6 can be used in the study of type 2 diabetes .
|
-
- HY-139675
-
-
- HY-173324
-
|
|
LPL Receptor
|
Others
|
|
LPA2 antagonist 5 (EX1) is a LPA2 antagonist, with an IC50 of 4.05 nM .
|
-
- HY-U00331
-
-
- HY-139873
-
|
|
CXCR
|
Cancer
|
|
CXCR2 antagonist 2 is a potent CXCR2 antagonist for cancer immunoresearch with an IC50 value of 95 nM.
|
-
- HY-160661
-
|
|
LPL Receptor
|
Others
|
|
LPAR1 antagonist 2 (example 76) is an LPAR1 antagonist with an average IC50 of 130 nM .
|
-
- HY-112263
-
-
- HY-163485
-
|
|
Androgen Receptor
|
Endocrinology
|
|
AR antagonist 8 (compound 16), an unnatural entestrane, is a potent Lupeol-inspired androgen receptor (AR) antagonist with an IC50 of 0.76 μM .
|
-
- HY-163072
-
|
|
FXR
|
Metabolic Disease
|
|
FXR antagonist 3 (V02-8) is an intestine-specific farnesoid X receptor (FXR) antagonist, with an IC50 of 0.89 μM .
|
-
- HY-131337
-
|
|
Bacterial
|
Infection
|
|
RhlR antagonist 1 is a potent RhlR antagonist with an IC50 of 26 μM. RhlR antagonist 1 displays selective RhlR antagonism over LasR and PqsR, strong inhibition of biofilm formation in static and dynamic settings, and reduces production of virulence factors such as rhamnolipid and pyocyanin in P. aeruginosa. RhlR antagonist 1 can be utilized for developing QS-modulating molecules in the control of P. aeruginosa infections . RhlR antagonist 1 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-P4717A
-
|
|
IFNAR
|
Inflammation/Immunology
|
|
IFN-γ Antagonist 1 (AYCRDGKIGPPKLDIRKEEKQI) acetate is an antagonist of interferon γ (IFN γ). IFN-γ Antagonist 1 inhibits IFN-γ induced HLR/DR antigen expression in Colon 205 cells with an IC50 value of approximately 35 μM. IFN-γ Antagonist 1 has potential applications in immune regulation .
|
-
- HY-153256
-
|
|
Prostaglandin Receptor
|
Metabolic Disease
|
|
EP3 antagonist 4 (Compound 28) is an EP3 antagonist, with a Ki value of 2 nM for hEP. EP3 antagonist 4 shows low in vivo clearance, high oral AUC, and good bioavailability in the rat full PK studies. EP3 antagonist 4 can be used for research of beta cell dysfunction in diabetes .
|
-
- HY-147978
-
|
|
CXCR
|
Infection
Cancer
|
|
CXCR4 antagonist 8 (Compound 3) is a CXCR4 antagonist with an IC50 of 57 nM. CXCR4 antagonist 8 inhibits CXCL12 induced cytosolic calcium increase with an IC50 of 0.24 nM. CXCR4 antagonist 8 inhibits CXLC12/CXCR4 mediated cell migration .
|
-
- HY-P4717
-
|
|
IFNAR
|
Inflammation/Immunology
|
|
IFN-γ Antagonist 1 (AYCRDGKIGPPKLDIRKEEKQI) is an antagonist of interferon γ (IFN γ). IFN-γ Antagonist 1 inhibits IFN-γ induced HLR/DR antigen expression in Colon 205 cells with an IC50 value of approximately 35 μM. IFN-γ Antagonist 1 has potential applications in immune regulation .
|
-
- HY-124668
-
|
|
CCR
|
Inflammation/Immunology
|
|
CCR1 antagonist 12 (Compound 12) is an antagonist for CCR1 with IC50 of 3 nM for human CCR1. CCR1 antagonist 12 inhibits CCL3-induced transwell chemotaxis with an IC50 of 0.009 µM. CCR1 antagonist 12 exhibits good pharmacokinetic characters in rats model .
|
-
- HY-144780
-
|
|
CXCR
|
Cancer
|
|
CXCR2 antagonist 4 (compound 7) is a potent CXCR2 antagonist with an IC50 value of 0.13 μM. CXCR2 antagonist 4 can inhibit CXCL8-induced cytosolic calcium increase (IC50 = 27 μM). CXCR2 antagonist 4 can be used for researching anticancer .
|
-
- HY-161682
-
|
|
GPR84
|
Neurological Disease
|
|
GPR84 antagonist 9 (compound 320) is an orally active GPR84 antagonist with the IC50 of 0.012 μM. GPR84 antagonist 9 can be used for study of inflammatory-driven pain diseases .
|
-
- HY-100321
-
-
- HY-146401
-
|
|
CXCR
|
Cancer
|
|
CXCR4 antagonist 6 (compound 46) is a potent CXCR4 antagonist with an IC50 value of 79 nM. CXCR4 antagonist 6 inhibits CXCL12 induced cytosolic calcium flux (IC50 = 0.25 nM). CXCR4 antagonist 6 significantly mitigates CXCL12/CXCR4 mediated cell migration. CXCR4 antagonist 6 exhibits marked efficacy in a cancer metastasis model in mice .
|
-
- HY-169349
-
|
|
Androgen Receptor
|
Cancer
|
|
Androgen receptor antagonist 12 (Compound EF2) is an orally active Androgen receptor (AR) antagonist (IC50: 0.30 μM). Androgen receptor antagonist 12 inhibits transcriptional activity of variant AR mutants and and the proliferation of AR-positive PCa cell lines. Androgen receptor antagonist 12 blocks AR nuclear translocation. Androgen receptor antagonist 12 inhibits tumor growth in a C4-2B xenograft mouse model. Androgen receptor antagonist 12 can be used for prostate cancer (PCa) research .
|
-
- HY-158124
-
|
|
Bacterial
|
Infection
|
|
LasR antagonist 1 (Compound 7) is an antagonist for LasR with an IC50 of 0.4 μM, that modulates the quorum sensing (QS) in the opportunistic pathogen Pseudomonas aeruginosa .
|
-
- HY-111443
-
-
- HY-157494
-
-
- HY-144197
-
-
- HY-159922
-
|
|
Androgen Receptor
|
Cancer
|
|
AR antagonist 9 is an orally bioavailable selective androgen receptor (AR) antagonist that exerts anticancer effects by disrupting the dimerization of AR ligand-binding domains, showing potential for overcoming drug resistance in prostate cancer (PCa). Its AR antagonistic activity has an IC50 value of 0.051 μM, comparable to Enzalutamide (HY-70002) (IC50 = 0.060 μM). AR antagonist 9 demonstrated superior efficacy against ARF876L/T877A and ARW741C mutants compared to Enzalutamide (HY-70002). Furthermore, AR antagonist 9 exhibited favorable pharmacokinetic properties, with an oral bioavailability of F = 66.24% in rats. In the LNCaP xenograft mouse model, oral administration of AR antagonist 9 significantly inhibited tumor growth. AR antagonist 9 holds promise for research into overcoming PCa drug resistance .
|
-
- HY-100331
-
-
- HY-161420
-
|
|
TRP Channel
|
Neurological Disease
|
|
TRPV1 antagonist 7 (Compound 36) is a selective TRPV1 antagonist that effectively blocks capsaicin activation (IC50=2.31 nM). TRPV1 antagonist 7 can be used in analgesic research .
|
-
- 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-162409
-
|
|
Protease Activated Receptor (PAR)
|
Others
|
|
PAR4 antagonist 4 (Compound 37) is a selective antagonist for protease activated receptor 4 (PAR4). PAR4 antagonist 3 exhibits antiplatelet efficacy with IC50 of 14.2 nM. PAR4 antagonist 3 improves metabolic stablility in human liver microsomes with T1/2 of 42.5 min .
|
-
- HY-163341
-
|
|
Protease Activated Receptor (PAR)
|
Cardiovascular Disease
|
|
PAR4 antagonist 1 (Compound 48) is a protease activated receptor 4 (PAR4) antagonist with an IC50 of 1.8 nM. PAR4 antagonist 1 has an IC50 of 2 nM against γ-thrombin-activated PAR4 in platelet-rich plasma (PRP). PAR4 antagonist 1 can be used in antithrombotic research .
|
-
- 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-162408
-
|
|
Protease Activated Receptor (PAR)
|
Others
|
|
PAR4 antagonist 3 (Compound 36) is a selective antagonist for protease activated receptor 4 (PAR4). PAR4 antagonist 3 exhibits antiplatelet efficacy with IC50 of 26.1 nM. PAR4 antagonist 3 improves metabolic stablility in human liver microsomes with T1/2 of 97.6 min .
|
-
- HY-157303
-
|
|
Somatostatin Receptor
|
Cardiovascular Disease
|
|
SSTR5 antagonist 3 (Compound 23) is an orally active somatostatin receptor subtype 5 (SSTR5) antagonist with low hERG inhibition. SSTR5 antagonist 3 exhibits potency with IC50 values of 2.8 nM and 1.4 nM in human and mouse, respectively. SSTR5 antagonist 3 can be used for the research of anti-gallstone .
|
-
- HY-176063
-
|
|
TRP Channel
Opioid Receptor
|
Neurological Disease
|
|
TRPV1 antagonist 11 (compound 2ac) is a potent TRPV1 antagonist with an IC50 of 29.3 nM. TRPV1 antagonist 11 is a potent μ-opioid receptor (MOR) agonist with a Ki of 60.3 nM. TRPV1 antagonist 11, a pyrimidine piperazine, exhibits pain relieving effects by antagonizing TRPV1 and stimulating MOR. TRPV1 antagonist 11 shows a potent, dose-dependent anti-nociceptive effect in a Formalin-induced pain model in mice .
|
-
- HY-159896
-
|
|
Protease Activated Receptor (PAR)
|
Cardiovascular Disease
|
|
PAR4 antagonist 8 (Compound 20f) is an effective, orally active, and selective PAR4 antagonist with an IC50 value of 15.32 nM. PAR4 antagonist 8 exhibits favorable pharmacokinetic properties. PAR4 antagonist 8 not only effectively inhibits human platelet aggregation induced by PAR4 agonists (IC50 = 6.39 nM) but also inhibits mouse platelet aggregation. PAR4 antagonist 8 can be used in antithrombotic research .
|
-
- HY-136220
-
|
|
Aryl Hydrocarbon Receptor
|
Cancer
|
|
AHR antagonist 5, a potent and orally active aryl hydrocarbon receptor (AHR) antagonist extracted from patent WO2018195397, example 39, has an IC50 of < 0.5 μΜ. AHR antagonist 5 significantly inhibits tumor growth combined with checkpoint inhibitor anti-PD-1 .
|
-
- HY-145250
-
-
- HY-168141
-
|
|
Androgen Receptor
|
Cancer
|
|
Androgen receptor antagonist 11 (compund N29) is a derivative of the androgen receptor (AR) antagonist M17-B15, and is a selective and orally active AR antagonist (IC50=18 nM). .
|
-
- HY-144372
-
|
|
TRP Channel
|
Neurological Disease
|
|
TRPV1 antagonist 3 (Compound 7q) is a potent TRPV1 antagonist with an IC50 of 2.66 nM against capsaicin. TRPV1 antagonist 3 is mode-selective, oral bioavailable (F = 60%) and CNS-penetrant .
|
-
- HY-149083
-
|
|
Leukotriene Receptor
|
Inflammation/Immunology
|
|
LTB4 antagonist 2, a carboxamide-acid compound, is an antagonist of leukotriene B4 (LTB4) with potentially anti-inflammatory activity. LTB4 antagonist 2 shows good affinity for the LTB4 receptor with IC50 of 439 nM .
|
-
- HY-156663
-
|
|
Calcium Channel
|
Cancer
|
|
Calcium Channel antagonist 2 (Compound 154) is a calcium channel antagonist (IC50=5-20 μM). Calcium Channel antagonist 2 can be used in study of calcium channel-mediated diseases such as pain and diabetes .
|
-
- 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-120653
-
-
- HY-U00359
-
-
- HY-143267
-
-
- HY-107551
-
|
|
Gli
|
Cancer
|
|
GLI antagonist-1 is a potent GLI antagonist with an IC50 value of 1.1 µM. GLI antagonist-1 shows anti-proliferative activity. GLI antagonist-1 decreases the GLI1 mRNA expression. GLI antagonist-1 inhibits colony formation in a dose-dependent manner .
|
-
- HY-112340
-
|
|
Cannabinoid Receptor
|
Metabolic Disease
|
|
CB1 antagonist 4 (compound 8) is a peripheral selective cannabinoid receptor type 1 (CB1) receptor antagonist. CB1 antagonist 4 shows limited penetrance to the brain in order to minimize or prevent CNS adverse reactions, and preserves potential antiobesity effects. CB1 antagonist 4 reduces propensity for psychiatric side effects .
|
-
- HY-149105
-
|
|
Estrogen Receptor/ERR
|
Endocrinology
|
|
FSH receptor antagonist 1 (compound 10) is a potent antagonist of the G(s)-protein-coupled human follicle-stimulating hormone (FSH) receptor. FSH receptor antagonist 1 exhibits an IC50 of 28 nM on a cell line expressing the human FSH receptor. FSH receptor antagonist 1 significantly inhibits follicle growth and ovulation in an ex vivo mouse model .
|
-
- HY-151247
-
|
|
GnRH Receptor
|
Cancer
|
|
GnRH-R antagonist 1 (compound 21a) is an orally safe and membrane-permeable GnRH-R antagonist with high binding affinity (IC50=0.57 nM) and potent in vitro antagonistic activity (IC50=2.18 nM). GnRH-R antagonist 1 can be used in studies of advanced prostate cancer and premature LH peaks preventing .
|
-
- HY-135773
-
|
|
Prostaglandin Receptor
PDK-1
|
Cardiovascular Disease
Inflammation/Immunology
|
|
CRTh2 antagonist 3 is a potent chemoattractant receptor-homologous molecule expressed on Th2 cells (CRTh2) antagonist . CRTh2 antagonist 3 enhances the activity of PDK1 toward a short peptide substrate, with an EC50 of 2 μM and a Kd of 8.4 μM. CRTh2 antagonist 3 has the potential for cardiovascular inflammation .
|
-
- 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-151392
-
|
|
LPL Receptor
|
Neurological Disease
Inflammation/Immunology
|
|
LPA5 antagonist 2 (compound 65) is a high aqueous solubility LPA5 (lysophosphatidic acid receptor 5) antagonist. LPA5 antagonist 2 significantly attenuates nociceptive hypersensitivity and it can be used for the research of inflammatory and neuropathic pains .
|
-
- HY-150205
-
|
|
Succinate Receptor 1
|
Inflammation/Immunology
|
|
Succinate/succinate receptor antagonist 1 (compound 7a) is a succinate/succinate receptor antagonist. Succinate/succinate receptor antagonist 1 blocks succinate signaling in gingival tissue. Succinate/succinate receptor antagonist 1 inhibits the activation of succinate receptor 1 (SucnRl) with an IC50 value of 20 μΜ. Succinate/succinate receptor antagonist 1 can be used for the research of periodontal disease .
|
-
- HY-142923
-
|
|
Androgen Receptor
|
Cancer
|
|
AR antagonist 2 (compound 58) is a potent androgen receptor (AR) inhibitor with an IC50 of 0.95 μM. AR antagonist 2 has the potential for cancer research .
|
-
- HY-168240
-
|
|
iGluR
|
Neurological Disease
|
|
NMDAR antagonist 2 (compound 3I) is a CNS penetrant NMDAR antagonist with the IC50 of 4.42 μM and 214.75 μM for hGluN1/hGluN2A at −60 mV or 40 mV membrane potentials, respectively. NMDAR antagonist 2 can reduce hippocampal damage .
|
-
- HY-151391
-
|
|
Biochemical Assay Reagents
|
Neurological Disease
|
|
LPA5 antagonist 1 (Compound 66) is a potent and selective lysophosphatidic acid receptor 5 (LPA5) antagonist (IC50=32 nM). LPA5 antagonist 1 shows high brain permeability and anti-nociceptive activity. LPA5 antagonist 1 can be used in inflammatory and neuropathic pain research . LPA5 antagonist 1 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-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-114193
-
-
- HY-114194
-
-
- HY-176403
-
-
- HY-125970
-
|
|
Prostaglandin Receptor
|
Endocrinology
|
|
CRTh2 antagonist 2 is selective and potent CRTH2 antagonist extracted from patent US20140148470A1, compound Example 1, has an IC50 of ≤10 nM. CRTh2 antagonist 2 can be used in research of androgenic alopecia .
|
-
- HY-145697
-
|
|
GPR84
|
Inflammation/Immunology
|
|
GPR84 antagonist 2 (compound 33) is a potent, selective, and orally active GPR84 antagonist (IC50=8.95 nM). GPR84 antagonist 2 shows improved potency in the calcium mobilization assay and the ability to inhibit the chemotaxis of neutrophils and macrophages upon GPR84 activation. GPR84 antagonist 2 has the potential for the research of ulcerative colitis .
|
-
- HY-155367
-
|
|
mAChR
|
Neurological Disease
|
|
mAChR antagonist 1 (compound 4a) is a mAChR antagonist with Ki values of 255 nM, 121 nM, 158 nM, and 255 nM for M1, M3, M4, and M5 subtype, respectively .
|
-
- 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-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-151435
-
|
|
CCR
|
Inflammation/Immunology
|
|
CCR6 antagonist 1 is a CCR6 antagonist that inhibits the CCL20/CCR6 axis. CCR6 antagonist 1 can be used in the research of autoimmune-mediated inflammatory diseases, such as inflammatory bowel diseases (IBDs) .
|
-
- HY-163694
-
|
|
Adrenergic Receptor
|
Inflammation/Immunology
|
|
ADRA2A antagonist 1 (compd 4n) is a potent and selective ADRA2A antagonist with an IC50 of 18 nM. ADRA2A antagonist 1 can be used for inflammation and sepsis research .
|
-
- HY-137093
-
-
- HY-112430
-
|
|
TRP Channel
|
Neurological Disease
|
|
TRPM8 antagonist 2 is a potent and selective TRPM8 antagonist, with an IC50 of 0.2 nM, used in the research of neuropathic pain syndromes.
|
-
- HY-112792
-
|
|
CCR
|
Endocrinology
|
|
CCR2 antagonist 1 (compound 15a) is a high-affinity and long-residence-time CCR2 antagonist, with a Ki of 2.4 nM .
|
-
- HY-111494
-
|
|
TRP Channel
|
Neurological Disease
|
|
TRPA1 Antagonist 1 is a methylene phosphate proagent which converts to its active parent agent, a TRPA1 antagonist with an IC50 of 8 nM.
|
-
- HY-W063197
-
|
|
Adenosine Receptor
|
Cancer
|
|
Adenosine receptor antagonist 4 (compound 2) is an adenosine A1 receptor antagonist with a Ki of 101 nM for human A1 receptor .
|
-
- HY-172774
-
-
- HY-U00334
-
|
|
Biochemical Assay Reagents
|
Neurological Disease
|
|
LH secretion antagonist 1 is an antagonist of luteinising hormone secretion, and may be used as an analgesic. LH secretion antagonist 1 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-144064
-
|
|
Adenosine Receptor
|
Cancer
|
|
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 .
|
-
- HY-162762
-
|
|
Protease Activated Receptor (PAR)
|
Cancer
|
|
PAR-2 antagonist 1 (Compound 9a) is a protease-activated receptor 2 (PAR2) antagonist with an IC50 value of 0.9 μM. PAR-2 antagonist 1 can effectively inhibit the proliferation and migration of breast cancer cells .
|
-
- HY-113973
-
|
|
LPL Receptor
|
Cancer
|
|
LPA2 antagonist 2 (H2L 5226501) is a selective LPA2 antagonist with an IC50 of 28.3 nM and a Ki of 21.1 nM. LPA2 antagonist 2 is >480-fold more selective than LPA3 (IC50 of 13.85 μM) .
|
-
- 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-163701
-
|
|
Adenosine Receptor
|
Cancer
|
|
hA2AAR antagonist 1 (compound 4a) is a highly selective hA2AAR antagonist with a Ki of 5 nM. hA2AAR antagonist 1 can be used in the study of immune-oncology .
|
-
- HY-138501
-
|
|
ERK
|
Inflammation/Immunology
|
|
GPR34 receptor antagonist 2 (Compound D2) is a GPR34 receptor antagonist. GPR34 receptor antagonist 2 can be used for immune diseases, inflammatory diseases research .
|
-
- HY-130261
-
|
|
Bcl-2 Family
|
Cancer
|
|
Mcl-1 antagonist 1 is a Mcl-1 protein antagonist extracted from patent WO2019173181, compound 200 .
|
-
- HY-100261
-
-
- HY-126217
-
-
- HY-161899
-
|
|
MCHR1 (GPR24)
|
Others
|
|
MCHR1 antagonist 4 (Compound 2m) is a blood-brain barrier permeable MCHR1 antagonist with Ki values of 0.74 nM and 0.76 nM for hMCHR1 and rMCHR1, respectively. MCHR1 antagonist 4 is also an effective anti-obesity agent .
|
-
- HY-157453
-
|
|
CCR
|
Inflammation/Immunology
|
|
CCR4 antagonist 4 (compound 22) is a selective and potent antagonist of the CC chemokine receptor-4 (CCR4), with an IC50 of 0.02 μM. CCR4 antagonist 4 also blocks MDC-mediated chemotaxis (IC50: 0.007 μM) and Ca 2+ mobilization (IC50: 0.003 μM). CCR4 antagonist 4 can be used for allergic inflammation research .
|
-
- HY-162669
-
|
|
Opioid Receptor
|
Neurological Disease
|
|
Mu opioid receptor antagonist 8 (368) is a μ-opioid receptor antagonist. Mu opioid receptor antagonist 8 (368) significantly inhibits met-enkephalin-induced µOR activation of Gi .
|
-
- HY-15544
-
|
|
CCR
|
Inflammation/Immunology
|
|
CCR1 antagonist 10 (example 1) is a potent and orally active CCR1 antagonist. CCR1 antagonist 10 inhibits 125I-MIP-1α binding to THP-1 cell membranes with an Ki value of 2.3 nM .
|
-
- HY-144784
-
|
|
CXCR
|
Inflammation/Immunology
Cancer
|
|
CXCR2 antagonist 7 (compound 19) is a potent CXCR2 antagonist. CXCR2 antagonist 7 shows potent CXCR2 binding affinity (IC50=0.044 µM) and calcium mobilization (IC50=0.66 µM) [ 1].
|
-
- HY-144781
-
|
|
CXCR
|
Inflammation/Immunology
Cancer
|
|
CXCR2 antagonist 5 (compound 25) is a potent CXCR2 antagonist. CXCR2 antagonist 5 shows potent CXCR2 binding affinity (IC50=0.013 µM) and calcium mobilization (IC50=0.1 µM) [ 1].
|
-
- HY-157495
-
|
|
Prostaglandin Receptor
|
Endocrinology
|
|
EP3 antagonist 6 (compound 5) is a potent, orally and selective EP3 receptor antagonist, with an IC50 of 1.9 nM. EP3 antagonist 6 can inhibits PGE2-induced (HY-101952) uterine contraction in pregnant rats .
|
-
- HY-161646
-
-
- HY-124759
-
|
|
CCR
|
Inflammation/Immunology
|
|
CCR1 antagonist 9 is a potent and selective CCR1 antagonist with an IC50 of 6.8 nM in calcium flux assay .
|
-
- HY-144609
-
|
|
Opioid Receptor
|
Neurological Disease
|
|
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) .
|
-
- HY-139874
-
|
|
CXCR
|
Inflammation/Immunology
Cancer
|
|
CXCR2 antagonist 3 (compound 11h) is a potent antagonist of CXC chemokine receptor 2 (CXCR2). CXCR2 antagonist 3 demonstrates double-digit nanomolar potencies against CXCR2 and significantly inhibited neutrophil infiltration into the air pouch. CXCR2 antagonist 3 reduces the infiltration of neutrophils and MDSCs and enhance the infiltration of CD3 + T lymphocytes into the Pan02 tumor tissues .
|
-
- HY-157189
-
|
|
G2A (GPR132)
|
Metabolic Disease
|
|
GPR132 antagonist 1 (GPR132-B-160, Compound 25) is a GPR132 antagonist with an EC50 value of 0.075 μM. GPR132 antagonist 1 has promote insulin secretion activity with an EC50 value of 0.7 μM .
|
-
- HY-144783
-
|
|
CXCR
|
Inflammation/Immunology
Cancer
|
|
CXCR2 antagonist 6 (compound 35c) is a potent CXCR2 antagonist. CXCR2 antagonist 6 shows potent CXCR2 binding affinity (IC50=0.044 µM) and calcium mobilization (IC50=0.66 µM) [ 1].
|
-
- HY-135830
-
|
|
Aryl Hydrocarbon Receptor
|
Cancer
|
|
AHR antagonist 4 is a 2-heteroaryl-3-oxo-2,3-dihydropyridazine-4-carboxamide compound and a potent aryl hydrocarbon receptor (AHR) antagonist extracted from patent WO2018146010A1, example 293, has an IC50 of 82.2 nM. AHR antagonist 4 has anti-cancer effects .
|
-
- HY-101915
-
-
- HY-116380
-
-
- HY-U00408
-
-
- HY-D2201
-
|
|
Fluorescent Dye
|
Cancer
|
|
Fluorescent ACKR3 antagonist 1(compound 18a) is a atypical chemokine receptor 3 antagonist .
|
-
- HY-158236
-
-
- 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-136220A
-
|
|
Aryl Hydrocarbon Receptor
|
Cancer
|
|
AHR antagonist 5 hemimaleate, a potent and orally active aryl hydrocarbon receptor (AHR) antagonist, has an IC50 of < 0.5 µΜ. AHR antagonist 5 hemimaleate significantly inhibits tumor growth combined with checkpoint inhibitor anti-PD-1 (WO2018195397, example 39) .
|
-
- HY-156667
-
|
|
Histamine Receptor
|
Inflammation/Immunology
|
|
H4R antagonist 3 (Example 18) is a histamine-4 receptor antagonist with an EC50 of ＜10 mM. H4R antagonist 3 can be used for the research of prevention of inflammatory, autoimmune, allergic, and ocular diseases .
|
-
- HY-128063
-
|
|
CXCR
|
Inflammation/Immunology
|
|
CXCR3 antagonist 1 (compound 6c) is a selective and non-cytotoxic CXCR3 antagonist (IC50=0.06 µM). CXCR3 antagonist 1 has potential in researching inflammatory diseases (including inflammatory bowel disease, multiple sclerosis, rheumatoid arthritis, and diabetes) .
|
-
- HY-144139
-
|
|
Estrogen Receptor/ERR
|
Cancer
|
|
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) .
|
-
- HY-172161
-
|
|
CCR
|
Inflammation/Immunology
|
|
CCR6 antagonist 2 (Compound 20c) is the antagonist for CCR6 with a Ki of 1.1 nM. CCR6 antagonist 2 inhibits CCL20-induced calcium ion influx (IC50 = 4.9 nM), inhibits the chemotactic migration of CCR6+ T cells (IC50 = 190 nM) .
|
-
- HY-144202
-
|
|
Estrogen Receptor/ERR
|
Cancer
|
|
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) .
|
-
- HY-147379
-
|
|
Ferroportin
|
Metabolic Disease
|
|
Hepcidin antagonist-1 (example 104) is a potent hepcidin (hepcidine) antagonist with an IC50<50 μM. Hepcidin antagonist-1 can be used for researching iron metabolism disorders, such as anemias .
|
-
- 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-149096
-
|
|
CXCR
|
Others
|
|
CCR7 antagonist 1 (30c) is a dual CXCR2 (IC50 of 11.02 μM) and CCR7 (IC50 of 0.43 μM) antagonist .
|
-
- HY-112792A
-
|
|
CCR
|
Endocrinology
|
|
(1S)-CCR2 antagonist 1 is a left-handed chiral body of CCR2 antagonist 1 (HY-112792). CCR2 antagonist 1 is a high-affinity and long-residence-time CCR2 antagonist, with a Ki of 2.4 nM .
|
-
- HY-130845
-
-
- HY-151266
-
|
|
Androgen Receptor
|
Cancer
|
|
AR antagonist 4 (Compound 67-b) is an orally active androgen receptor (AR) antagonist with an IC50 of 246.6 nM against wt-AR, and is also an AR degrader with a DC50 of 2.84 μM .
|
-
- HY-162787
-
|
|
Adenosine Receptor
|
Cancer
|
|
Adenosine receptor antagonist 5 (Compound 39) is a selective antagonist for human adenosine A3 receptor (hA3R) with Ki of 12 nM. Adenosine receptor antagonist 5 inhibits IB-MECA (HY-13591)-induced cAMP accumulation in NCI-H1792 cell, inhibits the proliferation of cancer cell LK-2 and NCI-H1792. Adenosine receptor antagonist 5 exhibits a fast metabolic rate in human liver microsomes .
|
-
- HY-147385
-
|
|
CCR
|
Inflammation/Immunology
|
|
CCR4 antagonist 3 is a potent chemokine receptor 4 (CCR4) antagonist with an IC50 value of 1.7 μM for [ 125I]TARC (thymus and activation regulated chemokine). CCR4 antagonist 3 inhibits binding of radiolabeled TARC and macrophage-derived chemokine (MDC) to CCR4 receptors on the surface of CEM cells. CCR4 antagonist 3 also inhibits the in vitro migration of CEM cells mediated by TARC (IC50 = 6.4 μM) .
|
-
- 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-168443
-
|
|
5-HT Receptor
Apoptosis
|
Cancer
|
|
HTR2A antagonist 1 (Compound 15f) is a HTR2A antagonist, with an IC50 of 42.79 nM. HTR2A antagonist 1 induces sub-G1 cell cycle arrest and apoptosis in colorectal cancer cells via the activation of p53/p21/caspase 3 signaling. HTR2A antagonist 1 has good liver microsomal stability. HTR2A antagonist 1 can be used for the research of colorectal cancer .
|
-
- HY-162998
-
-
- HY-18076
-
-
- HY-100170
-
-
- HY-U00397
-
-
- HY-130845A
-
-
- HY-135831
-
|
|
Aryl Hydrocarbon Receptor
|
Cancer
|
|
AHR antagonist 2 is a potent aryl hydrocarbon receptor (AHR) antagonist, extracted from patent WO2019101641A1, compound example 1, with IC50s of 0.885 and 2.03 nM for human and mouse AhR .
|
-
- HY-15645
-
-
- 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-155737
-
|
|
Estrogen Receptor/ERR
|
Cardiovascular Disease
|
|
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 .
|
-
- HY-155739
-
|
|
Estrogen Receptor/ERR
|
Cardiovascular Disease
|
|
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 .
|
-
- HY-155738
-
|
|
Estrogen Receptor/ERR
|
Cardiovascular Disease
|
|
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 .
|
-
- HY-144137
-
|
|
Estrogen Receptor/ERR
|
Cancer
|
|
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) .
|
-
- HY-143563
-
|
|
NOD-like Receptor (NLR)
|
Cancer
|
|
NLRP3 antagonist 1 is a potent antagonist of NLRP3. NLRP3 is mainly expressed in macrophages and neutrophils and is involved in the body's intrinsic immunity against pathogenic infections and stress injury. NLRP3 antagonist 1 has the potential for the research of cancer disease (extracted from patent WO2021114691A1, compound 3) .
|
-
- HY-161925
-
|
|
TGF-β Receptor
|
Neurological Disease
Inflammation/Immunology
|
|
sTGFBR3 antagonist 1 (Compound p24) is an antagonist for soluble transforming growth factor beta receptor 3 (sTGFBR3), thus activates TGF-β signaling pathway, and inhibits IκBα/NF-κB signaling pathway. sTGFBR3 antagonist 1 inhibits NO-release in LPS (HY-D1056) -induced BV2 cells with an IC50 of 0.52 μM. sTGFBR3 antagonist 1 exhibits anti-inflammatory and neuroprotective activities with blood brain barrier (BBB) permeability. sTGFBR3 antagonist 1 can be used in Alzheimer’s Disease research .
|
-
- HY-151387
-
|
|
Adenosine Receptor
|
Neurological Disease
|
|
A2AAR antagonist 1 (compound 21a) is an A2AAR (adenosine A2A receptor) antagonist with a Ki value of 20 nM. A2AAR antagonist 1 shows high ligand efficiency, and it can be used for the research of neurodegenerative diseases .
|
-
- 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-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-159632
-
-
- HY-146372
-
|
|
CXCR
|
Cancer
|
|
CXCR4 antagonist 5 (compound 23) is a highly potent CXCR4 antagonist with an IC50 value of 8.8 nM. CXCR4 antagonist 5 can inhibit CXCL12-induced cytosolic calcium increase (IC50 = 0.02 nM) and inhibits CXCR4/CXLC12-mediated chemotaxis. CXCR4 antagonist 5 has good physicochemical properties and in vitro safety profiles, inhibiting CYP isozymes and hERG marginally or moderately .
|
-
- HY-144608
-
|
|
Opioid Receptor
|
Neurological Disease
|
|
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) .
|
-
- HY-156460
-
|
|
CCR
|
Inflammation/Immunology
|
|
CMKLR1 antagonist 1 (compound S-26d) is a potent and orally active chemokine-like receptor 1 (CMKLR1) antagonist, with a pIC50 value of 7.44 in hCMKLR1-transfected CHO cells. CMKLR1 antagonist 1 can be used for psoriasis and metabolic diseases research .
|
-
- HY-161401
-
|
|
Protease Activated Receptor (PAR)
|
Cardiovascular Disease
|
|
PAR4 antagonist 2 (Compound 31) is a protease activated receptor 4 (PAR4) antagonist, with IC50 values of 95 nM and 367 nM for human PAR4 and mouse PAR4. PAR4 antagonist 2 is active against PAR4 activation by the native protease thrombin cleavage but not the synthetic PAR4 agonist peptide AYPGKF .
|
-
- HY-144204
-
|
|
Estrogen Receptor/ERR
|
Endocrinology
Cancer
|
|
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) .
|
-
- HY-144206
-
|
|
Estrogen Receptor/ERR
|
Endocrinology
|
|
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) .
|
-
- HY-134555
-
|
|
Adenosine Receptor
|
Neurological Disease
|
|
A3AR antagonist 4 (Compd 1) is an A3AR antagonist, with Ki values of 30.8 nM (hA3) and 203 nM (hA1), repectively. A3AR antagonist 4 (Compd 1) can be used for the study of cerebral ischemia .
|
-
- HY-146457
-
|
|
Adenosine Receptor
|
Inflammation/Immunology
|
|
A3AR antagonist 1 (compound 17) is a potent and selective human A3 adenosine receptor (AR) antagonist, with an Ki of 4.63 nM. A3AR antagonist 1 shows no affinity for the rat A3 AR even at high concentrations .
|
-
- HY-115745
-
|
|
Calmodulin
|
Cardiovascular Disease
|
|
Calmodulin antagonist-1 (A-5) is a calmodulin (CaM) antagonist. Calmodulin antagonist-1 inhibits calmodulin-activated Ca 2+-phosphodiesterase (PDE) (IC50=66 μM). Calmodulin antagonist-1 also inhibits trypsin-treated Ca 2+-PDE (IC50=560 μM) in a competitive fashion with respect to cyclic GMP .
|
-
- HY-152581
-
|
|
Cannabinoid Receptor
|
Inflammation/Immunology
|
|
CB2R antagonist 3 is a selective antagonist of cannabinoid type 2 receptor (CB2R). CB2R antagonist 3 has high affinity for human CB2R and specific selectivity for CB1R. CB2R antagonist 3 can be combined with CB65 (HY-110047), the activator of CB2R. CB2R antagonist 3 effectively up-regulates the expression of anti-inflammatory cytokines and down-regulates the expression of pro-inflammatory cytokines .
|
-
- HY-U00368
-
-
- HY-12099
-
-
- HY-118198
-
-
- 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-100274
-
-
- HY-114097A
-
|
|
CCR
|
Inflammation/Immunology
|
|
CCR1 antagonist 11 hydrochloride (A1B1) is an orally active CCR1 antagonist with the IC50 values of 0.03 μM, 0.58 μM and 0.32 μM for hCCR1, mCCR1 and rCCR1, respectively. CCR1 antagonist 11 hydrochloride can be used in the study of rheumatoid arthritis and other related inflammatory diseases .
|
-
- HY-U00353
-
|
|
MCHR1 (GPR24)
|
Metabolic Disease
Endocrinology
|
|
MCHR1 antagonist 1 is a selective antagonist of melanin concentrating hormone-1 (MCH1) receptor, with a Kb of 1 nM and a Ki of 4 nM at human MCH1, and may be used to reduce the body mass.
|
-
- HY-110091
-
|
|
TRP Channel
|
Neurological Disease
|
|
TRPV1 antagonist 9 (compound 13c) is an orally active transient receptor potential vanilloid 1 (TRPV1) channel antagonist. TRPV1 antagonist 9 blocks Ca 2+ uptake by CHO cells expressing TRPV1 receptors with IC50 values are 0.6 and 0.8 nM for Capsaicin (HY-10448) and acid-induced Ca 2+ uptake, respectively. TRPV1 antagonist 9 blocks Capsaicin (HY-10448)-induced flinch response and causes hyperthermia in rats .
|
-
- HY-124100
-
-
- HY-144699
-
|
|
Estrogen Receptor/ERR
|
Cancer
|
|
ERRα antagonist-2 (Compound 11) is a potential ERRα (estrogen related receptor α) inverse agonist with an IC50 of 0.80 μM. ERRα antagonist-2 suppresses the migration and invasion of the ER-negative MDA-MB-231 cell line. ERRα antagonist-2 inhibits breast cancer growth in vivo .
|
-
- HY-145919
-
-
- HY-147506
-
|
|
NOD-like Receptor (NLR)
|
Inflammation/Immunology
|
|
NOD2 antagonist 1 (compound 32) is a potent and selective NOD2 antagonist with an IC50 of 5.23 μM. NOD2 antagonist 1 inhibits Muramyl dipeptide (MDP)-induced IL-8 secretion in THP-1 cells and inhibits MDP-induced IL-6, IL-10, TNF-α release in PBMCs .
|
-
- HY-149336
-
-
- HY-164621
-
|
|
Adenosine Receptor
|
Others
|
|
A3AR antagonist 5 (Compound 16) is a selective antagonist for human adenosine A3 receptor with an affinity pC of 4.542 μM .
|
-
- HY-146456
-
|
|
Adenosine Receptor
|
Neurological Disease
|
|
A1AR antagonist 3 (compound 13) is a selective adenosine 1 (A1) receptor antagonist with Kis of 9.69 nM and 0.529 nM for human A1 and rat A1, respectively. A1AR antagonist 3 can be used for researching neurological diseases .
|
-
- HY-158262
-
|
|
Bradykinin Receptor
|
Neurological Disease
|
|
Bradykinin B1 receptor antagonist 1 (compound 6B) is a potent and cross the blood-brain barrier bradykinin B1 antagonist. Bradykinin B1 receptor antagonist 1 has the potential for the research of pain .
|
-
- HY-144607
-
|
|
Opioid Receptor
|
Neurological Disease
|
|
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) .
|
-
- HY-114191B
-
|
|
Somatostatin Receptor
|
Metabolic Disease
Endocrinology
|
|
SSTR5 antagonist 2 hydrochloride is a highly potent, oral active and selective somatostatin (receptor) subtype 5 (SSTR5) antagonist and has potential for the research of type 2 diabetes mellitus (T2DM) .
|
-
- 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-121094
-
|
|
Estrogen Receptor/ERR
|
Cancer
|
|
Androgen receptor allosteric antagonist 1(compound D36)is a a llosteric, competitive androgen receptor (AR) antagonist with the Ki of 9 μM. Androgen receptor allosteric antagonist 1 inhibits R1881-mediated transcription and proliferation and can be used for study of prostate cancer .
|
-
- HY-144610
-
|
|
Opioid Receptor
|
Neurological Disease
|
|
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) .
|
-
- HY-157189A
-
|
|
G2A (GPR132)
|
Metabolic Disease
|
|
GPR132 antagonist 1 dihydrocholide (GPR132-B-160, Compound 25) is a GPR132 antagonist with an EC50 value of 0.075 μM. GPR132 antagonist 1 dihydrocholide has promote insulin secretion activity with an EC50 value of 0.7 μM .
|
-
- HY-101913
-
-
- HY-163091
-
-
- HY-160173
-
|
|
LPL Receptor
|
Others
|
|
LPA receptor antagonist-1 (example 52) is an antagonist of lysophosphatidic acid (LPA) receptor. LPA receptor antagonist-1 can be used for kinds of studies .
|
-
- HY-125836
-
|
|
CCR
|
Endocrinology
Cancer
|
|
CCR4 antagonist 2 (Compound 31) is a novel potent, orally bioavailable small molecule antagonists of CC chemokine receptor 4 (CCR4) that inhibits Treg trafficking into the Tumor Microenvironment without suppressing the number of Treg in healthy tissues.
CCR4 antagonist 2 (Compound 31) exhibits IC50 values of Ca 2+flux and (chemotaxis) CTX are 40 nM and 70 nM, respectively .
|
-
- HY-146410
-
|
|
Angiotensin Receptor
|
Others
|
|
AT2R antagonist 1 (compound 21) is a potent and high selective AT2R (angiotensin II AT2 receptor) ligand. AT2R antagonist 1 exhibits a fair AT2R affinity, with a Ki of 29 nM. AT2R antagonist 1 also inhibits common agent-metabolizing CYP enzymes. AT2R antagonist 1 shows high stability in human, rat and mouse liver microsomes .
|
-
- HY-141845
-
|
|
LPL Receptor
|
Others
|
|
S1P2 antagonist 1 is an orally bioavailable S1P2 antagonist against fibrotic diseases.
|
-
- HY-149645
-
|
|
Cannabinoid Receptor
|
Others
|
|
CB2 receptor antagonist 2 (compound 39) is a potent antagonist of CB2 with an IC50 value of 0.33 μM. CB2 receptor antagonist 2 has strong interactions with L17, W6.48, V6.51, and C7.42 .
|
-
- HY-102037
-
-
- HY-146220
-
-
- HY-172624
-
|
|
Ligands for Target Protein for PROTAC
|
Cancer
|
|
AR antagonist 14 is is a PROTAC target protein ligand (Ligands for Target Protein for PROTAC). AR antagonist 14 can be combined with VH 101-amide-piperidine-Pip-alkyne (HY-172625) to synthesize PROTAC degraders (ARD-69 (HY-114402)) .
|
-
- HY-U00365
-
-
- HY-U00322
-
|
|
5-HT Receptor
|
Neurological Disease
|
|
5-HT3 antagonist 3 (Compound 15b) is a high-affinity 5-HT3 receptor antagonist. 5-HT3 antagonist 3 binds to 5-HT3 receptors in rat brain cortical membranes with Ki of 0.25 nM .
|
-
- HY-148259
-
|
|
Orphan Receptor
|
Cancer
|
|
SF-1 antagonist-1 (compound 11) is a antagonist of steroidogenic factor 1 (SF-1). SF-1 antagonist-1 affects SF-1 transcriptional activity with an EC50 value of ＜200 nM. SF-1 antagonist-1 inhibits the proliferation of Rat Leydig tumor cells. SF-1 antagonist-1 can be used for the research of cancer .
|
-
- HY-163645
-
|
|
P2Y Receptor
|
Cardiovascular Disease
|
|
P2Y12 antagonist 1 (compound 26) is a P2Y12 receptor antagonist with a Ki of 3.13 μM. P2Y12 antagonist 1 can be used to inhibit platelet aggregation and is a potential antithrombotic agent .
|
-
- HY-147132
-
|
|
iGluR
|
Neurological Disease
|
|
GluR6 antagonist-1 is a benzothiophene derivative, acting as a GluR6 antagonist. GluR6 antagonist-1 can be used for researching acute and chronic neurological disorders .
|
-
- HY-163378
-
|
|
Complement System
|
Inflammation/Immunology
|
|
C5aR1 antagonist 1 (Compound 7e) is an orally active C5a receptor 1 (C5aR1) antagonist. C5aR1 antagonist 1 is active in DISCO and migration assays, with IC50 values of 38 nM and 17 nM, respectively. C5aR1 antagonist 1 can be used for the research of acute and chronic inflammatory diseases .
|
-
- HY-146383
-
|
|
Histamine Receptor
Cholinesterase (ChE)
Monoamine Oxidase
|
Neurological Disease
|
|
H3R antagonist 2 (Compound 23) is a multitarget histamine H3 receptor (H3R) antagonist with a Ki of 170 nM for hH3R . H3R antagonist 2 shows inhibitory effects with IC50 values of 180, 880 and 775 nM for acetylcholinesterase, butyrylcholinesterase and human monoamine oxidase B (hMAO B), respectively. H3R antagonist 2 shows favorable anti-neuropathic pain and memory-enhancing effects. H3R can across BBB .
|
-
- HY-13232
-
|
|
Itk
|
Inflammation/Immunology
|
|
ITK antagonist (compound 10 n) is a potent, orally active and selective ITK (Interleukin-2 inducible T-cell kinase) antagonist (IC50=1 and 20 nM in different assays). ITK antagonist inhibits insulin receptor kinase (IRK) with an IC50 of 160 nM .
|
-
- HY-114191
-
|
|
Somatostatin Receptor
|
Metabolic Disease
Endocrinology
|
|
SSTR5 antagonist 2 (compound 10) is a highly potent, oral active and selective somatostatin (receptor) subtype 5 (SSTR5) antagonist and has potential for the research of treat type 2 diabetes mellitus (T2DM) .
|
-
- HY-156017
-
|
|
5-HT Receptor
|
Cardiovascular Disease
Neurological Disease
|
|
5-HT6R antagonist 1 (Comopund 8) is a 5-HT6R antagonist (Ki: 5 nM). 5-HT6R antagonist 1 inhibits platelet aggregation. 5-HT6R antagonist 1 has excellent metabolic stability. 5-HT6R antagonist 1 reverses MK-801 (HY-15084B)-induced memory impairments in rats. 5-HT6R antagonist 1 can be used for Alzheimer's disease (AD) research .
|
-
- HY-146808
-
|
|
Galectin
|
Cancer
|
|
Galectin-3 antagonist 1 (compound 15) is a potent and selective Galectin-3 (Gal-3) antagonist with Kd value of 5.3 μM. Meanwhile, Galectin-3 antagonist 1 binds to various Galectin with Kd values of 250 μM (Gal-4N), 18 μM (Gal-4C), 450 μM (Gal-8C), respectively .
|
-
- HY-158318
-
|
|
DNA/RNA Synthesis
|
Cancer
|
|
NUDT5/14 antagonist 1 (Compound 9) is a selective, dual antagonist for nucleotide diphosphate kinase NUDT5 and NUDT14, with IC50 of 0.27 and 0.16 μM, respectively. NUDT5/14 antagonist 1 binds to Bruton’s tyrosine kinase (BTK) with an IC50 of 0.377 μM .
|
-
- HY-111501
-
|
|
Histamine Receptor
|
Inflammation/Immunology
Endocrinology
|
|
H4R antagonist 1 is a potent and highly selective histamine H4 receptor (H4R) antagonist with an IC50 of 27 nM. H4R antagonist 1 does not show any noticeable binding affinity to other subtypes of histamine receptors, H1R, H2R, and H3R .
|
-
- HY-50159
-
-
- HY-10036
-
-
- HY-50158
-
-
- HY-145959
-
|
|
iGluR
|
Neurological Disease
|
|
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 .
|
-
- 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-136960
-
|
|
Adrenergic Receptor
|
Others
|
|
β2AR antagonist 1 (Cmpd-15PA) is an antagonist of β2 adrenergic receptor (β2AR). β2AR antagonist 1 binds to the intracellular surface of the β2AR .
|
-
- 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-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-144200
-
|
|
CCR
|
Neurological Disease
Cancer
|
|
CCR8 antagonist 2 is a potent antagonist of CCR8. CCR8 (C-C Motif Chemokine Receptor 8) is predominantly expressed on Treg cells and Th2 cells, but not on Th1 cells. CCR8 antagonist 2 inhibits CCR8 activity, which may be used in the research of diseases mediated by CCR8, such as cancer, and/or neuropathic pain (extracted from patent WO2022000443A1, compound 220) .
|
-
- HY-136905
-
|
|
iGluR
|
Others
|
|
AMPA receptor antagonist-2 (example 23) is an AMPA receptor antagonist .
|
-
- HY-155316
-
-
- HY-135270
-
-
- 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-173063
-
|
|
Toll-like Receptor (TLR)
NF-κB
MyD88
|
Inflammation/Immunology
|
|
TLR8 antagonist-1 (Compound 10) is a selective TLR8 antagonist. TLR8 antagonist-1 can inhibit TLR8-mediated inflammation and signaling pathways, reduce the recruitment of MyD88, and inhibit the NF-κB and IRF pathways. TLR8 antagonist-1 has anti-inflammatory activity .
|
-
- HY-116890
-
|
|
Prostaglandin Receptor
|
Inflammation/Immunology
|
|
CRTh2 antagonist 4 (compound 58) is an inhibitor (IC50: 212 nM) of TH2 lymphocyte (CRTH2 or DP2) receptor with high binding affinity (Ki= 37 nM). CRTh2 antagonist 4 can be used in the study of severe allergic diseases .
|
-
- HY-145195
-
-
- HY-172409
-
|
|
Cannabinoid Receptor
p38 MAPK
NF-κB
|
Inflammation/Immunology
|
|
CB1R antagonist 2 (Compound 11g) is the antagonist for cannabinoid receptor 1 (CB1R), that inhibits MAPK/NF-κB signaling pathway and exhibits anti-inflammatory activity. CB1R antagonist 2 inhibits LPS (HY-D1056)-induced IL-6, IL-1β and TNF-α expressions in RAW264.7. CB1R antagonist 2 ameliorates OVA-induced allergic rhinitis in mouse models .
|
-
- HY-144764
-
|
|
5-HT Receptor
|
Neurological Disease
|
|
5-HT1A antagonist 1 (compound 6f) is a potent and selective antagonist of 5-HT1A receptor, with a Ki of 35 nM. 5-HT1A antagonist 1 can be used for the research of CNS diseases .
|
-
- HY-145192
-
-
- HY-145193
-
-
- HY-145191
-
-
- HY-143568
-
-
- HY-168784
-
|
|
Leukotriene Receptor
|
Metabolic Disease
Inflammation/Immunology
|
|
LTD4 antagonist 2 (compound 6) is a leukotriene D4 (LTD4) antagonist with an IC50 of 2.8 μM against cysteinyl leukotriene 1 receptor (CysLT1R). LTD4 antagonist 2 is also a G protein-coupled bile acid receptor 1 (GPBAR1) agonist and can be utilized in research related to colitis, metabolic syndromes, and other GPBAR1/CysLT1R-related diseases .
|
-
- HY-146436
-
|
|
Angiotensin Receptor
|
Others
|
|
AT1R antagonist 2 (compound 6) is a potent AT1R selective ligand. AT1R antagonist 2 exhibits a fair AT1R affinity, with a Ki of 26 nM .
|
-
- 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-U00286
-
|
|
5-HT Receptor
|
Cardiovascular Disease
|
|
5-HT2A antagonist 1 is a 5-HT2A antagonist extracted from patent US5728835A and JP 1007727. 5-HT2A antagonist 1 may be useful in treatment of gastrointestinal disorders circulatory disorders.
|
-
- HY-148492
-
-
- HY-162394
-
|
|
Vasopressin Receptor
|
Metabolic Disease
|
|
Vasopressin V2 receptor antagonist 2 (Compound 33) is an antagonist of the arginine vasopressin V2 receptor (V2R) with a Ki value of 6.2 nM. Vasopressin V2 receptor antagonist 2 can effectively reduce cAMP levels, thereby inhibiting the growth of renal cysts[1].
|
-
- HY-147106
-
-
- HY-144285
-
|
|
CXCR
HIV
|
Inflammation/Immunology
|
|
CXCR4 antagonist 4 is a potent, orally active CXCR4 antagonist (IC50=24 nM) with diminished CYP 2D6 activity, improved PAMPA permeability, potent inhibition of human immunodeficiency virus entry (IC50=7 nM) .
|
-
- HY-146431
-
|
|
Angiotensin Receptor
|
Others
|
|
AT1R antagonist 1 (compound 10) is a potent AT1R selective ligand. AT1R antagonist 1 exhibits a fair AT1R affinity, with a Ki of 8.5 nM .
|
-
- 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-112659
-
|
|
MicroRNA
|
Neurological Disease
Cancer
|
|
Lin28-let-7 antagonist 1 (compound 1632) is a potent antagonist of Lin28/pre-let-7 interaction. Lin28-let-7 antagonist 1 inhibits Lin28A binding to pre-let-7a-2, with an IC50 of 8 μM. Lin28-let-7 antagonist 1 inhibits proliferation in human cancer cells .
|
-
- 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-163379
-
|
|
Complement System
|
Inflammation/Immunology
|
|
C5aR1 antagonist 2 (Compound 6a) is an orally active C5a receptor 1 (C5aR1) antagonist that shows efficacy in inhibiting the C5a-induced neutrophil count increase. C5aR1 antagonist 2 is potent in the DISCO and migration assays, with IC50 values of 21 and 3 nM, respectively. C5aR1 antagonist 2 can be used for the research of acute and chronic inflammatory diseases .
|
-
- HY-145194
-
-
- 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-162661
-
|
|
P2Y Receptor
|
Inflammation/Immunology
|
|
P2Y14R antagonist 2 (compound 39) is a potent, selective and orally active P2Y14R antagonist with an IC50 value of 0.40 nM. P2Y14R antagonist 2 shows anti-inflammatory activity. P2Y14R antagonist 2 has the potential for the research of colitis .
|
-
- HY-161273
-
|
|
TRP Channel
|
Neurological Disease
|
|
TRPV1 antagonist 6 (compound 51) is a mode-selective antagonist for transient receptor potential vanilloid member 1 (TRPV1), which shows antagonism with IC50 of 2.85 nM to capsaicin activation and 28.48 % inhibition against proton activation at a 3 µM concentration .
|
-
- HY-162682
-
-
- HY-144672
-
-
- HY-145124
-
|
|
TRP Channel
|
Others
|
|
TRPM8 antagonist 3 is a novel TRPM8 blocker with an IC50 value of 11 nM.
|
-
- HY-128103
-
|
|
GCGR
Adenylate Cyclase
|
Metabolic Disease
|
|
Glucagon receptor antagonist-7 (Compound 1) is an antagonist for hGCGR, that inhibits the binding of 125I-labeled glucagon to the human glucagon receptor (hGCGR) with IC50 of 181 nM. Glucagon receptor antagonist-7 activates glucagon-stimulated adenylyl cyclase with a KDB of 81 nM in CHO cell. Glucagon receptor antagonist-7 inhibits glucagon-mediated glycogenolysis in human hepatocytes, and lowers blood glucose levels .
|
-
- HY-120636
-
|
|
P2Y Receptor
|
Cardiovascular Disease
|
|
P2Y1 antagonist 1 (compound 10q) is a potent antagonist of P2Y1, with the IC50s of 1.1 nM and 0.24 μM in FLIPR assay and hPA assay, respectively. P2Y1 antagonist 1 plays an important role in antiplatelet research .
|
-
- HY-153460
-
|
|
Toll-like Receptor (TLR)
|
Inflammation/Immunology
|
|
TLR7/8/9 antagonist 2 is an orally active TLR7/8/9 antagonist. TLR7/8/9 antagonist 2 has inhibitory activities for HEK/hTLR7, HEK/hTLR8 and HEK/hTLR9 with IC50 values of 0.011 μM, 0.029 μM and 0,052 μM, respectively.TLR7/8/9 antagonist 2 has high bioavailability in vivo.TLR7/8/9 antagonist 2 can be used for the research of auto-inflammatory diseases such as systemic lupus erythematosus or lupus nephritis .
|
-
- HY-170447
-
|
|
NOD-like Receptor (NLR)
|
Inflammation/Immunology
|
|
NOD1 antagonist-2 (compound 66) is an orally active selective antagonist of both human and mouse NOD1. NOD1 antagonist-2 (compound 66) antagonizes NOD1-induced NF-κB and MAPK pathways .
|
-
- HY-133123
-
|
|
Prostaglandin Receptor
|
Inflammation/Immunology
Cancer
|
|
EP4 receptor antagonist 1 is a highly potent and selective competitive prostanoid EP4 receptor antagonist for cancer immunotherapy. EP4 receptor antagonist 1 inhibits human and mouse EP4 receptor with IC50s of 6.1 nM and 16.2 nM, respectively. IC50s >10 μM for human EP1, EP2,and EP3 receptors .
|
-
- HY-159090
-
|
|
Calcium Channel
Angiotensin Receptor
|
Cardiovascular Disease
|
|
AT1R antagonist 3 (Compound 1) is an antagonist for angiotensin II type 1 receptor (AT1R) and an inhibitor for calcium channel type-L CaV1.2 (IC50=0.57 μM). AT1R antagonist 3 exhibits vasodilation efficacy in solated rat aorta (10 μM, 88.7%) and antihypertensive efficacy in rat models .
|
-
- HY-145886
-
|
|
Toll-like Receptor (TLR)
|
Infection
Inflammation/Immunology
Cancer
|
|
TLR7/8 Antagonist 1 (Compound 16c) is the potent antagonist of TLR7/8 with IC50s of 3.91 and 2.19 μM, respectively. TLR7/8 Antagonist 1 is an imidazoquinoline derivative compound. Toll-like receptors (TLRs) 7 and 8 are key targets in the development of immunomodulatory drugs for researching infectious disease, cancer, and autoimmune disorders .
|
-
- HY-161405
-
|
|
Neuropeptide FF Receptor
Opioid Receptor
|
Neurological Disease
|
|
NPFF1-R antagonist 1 (compound 8b), a piperidine analogue, is a potent neuropeptide FF (NPFF) receptor antagonist. NPFF1-R antagonist 1 is 15-fold selective for the NPFF1-R subtype, with Ki values of 211 nM and 3270 nM for NPFF1-R and NPFF2-R, respectively .
|
-
- HY-U00321
-
-
- HY-139677
-
-
- HY-128781
-
|
|
GCGR
|
Metabolic Disease
|
|
Glucagon receptor antagonist-5 (compound 13K) is a potent and orally bioavailable indazole-based glucagon receptor antagonist (Ki=32 nM). Glucagon receptor antagonist-5 has potential for the treatment of type 2 diabetes mellitus (T2DM) .
|
-
- HY-145468
-
|
|
GPR52
|
Neurological Disease
|
|
GPR52 antagonist-1 (Compound 43) is a GPR52 antagonist with an IC50 of 0.63 μM. GPR52 antagonist-1 reduces mHTT (mutant huntingtin protein) levels by targeting GPR52 and promotes survival of mouse primary striatal neurons .
|
-
- HY-162759
-
|
|
Sigma Receptor
|
Neurological Disease
|
|
Sigma-1 receptor antagonist 6 (Compound 12) is an antagonist of the Sigma-1 receptor (σ1R). Sigma-1 receptor antagonist 6 exerts a robust antiallodynic effect by antagonizing σ1R. Sigma-1 receptor antagonist 6 can be used in neuropathic pain animal models to alleviate mechanical allodynia induced by paclitaxel (HY-B0015) .
|
-
- HY-170950
-
|
|
P2Y Receptor
NOD-like Receptor (NLR)
|
Inflammation/Immunology
|
|
P2Y14 antagonist 1 (compound 45) is a high selective and orally active P2Y14R antagonist with an IC50 of 0.70 nM. P2Y14R antagonist 1 demonstrates significant anti-inflammatory efficacy, effectively mitigating the pulmonary infiltration of immune cells and inflammatory response through suppressing the NLRP3 signaling pathway. P2Y14R antagonist 1 has the potential for the research of acute lung injury .
|
-
- HY-P2268
-
|
|
Amyloid-β
|
Inflammation/Immunology
Cancer
|
|
RAGE antagonist peptide is an advanced glycation end products (RAGE) antagonist. RAGE antagonist peptide prevents RAGE from binding with several of its most important ligands, including HMGB-1, S100P, and S100A4. RAGE antagonist peptide (RAP) possesses anti-tumor and anti-inflammatory activities .
|
-
- HY-115974
-
|
|
Bombesin Receptor
|
Cancer
|
|
GRPR antagonist-1 is a potent gastrin releasing peptide receptor (GRPR) antagonist, having the cytotoxicity against certain cancer cells (IC50 of 4.97, 4.36 and 3.40 μM in PC3, Pan02 and HGC-27 cells, respectively). GRPR antagonist-1 inhibits HGC-27 cell viability by decreasing the Bcl-2 level and increasing the Bax level, causing apoptosis, with anticancer activity .
|
-
- HY-145893
-
-
- HY-145892
-
-
- HY-160664
-
|
|
Prostaglandin Receptor
|
Cardiovascular Disease
|
|
TP receptor antagonist-2 (example 7n) is a thromboxane A2 receptor (TP receptor) antagonist, with IC50 values of 5.64 and 5.27 μM for TPα and TPβ, respectively. TP receptor antagonist-2 inhibits platelet aggregation .
|
-
- HY-114191A
-
|
|
Somatostatin Receptor
|
Metabolic Disease
Endocrinology
|
|
SSTR5 Antagonist 1 (compound 10) is a highly potent, oral active and selective somatostatin (receptor) subtype 5 (SSTR5) antagonist and has potential for the research of treat type 2 diabetes mellitus (T2DM) .
|
-
- HY-101116
-
|
|
GCGR
|
Metabolic Disease
|
|
GLP-1R Antagonist 1 (compound 5d) is an orally active, CNS penetrant and non-competitive antagonist of glucagon-like peptide 1 receptor (GLP-1R), with an IC50 of 650 nM .
|
-
- HY-162011
-
|
|
EBI2/GPR183
|
Inflammation/Immunology
|
|
GPR183 antagonist-2 (compound 32) is a selective GPR183 antagonist with good water solubility and excellent pharmacokinetic properties. GPR183 antagonist-2 significantly reduces paw and joint swelling and gene expression of pro-inflammatory cytokines (MCP-1, MMPs, and VEGF) in a collagen-induced arthritis (CIA) mouse model in a dose-dependent manner. GPR183 antagonist-2 can be used in the study of autoimmune diseases .
|
-
- HY-170382
-
|
|
Estrogen Receptor/ERR
Apoptosis
|
Cancer
|
|
ER covalent antagonist-1 (Compound 39D) is the antagonist for estrogen receptor α (ERα). ER covalent antagonist-1 inhibits the proliferation of ERα-positive cell MCF-7 with an IC50 of 0.98 μM, arrests the cell cycle at G0/G1 phase, and induces apoptosis. ER covalent antagonist-1 exhibits antitumor efficacy in mouse model .
|
-
- HY-157939
-
|
|
EBI2/GPR183
|
Inflammation/Immunology
|
|
GPR183 antagonist-3 (compound 33) is an oral active GPR183 antagonist with the IC50 of 8.7 μM. GPR183 antagonist-3 displays strong in vitro antimigration and anti-inflammatory activity in monocytes, and improves the pathological symptoms of DSS-induced experimental colitis .
|
-
- HY-160615
-
-
- HY-101695
-
-
- 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-169941
-
|
|
Estrogen Receptor/ERR
|
Metabolic Disease
Cancer
|
|
ERα/ERβ antagonist-1 (Compound 10) is partial antagonists of ERα and ERβ. ERα/ERβ antagonist-1 reduces ERα and ERβ activity in a dose-dependent manner in HepG2 liver cells .
|
-
- HY-123695
-
-
- HY-116649
-
-
- HY-P4745
-
|
|
MCHR1 (GPR24)
|
Metabolic Disease
|
|
hMCH-1R antagonist 1 (Compound 30) is an effective and selective antagonist of human melanin-concentrating hormone receptor 1 (hMCHR1) with an KB value of 3.6 nM. HMCH-1R antagonist 1 can bind to hMCHR1 and hMCHR2 with IC50 values of 65 nM and 49 nM, respectively. HMCH-1R antagonistist 1 can be used for metabolic research .
|
-
- HY-147557
-
|
PAC1R antagonist 1
|
PACAP Receptor
|
Neurological Disease
|
|
PA-915 (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-153553
-
-
- HY-176446
-
|
|
Mas-related G-protein-coupled Receptor (MRGPR)
|
Inflammation/Immunology
|
|
Mrgx2 antagonist-3 (Compound B-40) is a highly selective antagonist of MrgX2 receptor with an IC50 value of 0.042-2.5 nM. Mrgx2 antagonist-3 blocks downstream G protein signaling and β-Arrestin recruitment, thereby inhibiting MrgX2 receptor-mediated calcium influx and cellular degranulation. Mrgx2 antagonist-3 is promising for research of inflammation-related diseases and pruritus, such as chronic urticaria, allergic asthma .
|
-
- HY-144138
-
|
|
Estrogen Receptor/ERR
|
Cancer
|
|
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) .
|
-
- HY-157230
-
|
|
IAP
|
Cancer
|
|
XIAP antagonist 1 degrades rather than inhibits XIAP, catalyzing rapid degradation of XIAP through the ubiquitin-proteasome pathway [2].
|
-
- HY-143576
-
-
- HY-163703
-
|
|
Dopamine Receptor
|
Neurological Disease
|
|
D4R antagonist-2 (compound 33) is a D4R antagonist. D4R antagonist-2 has a IC50 value of 210 nM, and a Ki value of 59 nM for D4R. D4R antagonist-2 can be used in the Parkinson's disease research .
|
-
- 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-114017
-
|
SAF312; Vanilloid receptor antagonist 1
|
TRP Channel
|
Inflammation/Immunology
|
|
Vanilloid receptor antagonist 1 is a potent vanilloid receptor TRPV1 antagonist extracted from patent US8349852B2, compound B8 .
|
-
- HY-139904
-
|
|
TRP Channel
|
Others
|
|
TRPA1 Antagonist 3 is a photoswitchable TRPA1 agonist that enables optical control of the TRPA1 channel.
|
-
- HY-115975
-
|
|
Bombesin Receptor
|
Cancer
|
|
GRPR antagonist-2 is a potent gastrin releasing peptide receptor (GRPR) antagonist, having the cytotoxicity against certain cancer cells (IC50 of 0.77 and 2.5 μM in HGC-27 and Pan02 cells, respectively). Anticancer activity .
|
-
- HY-156522
-
|
|
CFTR
|
Endocrinology
|
|
CRF1 receptor antagonist-1 (Compound 2) is a CRF1 receptor antagonist. CRF1 receptor antagonist-1 can be used for research of congenital adrenal hyperplasia (CAH) .
|
-
- HY-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-116581
-
|
|
5-HT Receptor
|
Neurological Disease
|
|
5-HT7R antagonist 4 (Compound 4) is a potent 5-HT7 receptor antagonist (Ki=2.6 nM) with low binding affinity for the 5-HT1A receptor (Ki= 476 nM). 5-HT7R antagonist 4 is promising for research of neurological diseases .
|
-
- HY-149386
-
|
|
Dopamine Receptor
Opioid Receptor
|
Inflammation/Immunology
|
|
D3R/MOR antagonist 1 (Compound 114) is a D3R/MOR antagonist (Ki: 46.5 nM and 691 nM respectively). D3R/MOR antagonist 1 has the potential to produce analgesic effects through MOR partial agonism, reduce opioid-misuse liability via D3R antagonism .
|
-
- HY-149387
-
|
|
Dopamine Receptor
Opioid Receptor
|
Inflammation/Immunology
|
|
D3R/MOR antagonist 2 (Compound 121) is a D3R/MOR antagonist (Ki: 361 nM and 85.2 nM respectively). D3R/MOR antagonist 2 has the potential to produce analgesic effects through MOR partial agonism, reduce opioid-misuse liability via D3R antagonism .
|
-
- HY-161247
-
|
|
5-HT Receptor
|
Metabolic Disease
|
|
5HT2A antagonist 2 is an orally active, selective antagonist for 5HT2A with IC50 of 14 nM. 5-HT2A antagonist 2 exhibits good chemical, hepatocyte, and plasma stability, without significant cytotoxicity in cell lines VERO, HFL-1, L929, NIH3T3, CHO-K1 .
|
-
- HY-113960
-
|
|
Estrogen Receptor/ERR
|
Cancer
|
|
ERRα antagonist-1 (Compound A) is a selective and high affinity agonist for estrogen-related receptor α (ERRα). ERRα antagonist-1 inhibits interaction of ERRα with Proliferator-activated Receptor γ Coactivator-1α (PGC-1α) and PGC-1β, the IC50 values are 170 nM and 180 nM, respectively .
|
-
- HY-153129
-
|
|
Prostaglandin Receptor
|
Endocrinology
|
|
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) .
|
-
- HY-14517
-
|
|
Histamine Receptor
|
Neurological Disease
|
|
H3R antagonist 5 (Compound 1b) is a selective histamine H3 receptor inverse agonist with a IC50 of 0.54 nM and the ability to cross the blood-brain barrier. H3R antagonist 5 can be used in central nervous system-related research .
|
-
- HY-145684
-
|
|
Prostaglandin Receptor
|
Inflammation/Immunology
|
|
EP2 receptor antagonist-1 (compound 1) is a potent, reversible, and agonist dependent allosteric prostaglandin EP2 receptor antagonist. EP2 receptor antagonist-1 shows anti-inflammatory effects .
|
-
- HY-145905
-
|
|
Dopamine Receptor
|
Neurological Disease
|
|
D4R antagonist-1 is a potent and selective D4R antagonist with an IC50 of 6.87 µM. D4R antagonist-1 has the potential for the research of Parkinson’s disease .
|
-
- HY-153333
-
|
|
Adenosine Receptor
|
Cardiovascular Disease
|
|
A1/A3 AR antagonist 3 is an A1R/A3R dual antagonist with high affinity at low-micromolar to low-nanomolar. A1/A3 AR antagonist 3 can be used for the research of chronic heart diseases .
|
-
- HY-W471937
-
-
- HY-101704
-
-
- HY-161727
-
|
|
P2Y Receptor
NOD-like Receptor (NLR)
|
Inflammation/Immunology
|
P2Y14R antagonist 1 (compound I-17) is a selective P2Y14R antagonist with an IC50 of 0.6 nM. It exhibits potent P2Y14R antagonistic activity, both in vitro and in vivo efficacy, and favorable pharmacokinetic profiles. P2Y14R antagonist 1 reduces the release of inflammatory factors and cell pyroptosis through the NOD-like receptor family pyrin domain-containing 3 (NLRP3)/gasdermin D (GSDMD) signaling pathway. P2Y14R antagonist 1 holds promise for research in the field of acute gouty arthritis .
|
-
- HY-144603
-
-
- HY-111449
-
BAY-218
1 Publications Verification
AHR antagonist 1
|
Aryl Hydrocarbon Receptor
|
Inflammation/Immunology
Cancer
|
|
BAY-218 (AHR antagonist 1) is an aryl hydrocarbon receptor (AHR) antagonist. BAY-218 has AHR inhibitory activity with an IC50 of 39.9 nM in in U87 glioblastoma cells. BAY-218 can be used for the research of cancer or conditions with dysregulated immune responses .
|
-
- HY-169849
-
|
|
Ephrin Receptor
|
Others
|
|
EphA2 antagonist 1 (4b) is a bile acid conjugate and an ephrin type-A receptor 2 (EPHA2) inhibitor .
|
-
- 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-163363
-
|
|
Adrenergic Receptor
|
Cancer
|
|
β-AR antagonist 2 (compound 43) is an antagonist of β-AR (IC50: 0.17 μM). β-AR-IN-1 inhibits the growth of mouse A549 xenograft tumors and shows cardioprotective efficacy against DOX-induced HF in C57 mice .
|
-
- 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-135976
-
|
|
P2X Receptor
|
Neurological Disease
Inflammation/Immunology
|
|
P2X3 antagonist 34 is a potent, selective and orally active P2X3 homotrimeric receptor antagonist with IC50s of 25 nM, 92 nM and 126 nM for human P2X3, rat P2X3 and guinea pig P2X3 receptors, respectively. P2X3 antagonist 34 is less active against human, rat and guinea pig P2X2/3 heterotrimeric receptors. P2X3 antagonist 34 has strong anti-tussive effect .
|
-
- HY-159942
-
|
|
5-HT Receptor
Dopamine Receptor
|
Neurological Disease
|
|
5-HT7R antagonist 3 (Compound 6.4) is a selective 5-HT7R antagonist (Ki: 8 nM), with Ki of 511 nM (D2), 8930 nM (5-HT1A) and 5786 nM (5-HT2A), respectively. 5-HT7R antagonist 3 possesses antidepressant and anxiolytic effects in mice .
|
-
- HY-156922
-
-
- HY-172600
-
|
|
TRP Channel
|
Inflammation/Immunology
|
|
TRPC6 antagonist-1 (X26) is a TRPC6 antagonist with IC50 values of 0.97 μM, 3.93 μM, 5.77 μM and 4.37 μM for TRPC6, TRPC3, TRPC5 and TRPC7, respectively. TRPC6 antagonist-1 inhibits TGF-β1-induced myofibroblast differentiation, and attenuates renal fibrosis .
|
-
- HY-169859
-
|
|
Prostaglandin Receptor
Interleukin Related
|
Inflammation/Immunology
Cancer
|
|
EP4 receptor antagonist 7 (Compound 14) is an antagonist of the prostaglandin E2 (PGE2) receptor subtype EP4 with an IC50 value of 1.1 nM. EP4 receptor antagonist 7 inhibits PGE2-induced β-arrestin recruitment in HEK293 cells with an IC50 value of 0.9 nM. EP4 receptor antagonist 7 decreases PGE2-induced expression of mRNA encoding IL-4, macrophage mannose receptor 1 (Mrc1), chitinase-like protein 3 (Chil3), chemokine (C-X-C) motif ligand 1 (Cxcl1), triggering receptor expressed on myeloid cells 2 (Trem2), and arginase-1 (Arg1), in RAW 264.7 macrophages. EP4 receptor antagonist 7 combined with an anti-PD-1 antibody inhibits tumor growth and increases infiltration of CD 8+ T cells into tumors in a CT26 murine colon cancer model .
|
-
- HY-173043
-
|
|
5-HT Receptor
|
Cancer
|
|
5-HT6R antagonist 6 exhibits high affinity and selectivity for 5-HT6R , with a Ki value of 42 nM. 5-HT6R antagonist 6 shows weak antiproliferative activity against tumor cells and low toxicity to normal cells. 5-HT6R antagonist 6 can be used in the study of cancer .
|
-
- HY-139314
-
|
|
Adenosine Receptor
|
Metabolic Disease
|
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 .
|
-
- HY-156664
-
-
- HY-156669
-
-
- HY-145193A
-
-
- HY-165155
-
|
|
Leukotriene Receptor
|
Inflammation/Immunology
|
|
CysLT1 receptor antagonist-1 (Compound 4) is an antagonist for cysteinyl leukotriene receptor 1 (CysLT1R) with an IC50 of 3.9 μM. CysLT1 receptor antagonist-1 exhibits weak agonist activity against G-protein-coupled bile acid receptor 1 (GPBAR1) with an efficact of 23% at 10 μM. CysLT1 receptor antagonist-1 can be used for asthma and allergic diseases researchs .
|
-
- HY-101704A
-
|
H 409-22 isomer formic
|
Neurokinin Receptor
|
Neurological Disease
|
|
Y1 receptor antagonist 1 formic (H 409-22 isomer formic) is the formic salt form of Y1 receptor antagonist 1 (HY-101704). Y1 receptor antagonist 1 formic is a neuropeptide Y1 receptor antagonist.
|
-
- HY-157659
-
|
|
WDR5
|
Others
|
|
WDR5-MLL1 antagonist 1 (compound 47) is a compound optimized through protein crystal structure guidance. It has stronger antagonistic activity against WDR5-MLL interaction with a dissociation constant (Kd) of 0.3μM.
|
-
- HY-103362
-
|
Teijin compound 1 hydrochloride
|
CCR
|
Inflammation/Immunology
|
|
CCR2 antagonist 4 hydrochloride (Teijin compound 1 hydrochloride) is a potent and specific CCR2 antagonist, with IC50s of 180 nM for CCR2b. CCR2 antagonist 4 hydrochloride potently inhibits MCP-1-induced chemotaxis with an IC50 of 24 nM .
|
-
- HY-108323
-
|
Teijin compound 1
|
CCR
|
Inflammation/Immunology
|
|
CCR2 antagonist 4 (Teijin compound 1) is a potent and specific CCR2 antagonist, with IC50s of 180 nM for CCR2b. CCR2 antagonist 4 potently inhibits MCP-1-induced chemotaxis with an IC50 of 24 nM .
|
-
- HY-137175
-
|
|
mTOR
|
Cancer
|
|
TMBIM6 antagonist-1, a potential TMBIM6 antagonist, prevents TMBIM6 binding to mTORC2, decreases mTORC2 activity, and also regulates TMBIM6-leaky Ca 2+ .
|
-
- HY-163150
-
|
|
5-HT Receptor
|
Neurological Disease
|
|
5-HT6R antagonist 3 (compound 15) is a potent, selective and brain-penetrant 5-HT6R antagonist with Ki values of 14 nM, 3533 nM, 35 nM, 1449 nM for 5-HT6, 5-HT1A, 5-HT2A, 5-HT7, respectively. 5-HT6R antagonist 3 shows anxiolytic-like and properties neuroprotective and procognitive-like effects. 5-HT6R antagonist 3 has the potential for the research of Alzheimer’s Disease .
|
-
- HY-134542
-
|
|
Calcium Channel
|
Neurological Disease
|
|
CaV1.3 antagonist-1 is a potent and highly selective CaV1.3 L-type calcium channel (LTCC) antagonist with an IC50 of 1.7 μM. CaV1.3 antagonist-1 inhibits CaV1.3 LTCC >600-fold more potently than CaV1.2 LTCC. CaV1.3 antagonist-1, a cyclopentyl derivative, has the potential for Parkinson's disease research .
|
-
- HY-P2268A
-
|
|
Amyloid-β
|
Inflammation/Immunology
Cancer
|
|
RAGE antagonist peptide TFA is an advanced glycation end products (RAGE) antagonist. RAGE antagonist peptide TFA prevents RAGE from binding with several of its most important ligands, including HMGB-1, S100P, and S100A4. RAGE antagonist peptide TFA possesses anti-tumor and anti-inflammatory activities .
|
-
- HY-114025
-
-
- HY-102051
-
|
|
IAP
|
Cancer
|
|
XIAP/cIAP1 antagonist-1 is a potent and orally active XIAP/cIAP1 antagonist with EC50s of 5.1 nM and 0.32 nM for XIAP and cIAP1, respectively. XIAP/cIAP1 antagonist-1 inhibits the tumor growth in dose-dependent manner in vivo .
|
-
- 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-139677A
-
-
- HY-149967
-
|
|
iGluR
|
Neurological Disease
Inflammation/Immunology
|
|
GluN2B-NMDAR antagonist-1 is an orally active GluN2B-NMDAR antagonist. GluN2B-NMDAR antagonist-1 has neuroprotective activity. GluN2B-NMDAR antagonist-1 can be used for research of ischemic injury .
|
-
- HY-131868
-
|
|
TRP Channel
|
Neurological Disease
|
|
TRPV3 antagonist 74a is a potent and selective TRPV3 antagonist. TRPV3 antagonist 74a displays no significant activity against a panel of other ion channels. TRPV3 antagonist 74a can be used for the research of neuropathic pain .
|
-
- HY-133555
-
|
|
mGluR
|
Neurological Disease
|
|
mGluR2 antagonist 1 is a highly potent, orally bioavailable and selective class of mGluR2 negative allosteric modulator (IC50 of 9 nM) with excellent brain permeability .
|
-
- HY-118914
-
|
|
GCGR
|
|
|
Glucagon receptor antagonist inactive control (Compound 2) is a compound structurally similar to the glucagon receptor (GCGR) antagonist Glucagon receptor antagonist (Compound 1) but lacks antagonistic activity against glucagon receptor (GCGR). Glucagon receptor antagonist inactive control can be used as a negative control to study mechanisms related to glucagon receptor-mediated signaling pathways .
|
-
- HY-163274
-
-
- HY-147398
-
|
|
Dopamine Receptor
|
Neurological Disease
|
|
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 .
|
-
- HY-146034
-
|
|
NOD-like Receptor (NLR)
|
Inflammation/Immunology
Cancer
|
|
NOD1/2 antagonist-1 (compound 36b) is a potent NOD1/2 (nucleotide-binding
oligomerization domain-like receptor 1/2) dual antagonist, with IC50 values of 1.13 (NOD1) and 0.77 μM (NOD2), respectively. NOD1/2 antagonist-1 has a acceptable T1/2 (67.6 min). NOD1/2 antagonist-1 (compound 36b) can improve the antitumor efficacy of Paclitaxel (PTX) .
|
-
- HY-153710
-
|
|
P2X Receptor
|
Inflammation/Immunology
|
|
P2X3 antagonist 38 (compound 4) is a potent and orally active P2X3 antagonist with IC50 values of 0.132, 0.165, 0.421 µM for hP2X3, rP2X3, gpP2X3, respectively .
|
-
- HY-U00382
-
-
- HY-160668
-
-
- HY-106659
-
|
NK-1 antagonist 1
|
Neurokinin Receptor
|
Neurological Disease
Endocrinology
|
|
SCH 900978 (NK-1 Antagonist 1) is an antagonist of NK-1 receptor, used in the research of NK-1 related diseases and conditions such as cough, overactive bladder, alcohol dependency and depression .
|
-
- HY-144619
-
|
|
Toll-like Receptor (TLR)
|
Inflammation/Immunology
|
|
TLR7/8 antagonist 2 (Compound 15) is a potent and orally active agonist of TLR7/8 with IC50s of 4.9 and 0.6 nM, respectively. Inappropriate activation of TLR7 and TLR8 is linked to several autoimmune diseases, such as lupus erythematosus. TLR7/8 antagonist 2 has the potential for the research of autoimmune diseases .
|
-
- HY-159179
-
|
|
Integrin
|
Inflammation/Immunology
|
|
α4 integrin receptor antagonist 3 (Compound 11) is an orally active α4integrin receptor antagonist. α4 integrin receptor antagonist 3 can inhibit the adhesion of K562 cells mediated by the interaction between α4β1/VCAM-1 and α4β7/MAdCAM-1, with IC50 values of 130 nM and 2 nM, respectively. α4 integrin receptor antagonist 3 has the potential to be used in the study of dextran sulfate sodium (DSS) colitis mouse model .
|
-
- HY-107698
-
|
|
iGluR
|
Neurological Disease
|
|
PMPA (NMDA antagonist) is an NMDA receptor antagonist with Ki values of 0.84, 2.74, 3.53 and 4.16 μM for NR2A, NR2B, NR2C and NR2D, respectively .
|
-
- HY-163345
-
|
|
5-HT Receptor
|
Neurological Disease
|
|
5-HT7R antagonist 2 (compound 4h) is a 5-HT7R antagonist that antagonizes the G protein and β-arrestin signaling pathways, with a Ki of 67 nM, the IC50 values in cAMP and Tango tests were 2.59 μM and 39.57 μM, respectively. 5-HT7R antagonist 2 has an effect on neurogenesis and can reduce repetitive behaviors related to autism spectrum disorder (ASD) and restore neurogenesis of ASD impairment .
|
-
- HY-102024
-
-
- HY-160677
-
-
- HY-157936
-
|
|
iGluR
|
Neurological Disease
|
|
GluN2B-NMDAR antagonist-2 (compound S-58) is a potent, selective and cross the blood-brain barrier NMDAR-GluN2B antagonist with an IC50 value of 74.01, nM. GluN2B-NMDAR antagonist-2 shows mild cytotoxicity. GluN2B-NMDAR antagonist-2 decreases the cerebral infarction rates and neurologic deficit scores. GluN2B-NMDAR antagonist-2 has the potential for the research of stroke .
|
-
- 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-168742
-
|
|
Vasopressin Receptor
|
Neurological Disease
|
|
V1a/V2 antagonist 1 (Compound 18j) is an orally active dual V1a and V2 receptor antagonist with high binding affinity for both receptors (Ki: 0.13 nM for hV1a, 0.53 nM for hV2 and 0.5 nM for mV1a; IC50: 2.2 nM for hV1a). V1a/V2 antagonist 1 inhibits Oxytocin (HY-17571)-induced scratching behavior in mice .
|
-
- HY-173407
-
|
|
P2Y Receptor
Interleukin Related
|
Inflammation/Immunology
|
|
P2Y14R antagonist 4 (Compound 25l) is an orally active P2Y14R antagonist (IC50: 5.6 nM) with superior binding affinity to P2Y14R over PPTN. P2Y14R antagonist 4 has anti-inflammatory activity and reduces LPS (HY-D1056)-induced proinflammatory cytokines (IL-1β, IL-6, and TNF-α) release .
|
-
- HY-146478
-
|
|
Adenosine Receptor
|
Neurological Disease
Inflammation/Immunology
|
|
A1/A3 AR antagonist 1 (compound 10) is a potent adenosine 1 (A1) and adenosine 3 (A3) receptor dual antagonist with Kis of 36.7 nM, 25.4 nM and 1.47 nM for human A1, human A3 and rat A1, respectively. A1/A3 AR antagonist 1 can be used for researching kidney failure, inflammatory pulmonary diseases, and Alzheimer’s disease .
|
-
- 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-170804
-
-
- 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-158052
-
|
|
PD-1/PD-L1
|
Cancer
|
|
PD-1/PD-L1 antagonist 1 (Compound A5) is an antagonist for programmed cell death-1 (PD-1) and programmed cell death ligand-1 (PD-L1) interaction, with an IC50 of 23.78 nM .
|
-
- 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-155481A
-
|
|
Cannabinoid Receptor
|
Others
|
|
CB2 receptor antagonist 4 (compound (R)-1) is a CB2R-selective inverse agonist with a Kd value of 39 nM .
|
-
- HY-160645
-
-
- HY-100692
-
|
|
MicroRNA
|
Cancer
|
|
Lin28-let-7a antagonist 1 shows a clear antagonistic effect against the Lin28-let-7a interaction with an IC50 of 4.03 μM for Lin28A-let-7a-1 interaction.
|
-
- HY-111669
-
CT1812
1 Publications Verification
Sigma-2 receptor antagonist 1
|
Sigma Receptor
|
Neurological Disease
|
|
CT1812 (Sigma-2 receptor antagonist 1) is an orally active and brain penetrant sigma-2 receptor antagonist with a Ki of 8.5 nM. CT1812 can be used for the research of Alzheimer’s disease .
|
-
- HY-168474
-
|
|
P2X Receptor
|
Inflammation/Immunology
|
|
P2X4 antagonist-4 (compound 64) is a potent P2X4R antagonist with an IC50 value of 8 µM. P2X4 antagonist-4 blocks the ATP-induced NLRP3 inflammasome activation and release of IL-1β .
|
-
- HY-112219A
-
-
- HY-145106
-
-
- HY-158057
-
|
|
Adenosine Receptor
|
Cancer
|
|
A2AR/A2BR antagonist 1 (compound 7ai) has a dual antagonistic effect on A2AR/A2BR, with the IC50 values of 11.2 nM and 6.4 nM for A2AR and A2BR, respectively. A2AR/A2BR antagonist 1 promotes T cell-mediated cancer cell death .
|
-
- HY-173491
-
|
|
CXCR
CCR
|
Inflammation/Immunology
Cancer
|
|
CXCR2/CCR7 antagonist-1 (compound 6) is a potent CXCR2 and CCR7 dual antagonist with IC50s of 0.0046 and 0.0014 μM, respectively. CXCR2/CCR7 antagonist-1 can be used in the study of cancer metastasis and autoimmune diseases .
|
-
- HY-10815
-
|
|
Sigma Receptor
Apoptosis
|
Neurological Disease
Cancer
|
|
σ1 Receptor antagonist-1 is a highly potent and selective sigma 1 receptor antagonist (pKi=10.28). σ1 Receptor antagonist-1 inhibits cell growth, arrests cell cycle at G0/G1 phase and induces apoptosis of MCF-7/ADR cells .
|
-
- HY-146479
-
-
- HY-150059
-
-
- HY-W097612
-
|
|
P2X Receptor
|
Others
|
|
P2X4 antagonist-5 (compound 63) is a control compound for P2X4 antagonists (IC50>100 μM, hP2X4) .
|
-
- HY-155876
-
-
- HY-126123
-
|
|
iGluR
Potassium Channel
|
Neurological Disease
|
|
NR2B-selective NMDA receptor antagonist 1 (compound 29) is a potent antagonist of NR1/NR2B receptors, with IC50s of 0.05 μM, 0.73 μM, 2.4 μM to NR1/NR2B NMDA receptor, hERG, α1-AdR, respectivity. NR2B-selective NMDA receptor antagonist 1 exhibites efficient permeability across the blood–brain barrier .
|
-
- HY-P1376
-
|
|
mAChR
Adrenergic Receptor
|
Endocrinology
|
|
G-Protein antagonist peptide is the substance P-related peptide that inhibits binding of G proteins to their receptors. G-Protein antagonist peptide competitively and reversibly inhibits M2 muscarinic receptor activation of Gi or Go and inhibits Gs activation by β-adrenoceptors.
|
-
- HY-172258
-
|
|
5-HT Receptor
|
Cancer
|
|
5-HT2B antagonist-2 (Compound 19c) is a 5HT2B receptor antagonist with an IC50 of 1.09 nM. 5-HT2B antagonist-2 can downregulate the expression of fibrosis-related genes α-SMA, Timp1, Col1a1, and Col3a1, and significantly reduce the deposition of fibrosis, thereby reducing the fibrotic area and inhibiting the fibrotic process in CCl4-induced liver fibrosis mouse models. 5-HT2B antagonist-2 can be used in the study of immune inflammatory-related diseases, particularly in the research of pulmonary fibrosis diseases .
|
-
- HY-146486
-
|
|
P2Y Receptor
|
Inflammation/Immunology
|
|
P2Y2R/GPR17 antagonist 1 (Compound 14m) is a dual P2Y2R and GPR17 antagonist with IC50 values of 3.17 µM and 1.67 µM against P2Y2R and GPR17, respectively. P2Y2R/GPR17 antagonist 1 shows excellent metabolic stability in human liver microsomes .
|
-
- HY-115833
-
|
|
Histamine Receptor
|
Cancer
|
|
Histamine H4 receptor antagonist-2 serves as a potent activator of p53, demonstrating significant antitumor efficacy.
|
-
- HY-10672
-
|
|
Urotensin Receptor
Cytochrome P450
Sodium Channel
Opioid Receptor
|
Cardiovascular Disease
|
|
Urotensin-II receptor antagonist-1 (compound 1) is a low oral bioavailability (F=0-3%, rat) selective human Urotensin II receptor antagonist, Ki=16 nM (test on HEK293 cells expressing recombinant human UT receptor). Urotensin-II receptor antagonist-1 inhibits cytochrome P450 (IC50=0.75 μM, CYP2D6; 1.4 μM, CYP3A4), inhibits κ-opioid receptor (EC50=3.2 μM), targets cardiac sodium channels (Ki=2.5 μM) .
|
-
- HY-162951
-
|
|
P2X Receptor
|
Cancer
|
|
P2X7 receptor antagonist-5 (compund 13a) is a potent, orally active and long-lasting P2X7 receptor antagonist .
|
-
- HY-110203
-
|
TNF-α antagonist III
|
TNF Receptor
|
Cancer
|
|
R-7050 (TNF-α Antagonist III) is a tumor necrosis factor receptor (TNFR) antagonist with greater selectivity toward TNFα.
|
-
- HY-176143
-
-
- HY-16692
-
-
- HY-101622
-
-
- HY-129946
-
-
- HY-126806
-
|
|
Antibiotic
|
Cancer
|
|
Pyrrofolic acid is a folate antagonist with a low activity as a folate antagonist for Streptococcus faecalis .
|
-
- HY-127024
-
|
|
Thyroid Hormone Receptor
|
Metabolic Disease
|
|
Thyroid hormone receptor antagonist (1-850) is a competitive, selective and high-affinity thyroid hormone receptor (TR) antagonist with an IC50 of 1.5 μM for antagonizing the effect of T3 on TR. Thyroid hormone receptor antagonist (1-850) blocks T3-mediated interaction of TRα and TRβ with nuclear receptor coactivator. Thyroid hormone receptor antagonist (1-850) has no effect on the activity of RARα .
|
-
- HY-120588
-
-
- 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-149916
-
|
|
Adenosine Receptor
|
Cancer
|
|
A2AR-antagonist-1 (compound 38) is an orally active adenosine A2A receptor (A2AR) antagonist (IC50=29 nM). A2AR-antagonist-1 exhibits anti-tumor activity and mouse liver microsomal metabolic stability (t1/2=86.1 min). A2AR-antagonist-1 is also a T cells activator, via inhibiting immunosuppressive molecules (LAG-3 and TIM-3) and enhancing effector molecules (GZMB, IFNG, and IL-2) .
|
-
- 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-145706
-
|
|
Adenosine Receptor
|
Neurological Disease
|
|
A2A/A1 AR antagonist-1 (compound 1a) is dual potent A2A/A1 AR antagonist with Kis of 5.58 and 24.2 nM, respectively. A2A/A1 AR antagonist-1 has the potential for the research of ischemic stroke .
|
-
- 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-138453
-
|
LPA1 receptor antagonist 2
|
LPL Receptor
|
Inflammation/Immunology
|
|
ACT-1016-0707 (Compound 49) is an orally active and selective LPA1 receptor antagonist. ACT-1016-0707 can be used for the research of fibrotic diseases .
|
-
- HY-144390
-
|
GPVI antagonist 1
|
Glycoprotein VI
|
Cardiovascular Disease
|
|
(S)-S007-1558 (compound 5) is a glycoprotein VI (GPVI) platelet receptor antagonist. (S)-S007-1558 inhibits collagen-induced platelet aggregation with an IC50 of 25.3 μM .
|
-
- HY-P1376A
-
|
|
mAChR
Adrenergic Receptor
|
Endocrinology
|
|
G-Protein antagonist peptide TFA is a truncated substance P-related peptide, competes with receptor for G protein binding. G-Protein antagonist peptide TFA inhibits the activation of Gi or Go by M2 muscarinic cholinergic receptor (M2 mAChR) or of Gs by beta-adrenergic receptor in the reconstituted phospholipid vesicles, assayed by receptor-promoted GTP hydrolysis .
|
-
- HY-101306
-
|
|
Opioid Receptor
|
Neurological Disease
|
|
Clocinnamox (mesylate) is a potent opioid antagonist acting at mu, kappa and delta-receptors. Clocinnamox is a selective mu-receptor antagonist than kappa and delta-receptors .
|
-
- HY-13499
-
|
CCR2 antagonist 5
|
CCR
|
Inflammation/Immunology
|
|
JNJ-41443532 (CCR2 antagonist 5) is a selective, orally active hCCR2 inhibitor with good binding affinity (IC50=37 nM) and potent functional antagonism (chemotaxis IC50=30 nM). JNJ-41443532 displays a Ki of 9.6 µM for mCCR2 binding. JNJ-41443532 can be used in the research of inflammatory disease .
|
-
- HY-N12422
-
|
|
Adenosine Receptor
|
Inflammation/Immunology
Cancer
|
|
3′-Methoxyfurano[4″,5″:3,4]chalcone (compound 2) is a selective A2AAR antagonist (IC50=33.5 nM) with high affinity. 3′-Methoxyfurano[4″,5″:3,4]chalcone is also a natural product obtained from the bark of Allium cepa L. 3′-Methoxyfurano[4″,5″:3,4]chalcone can promote T cell activation and can be used in cancer immunity research .
|
-
- HY-145862
-
-
- HY-50713
-
|
|
CaSR
|
Others
|
|
Calcium-Sensing receptor antagonist I is a click chemistry reagent, it contains an Alkyne group and can undergo copper-catalyzed azide-alkyne cycloaddition (CuAAc) with molecules containing Azide groups.
|
-
- HY-149454
-
|
|
P2Y Receptor
|
Cancer
|
|
P2Y1/P2Y12 antagonist-1 (compound 24w) is an orally available dual inhibitor of P2Y1 and P2Y12 with antiplatelet activity. P2Y1/P2Y12 antagonist-1 inhibits ADP-induced platelet aggregation in rabbit plasma with an IC50 of 4.23 μM. P2Y1/P2Y12 antagonist-1 exhibits potent inhibitory effects in rat thrombosis model.
|
-
- HY-120499
-
|
|
Hedgehog
Smo
|
Cancer
|
|
AZD8542 is an antagonist of Smoothened (SMO), playing an important role in oncology. AZD8542 is a? Hedgehog (Hh) pathway antagonist on tumor progression with an emphasis on the role of the stroma compartment .
|
-
- HY-P10938
-
-
- HY-N8892
-
-
- HY-112050
-
-
- HY-147541
-
|
|
Adenosine Receptor
|
Inflammation/Immunology
|
|
A2A/A3 AR antagonist-1 (compound 23) is a dual A2A/A3 adenosine receptor (AR) fluorescent ligand, with Kis of 90 nM and 31.8 nM for hA2A AR and hA3 AR, respectively .
|
-
- HY-P5188A
-
-
- HY-122175
-
-
- HY-153990
-
|
|
FKBP
|
Neurological Disease
|
|
FKBP51F67V-selective antagonist Ligand2 (example 3-3) is a potent FKBP51 F67V-selective antagonist ligand. FKBP51F67V-selective antagonist Ligand2 reverses the anxiogenic phenotype induced by overexpression of FKBP51 F67V in the amygdala. FKBP51F67V-selective antagonist Ligand2 binds to FKBP51 F67V, but not to wild-type FKBP51 or FKBP52 .
|
-
- HY-121394
-
-
- HY-124391
-
-
- HY-116859
-
-
- HY-P1100
-
|
HepArrest
|
Thrombin
|
Cardiovascular Disease
|
|
PM102 (HepArrest) is a heparin antagonist that can reverses the anticoagulant effect of heparin. PM102 potently binds heparin (Kd = 36 nM) in vitro .
|
-
- HY-101440A
-
|
CHF-3381
|
iGluR
|
Neurological Disease
|
|
Indantadol (CHF-3381) hydrochloride is a novel putative NMDA antagonist. Indantadol blocks the NMDA receptor in a dose-dependent and prevents cell damage .
|
-
- HY-120928
-
-
- HY-116495
-
-
- HY-169822
-
-
- HY-169139
-
-
- HY-120277
-
-
- 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-129636A
-
|
GABAB receptor antagonist 1
|
GABA Receptor
ERK
|
Neurological Disease
|
|
(E/Z)-CLH304a (GABAB receptor antagonist 1) is a mixture of (E)-CLH304a and (Z)-CLH304a. (E)-CLH304a (CLH304a; HY-129636) is a specific and noncompetitive GABAB receptor negative allosteric modulator (NAM). CLH304a inhibits Baclofen (HY-B0007)-induced ERK1/2 phosphorylation in HEK293 cells overexpressing GABAB receptors .
|
-
- HY-14388
-
|
|
CCR
HIV
|
Infection
|
|
PF-232798 is an orally active CCR5 antagonist with anti-HIV effects .
|
-
- HY-123397
-
-
- HY-N3436
-
-
- HY-120188
-
|
|
PPAR
|
Others
|
|
CC618 is a selective peroxisome proliferator-activated receptor (PPARβ/δ) antagonist that exhibits antagonism by covalently binding to PPARβ/δ receptors .
|
-
- HY-122216
-
-
- HY-119482
-
|
|
Progesterone Receptor
|
Others
|
|
Cymipristone (ZXH-951), a progesterone receptor antagonist, is used potentially for termination of intrauterine pregnancy .
|
-
- HY-131016
-
|
|
Smo
|
Cancer
|
|
IHR-Cy3 is a potent fluorescent Smo antagonist with an IC50 of 100 nM .
|
-
- HY-100842
-
-
- HY-129783
-
-
- HY-107519
-
|
|
iGluR
|
Neurological Disease
|
|
(R)-3,4-DCPG is an AMPA and NMDA antagonist with a Kd of 77 μM for AMPA. (R)-3,4-DCPG complete antagonizes the NMDA-induced depolarization at a concentration of 500 μM. (R)-3,4-DCPG exhibits a weak antagonistic effect on kainate-induced depolarizations .
|
-
- HY-117099
-
|
|
Calcium Channel
|
Neurological Disease
|
|
TMB-8 is a novel Ca 2+ antagonist. TMB-8 may exert inhibitory effects in smooth muscle by blocking Ca 2+ release from intracellular bound stores.
|
-
- HY-109147A
-
-
- HY-P4857
-
-
- HY-123399
-
-
- HY-P10151
-
|
|
Endothelin Receptor
|
Cardiovascular Disease
|
|
PD 156252 is a hexapeptide that is a highly potent endothelin (ET) antagonist. PD 156252 has enhanced binding affinity for rabbit ETA and rat ETB receptor subtypes with IC50 values of 1.0 and 40 nM, respectively.
|
-
- HY-105109
-
-
- HY-105108
-
|
|
5-HT Receptor
|
Neurological Disease
|
|
Cilansetron hydrochloride hydrate is a 5-HT3 receptor antagonist. Cilansetron hydrochloride hydrate can be used in studies of irritable bowel syndrome .
|
-
- HY-123182
-
-
- HY-103425
-
-
- HY-19429A
-
-
- HY-105798
-
-
- 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-10635A
-
-
- HY-123677
-
|
|
CRFR
|
Neurological Disease
|
|
E2508 is an orally active corticotropin-releasing factor 1 (CRF1) receptor antagonist with a Ki value of 11 nM for hCRF1 .
|
-
- HY-12701
-
-
- HY-122149
-
-
- HY-44132A
-
|
RS 42358-197 hydrochloride
|
5-HT Receptor
|
Cancer
|
|
Dehydro Palonosetron hydrochloride (RS 42358-197 hydrochloride) is a 5-HT3 receptor antagonist. Dehydro Palonosetron hydrochloride has an antiemetic effect .
|
-
- HY-118904
-
-
- HY-105137
-
-
- HY-120161
-
|
3'-Hexylsulfanylabscisic acid
|
ABA Receptor
|
Others
|
|
AS6 (3'-Hexylsulfanylabscisic acid) can bind to PYL proteins, and acts as a PYL antagonist (Kd: 0.48 μM for PYL5) .
|
-
- HY-123869
-
-
- HY-P2276A
-
-
- HY-155117
-
-
- HY-P2638
-
-
- HY-120939
-
-
- HY-101747A
-
-
- HY-10666
-
-
- HY-120682
-
|
|
mAChR
|
Neurological Disease
|
|
UH-AH 37 is a muscarinic (mAChR) antagonist. UH-AH 37 exhibits a higher potency in inhibiting muscarinic responses in intestinal tissue than cardiac tissue .
|
-
- HY-101344
-
-
- HY-120189
-
-
- HY-103010
-
|
|
CXCR
|
Cancer
|
|
MSX-130 is a CXCR4 antagonist. MSX-130 inhibits cancer metastasis .
|
-
- HY-103009
-
MSX-127
1 Publications Verification
|
CXCR
|
Cancer
|
|
MSX-127 is a CXCR4 antagonist. MSX-127 inhibits cancer metastasis .
|
-
- HY-128544A
-
-
- HY-115413
-
-
- HY-W040046
-
|
Nafoxidene hydrochloride
|
Estrogen Receptor/ERR
|
Cancer
|
|
Nafoxidine hydrochloride is a non-steroidal estrogen receptor antagonist with antitumor activity for breast cancer .
|
-
- HY-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-120239
-
|
|
5-HT Receptor
|
Neurological Disease
|
|
Ro 63-0563 is a potent, competitive and selective 5-HT6 receptor antagonist with pKi values of 7.83 and 7.91 for rat and human 5-HT6 receptors, respectively. Ro 63-0563 has no affinity for other receptors .
|
-
- HY-107031
-
|
19560 RP
|
iGluR
|
Others
|
|
Metapramine (19560 RP) is an antidepressant agent, belonging to the class of tricyclic compounds . Metapramine inhibits norepinephrine reuptake, without affecting the reuptake of serotonin or dopamine . Metapramine is a low-affinity antagonist of the N-methyl-D-aspartic acid (NMDA) receptor complex channel .
|
-
- HY-P3232
-
-
- HY-101747
-
-
- HY-101230
-
|
|
Opioid Receptor
|
Neurological Disease
|
|
ICI 174864 is a highly selective, potent δ-receptor antagonist. ICI 174864 is equipotent with naloxone and can not reverse the effect of the μ-agonist [D-Ala2, MePhe4, Gly-Ol5]enkephalin or the κ-agonist-tifluadom .
|
-
- 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-114674
-
-
- HY-132210
-
-
- HY-106810
-
|
Ro 23-6152
|
Calcium Channel
|
Others
|
|
Naltiazem (Ro 23-6152) is a thiazepinone-type calcium antagonist. Naltiazem inhibits platelet aggregation in vitro and in vivo .
|
-
- HY-106810A
-
|
Ro 23-6152 hydrochloride
|
Calcium Channel
|
Cardiovascular Disease
|
|
Naltiazem (Ro 23-6152) hydrochloride is a thiazepinone-type calcium antagonist. Naltiazem hydrochloride inhibits platelet aggregation in vitro and in vivo .
|
-
- HY-A0125
-
-
- HY-101262
-
-
- HY-100785A
-
|
γDGG acetate; γ-D-Glutamylglycine acetate
|
iGluR
|
Neurological Disease
|
|
gamma-DGG acetate (γDGG acetate) is a competitive AMPA receptor blocker. gamma-DGG acetate is also a reversible Excitatory post-synaptic potentials (e.p.s.p.s) antagonist .
|
-
- HY-117547
-
|
ACEA-1021
|
iGluR
|
Neurological Disease
|
|
Licostinel (ACEA-1021) is a glycine receptor antagonist (IC50: 59 nM). Licostinel has neuroprotective activity .
|
-
- HY-124462
-
|
R 2498
|
Sigma Receptor
|
Neurological Disease
|
|
Trifluperidol hydrochloride is a Sigma-1 receptor antagonist with a Ki value of 3.3 nM. Trifluperidol hydrochloride is used in the study of psychosis .
|
-
- HY-124223
-
|
|
mAChR
|
Neurological Disease
|
|
AF-DX 384 (methanesulfonate) is a selective antagonist of M2 and M4 muscarinic acetylcholine receptors (Kis=6.03 and 10 nM, respectively) . AF-DX 384 (methanesulfonate) reverses deficits in novel object recognition and passive avoidance in aged rats, as well as in young rats with impairments induced by scopolamine .
|
-
- HY-117636
-
-
- HY-103473
-
-
- HY-113329
-
|
Taurocyamine
|
Endogenous Metabolite
|
Metabolic Disease
|
|
Guanidinoethyl sulfonate (Taurocyamine) is an orally available, blood-brain permeable competitive inhibitor of taurine transporters and a competitive antagonist of glycine receptors (GlyR) (IC50=565 μM). Guanidinoethyl sulfonate has both weak agonist and antagonist effects on GABAA receptors. Guanidinoethyl sulfonate inhibits taurine transmembrane transport and competitively binds to the GlyR ligand binding domain, thereby blocking glycine-mediated chloride influx, and may regulate brain pH to exert neuroprotective effects. Guanidinoethyl sulfonate can be used for neuroprotection studies of ischemic brain injury .
|
-
- HY-100452A
-
|
OX2R antagonist
|
Orexin Receptor (OX Receptor)
|
Endocrinology
Cancer
|
|
TCS-OX2-29 (hydrochloride) is a potent, high affinities and selective orexin-2 receptor (OX2R) antagonist with an IC50 value of 40 nM and a pKI value of 7.5. TCS-OX2-29 displays ~250-fold selectivity for OX2 over OX1 .
|
-
- HY-131947
-
-
- HY-119667
-
-
- HY-44132AR
-
|
|
5-HT Receptor
|
Cancer
|
|
Dehydro Palonosetron (hydrochloride) (Standard) is the analytical standard of Dehydro Palonosetron (hydrochloride). This product is intended for research and analytical applications. Dehydro Palonosetron hydrochloride (RS 42358-197 hydrochloride) is a 5-HT3 receptor antagonist. Dehydro Palonosetron hydrochloride has an antiemetic effect .
|
-
- HY-123757
-
-
- HY-111036
-
|
|
TRP Channel
|
Others
|
|
AMG0347 is a transient receptor potential type V1 receptor antagonist. AMG0347 inhibits activation of the rat TRPV1 channel by heat (IC50 = 0.2 nm), protons (IC50= 0.8 nm), or capsaicin (IC50 = 0.7 nm) .
|
-
- HY-107327
-
|
(±)-Carazolol; DL-Carazolol; Suacron
|
Adrenergic Receptor
|
Cardiovascular Disease
|
|
Carazolol is a β1/β2 adrenoceptor antagonist of high potency used in the research of hypertension. Carazolol is also a potent, selective β3-adrenoceptor agonist .
|
-
- HY-123374
-
|
|
TRP Channel
|
Neurological Disease
|
|
(Rac)-AMG 628 is the racemate of AMG 628, a potent TRPV1 antagonist with an IC50 of 3.7nM. AMG 628 can be used in chronic pain research .
|
-
- HY-121301
-
|
|
5-HT Receptor
|
Neurological Disease
|
|
Amperozide is an atypical antipsychotic that acts as an antagonist of the 5-HT2 receptor with a Ki value of 26 nM. Amperozide has a low affinity for D2 receptors .
|
-
- HY-W114419
-
-
- HY-135501
-
-
- HY-121453
-
-
- HY-158100
-
-
- HY-171175
-
|
|
Ephrin Receptor
|
Cancer
|
|
UniPR500, a UniPR129 derivative, is a competitive EphA2 receptor antagonist with a Ki of 0.78 μM. UniPR500 dose-dependently reduces binding of biotinylated ephrin-A1 to EphA2 with an IC50 value of 1.1 μM .
|
-
- HY-162130
-
|
|
Bacterial
|
Infection
|
|
Antibacterial agent 176 (Compound 6f) is a potent PqsR antagonist. Antibacterial agent 176 has a good inhibitory effect on P. aeruginosa CF, and a significant inhibitory effect on the production of pyocyanin, 2-alkyl-4 (1H) -quinolones .
|
-
- HY-108530
-
|
|
RAR/RXR
|
Cancer
|
|
MM11253 is a potent and selective RARγ antagonist with an IC50 of 44 nM. MM11253 has lower inhibition of RARα, RARβ and RXRα. MM11253 blocks the growth inhibitory effects of RARγ-selective agonists .
|
-
- HY-120192
-
|
|
GABA Receptor
|
Neurological Disease
|
|
CGP 62349 is a selective and orally active GABAB receptor antagonist that improves cognitive performance in multiple learning paradigms .
|
-
- HY-D1387
-
|
|
Fluorescent Dye
|
Neurological Disease
|
|
Naloxone fluorescein acetate is the fluorescent-derivative of Naloxone. Naloxone is an opioid antagonist. Naloxone is the antidote for reversing the effects of an opioid overdose .
|
-
- HY-12701A
-
|
U-99194A; PNU-99194A maleate; JPC-211 maleate
|
Dopamine Receptor
|
Neurological Disease
|
|
U-99194 maleate is a potent and selective Dopamine3 Receptor (D3 receptor) antagonist. U-99194 maleate also enhances prolactin secretion and striatal dopamine synthesis .
|
-
- HY-131914
-
|
|
Sigma Receptor
|
|
|
EST64454 (compound 9k) is a selective, orally active sigma-1 receptor antagonist with Ki 22 nM. EST64454 can be used to study pain .
|
-
- HY-125615
-
|
|
Glycoprotein VI
|
Cardiovascular Disease
Others
|
|
DMP 728 methanesulfonate is a platelet glycoprotein (GP) IIb/IIIa receptor antagonist. DMP 728 methanesulfonate shows dose-dependent antiplatelet and antithrombotic effects. DMP 728 methanesulfonate can be used in the study of effective antithrombotic agents in thromboembolic diseases of coronary and peripheral arteries .
|
-
- HY-106356
-
-
- HY-117824
-
|
|
Integrin
|
Others
|
|
L-703014 is a fibrinogen receptor antagonist, with the IC50 of 94 nM, that acts as a novel parenteral and potential oral antithrombotic agent .
|
-
- HY-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-19007
-
|
DA 4577
|
Histamine Receptor
|
Endocrinology
|
|
Mifentidine (DA 4577) is a potent and selective H2 Receptor antagonist. Mifentidine has an anti-secretion effect and can antagonize the acid-promoting activity of histamine with EC50 3.28 μM .
|
-
- HY-106745
-
|
Ro 22-4839
|
Calmodulin
|
Cardiovascular Disease
|
|
Elziverine (Ro 22-4839) is a brain circulation improvement agent with vasospasm antispasmodic effects. Elziverine is a calmodulin antagonist. Elziverine inhibits erythrocyte cell membrane rupture, platelet aggregation and lipid peroxidation .
|
-
- HY-W018061C
-
|
(R,R)-CP101,606
|
iGluR
|
Neurological Disease
|
|
(R,R)-Traxoprodil is the the (R,R)-enantiomer of Traxoprodil (HY-W018061). Traxoprodil (CP101,606) is a potent and selective NMDA antagonist and protect hippocampal neurons with an IC50 of 10 nM .
|
-
- HY-14794
-
|
(1R,2S)-milnacipran; F2696
|
Serotonin Transporter
|
Metabolic Disease
|
|
Dextromilnacipran (F2696; (1R,2S)-milnacipran), an enantiomer of milnacipran, is a selective serotonin and norepinephrine (5-HT/NE) reuptake inhibitor. Dextromilnacipran also is a human alpha-adrenergic receptor antagonist, with an IC50 of 3.4 μM. (patent WO2013014263A1).
|
-
- HY-123571
-
-
- HY-170410
-
|
|
iGluR
|
Neurological Disease
|
|
EMD-95885 is a selective NR2B-containing NMDA receptors antagonist with an IC50 of 3.9 nM. EMD-95885 does not interact with other sites on the NMDA receptor .
|
-
- HY-110314
-
|
|
LPL Receptor
|
Infection
|
|
CYM50358 hydrochloride (compound 4v) is a potent, selective sphingosine-1-phosphate 4 (S1P4) receptor antagonist. CYM50358 hydrochloride can be used in the study of influenza infection .
|
-
- HY-N12638
-
|
|
Vasopressin Receptor
|
Endocrinology
|
|
Endolide F (Compound 2) is a proline-containing lactone. Endolide F is a moderate antagonist of the arginine antidiuretic hormone V1A receptor .
|
-
- HY-117683
-
|
|
TRP Channel
|
Neurological Disease
|
|
BCTP is a TRPV1 antagonist. BCTP activated at low pH showed functional antagonist activity against human TRPV1 in CHO cells (IC50=18 nM). BCTP can be used in the study of chronic pain .
|
-
- HY-P2109
-
|
|
Bradykinin Receptor
|
Inflammation/Immunology
|
|
JMV-1645 is a potent and selective B1 bradykinin receptor antagonist with a Ki value of 0.023 nM on the human cloned B1 receptor. JMV-1645 can be utilized in trauma and infection research .
|
-
- HY-103518
-
|
|
GABA Receptor
|
Neurological Disease
|
|
CGP36216 is a selective antagonist at GABA presynaptic receptor. CGP36216 binds to GABAB receptor with a Ki value of 0.3 μM. CGP36216 hydrochloride can be used for research of anxiety and trauma-related disorders .
|
-
- HY-107327R
-
|
|
Adrenergic Receptor
|
Cardiovascular Disease
|
|
Carazolol (Standard) is the analytical standard of Carazolol. This product is intended for research and analytical applications. Carazolol is a β1/β2 adrenoceptor antagonist of high potency used in the research of hypertension. Carazolol is also a potent, selective β3-adrenoceptor agonist .
|
-
- HY-107704
-
|
|
iGluR
|
Neurological Disease
|
|
SDZ 220-040 is a competitive the mammalian NMDA receptor antagonist with a pKi of 8.5. SDZ 220-040 can be used in the study of neurological diseases .
|
-
- HY-101367A
-
|
|
5-HT Receptor
|
Neurological Disease
|
|
GR 55562 dihydrochloride is a selective 5-HT1B receptor antagonist. GR 55562 dihydrochloride can be used for the research of nerve disease .
|
-
- HY-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-76711
-
|
|
Opioid Receptor
|
Cancer
|
|
Naltrexone is an antagonist of Opioid receptor. Naltrexone inhibits cell proliferation in vivo. Naltrexone reduces tumor growth by interfering with cell signalling and modifying the immune system .
|
-
- HY-160603
-
|
|
TRP Channel
|
Others
|
|
PF-05214030 is a TRPV4 antagonist (IC50: 4 and 27nM for hTRPV4 and rTRPV4 respectively). PF-05214030 reverses the reduction in bladder capacity caused by intravesical infusion of a TRPV4 agonist .
|
-
- HY-P3226
-
|
|
IGF-1R
|
Metabolic Disease
|
|
JB-1, an IGF-1 peptide analog, is a selective and potent IGF-1R antagonist. JB-1 competes with IGF-1 by binding the IGF-1 receptor. JB-1 prevents the autophosphorylation of IGF-1R, and has no activity in IGF-II .
|
-
- HY-137628
-
|
|
PKA
|
Cancer
|
|
Sp-8-PIP cAMP sodium is a non-corresponding isomer of 8-Piperidino-cAMP. 8-Piperidino-cAMP binds with high affinity to site A of the regulatory subunit of cAMP-dependent protein kinase type I (AI). Sp-8-PIP cAMP sodium can be used as an antagonist of cAMP-induced activation .
|
-
- HY-123311
-
|
|
Adrenergic Receptor
|
Endocrinology
|
|
CP59430 is an azide analog of the α-adrenaline receptor antagonist Prazosin (HY-B0193). P59430 behaves as a competitive antagonist of α1-adrenaline receptor before photolysis. After photolysis, it specifically and irreversibly labels α1-adrenaline receptor and exhibits non-competitive antagonist activity. CP59430 can be used for the study of receptor molecular characterization .
|
-
- HY-124539
-
|
|
iGluR
|
Neurological Disease
|
|
ZK 187638 is an AMPA receptor antagonist. ZK 187638 antagonizes the kainate-induced currents in cultured hippocampal neurons with an IC50 of 3.4 μM in a noncompetitive fashion .
|
-
- HY-119739
-
|
|
GCGR
|
Metabolic Disease
Cancer
|
|
Skyrin is an anthraquinone compound that can be isolated from almond fruit. Skyrin is a receptor-selective glucagon antagonist. Skyrin can inhibit the growth of tumor cells .
|
-
- HY-107019
-
|
SR 147778
|
Cannabinoid Receptor
|
Metabolic Disease
|
|
Surinabant (SR 147778) is an orally active, selective cannabinoid receptor type 1 CB1R antagonist. Surinabant is used in studies of obesity and alcoholism .
|
-
- HY-10858A
-
|
|
sFRP-1
Wnt
|
Cancer
|
|
WAY 316606 hydrochloride is an inhibitor of the secreted protein sFRP-1, an endogenous antagonist of the secreted glycoprotein Wnt. The affinity of WAY-316606 for sFRP-1 is determined using the FP binding assay with IC50 of 0.5 μM .
|
-
- HY-101139B
-
|
XAC trihydrochloride
|
Adenosine Receptor
|
Neurological Disease
|
|
Xanthine amine congener trihydrochloride (XAC dihydrochloride) is a potent Adenosine A1 receptor and A2?receptor antagonist with IC50 values of 1.8 and 114 nM, respectively. Xanthine amine congener acts as a convulsant agent in mice model .
|
-
- HY-116854
-
|
|
GCGR
|
Metabolic Disease
|
|
NNC 92-1687 is a non-peptide competitive human glucagon receptor antagonist (IC50=20 μM; Ki=9.1 μM). NNC 92-1687 can be used in the research of type 2 diabetes .
|
-
- 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-148088A
-
|
|
Adenosine Receptor
|
Cancer
|
|
M1069 (free base) is a selective and orall active, dual A2A/A2B adenosine receptor antagonist with a selectivity of >100 fold against the A1 and A3 receptors. M1069 (free base) counteracts immune-suppressive mechanisms of adenosine, and exhibits anti-tumor activity .
|
-
- HY-P3225
-
-
- HY-100243
-
|
Ticalopride
|
5-HT Receptor
|
Neurological Disease
|
|
(+)-Norcisapride (Ticalopride) is a potent 5-HT4 agonist and a 5-HT3 antagonist. (+)-Norcisapride has activity in animals models of constipation .
|
-
- HY-101986C
-
|
AR-H 053591 dihydrochloride
|
Neuropeptide Y Receptor
|
Neurological Disease
|
|
BIIE-0246 dihydrochloride (AR-H 053591 dihydrochloride) is a potent and highly selective non-peptide neuropeptide Y (NPY) Y2 receptor antagonist, with an IC50 value of 15 nM .
|
-
- HY-103136
-
-
- HY-162505
-
|
|
CCR
CXCR
|
Inflammation/Immunology
Cancer
|
|
SQA1, a squaramide (SQA) derivative, is a CCR6 antagonist with a Kd of 250 nM. SQA1 is also a CXCR2 inhibitor. The intracellular pocket occupied by SQA1 overlaps with the G protein binding site and stabilizes the closed conformation of the intracellular pocket .
|
-
- HY-109171
-
|
NT-814; BAY3427080
|
Neurokinin Receptor
|
Cardiovascular Disease
Neurological Disease
|
|
Elizanetant (NT-814) is an orally active, selective NK-1,3 receptor antagonist. Elizanetant can reduce the levels of estradiol and progesterone, and is used in the study of vascular motor symptoms and sleep disorders related to menopause in women .
|
-
- HY-117627
-
|
|
Angiotensin Receptor
|
Cardiovascular Disease
|
|
L 158338 is an angiotensin II receptor antagonist. L 158338 alleviates acidosis and increases coronary blood flow during the ischemic period and increases coronary blood flow during the reperfusion period. L 158338 can be used to study myocardial injury during ischemia and reperfusion .
|
-
- HY-P10949
-
|
|
Glycoprotein VI
|
Cardiovascular Disease
|
|
Pep-10L peptide is a glycoprotein VI (GPVI) antagonist with Ki values of 180, 225, and 179 μM for CPR, GPO-1, and Type 1 collagen, respectively. Pep-10L peptide has anti-thrombotic effects .
|
-
- HY-146809
-
|
|
Galectin
|
Cancer
|
|
Galectin-3 is a β Galactoside specific carbohydrate recognition protein (lectin) has the ability to promote the migration of B cell precursor acute lymphoblastic leukemia (BCP-ALL) cells and withstand drug research.
|
-
- HY-103115
-
|
EMD 281014; LY 2422347 hydrochloride
|
5-HT Receptor
|
Neurological Disease
|
|
Pruvanserin hydrochloride (EMD 281014) is a selective serotonin 5-HT2A receptor antagonist with IC50 values of 0.35 nM and 1 nM for human and rat 5-HT2A receptors. Pruvanserin (hydrochloride) can be used for the research of schizophrenia .
|
-
- HY-117184
-
-
- HY-N10663
-
-
- HY-105010
-
-
- HY-B1485
-
|
|
Opioid Receptor
|
Neurological Disease
|
|
Nalmefene hydrochloride is a long acting opioid (MOR and DOR antagonist), and a partial KOR agonist. Nalmefene hydrochloride is used for opioid overdose and alcohol dependence .
|
-
- HY-100356
-
|
CNS 1102 free base
|
iGluR
|
Neurological Disease
|
|
Aptiganel (CNS 1102 (free base)), peptide, is a noncompetitive NMDA antagonist with cerebroprotective effects. Aptiganel can be used for the research of stroke .
|
-
- HY-107537
-
-
- HY-121453R
-
|
|
Adenosine Receptor
|
Cardiovascular Disease
|
|
Bamifylline (hydrochloride) (Standard) is the analytical standard of Bamifylline (hydrochloride). This product is intended for research and analytical applications. Bamifylline hydrochloride is a drug in the chemical class of xanthine that acts as a selective adenosine A1 receptor antagonist .
|
-
- HY-117858
-
-
- HY-165425
-
|
|
Angiotensin Receptor
|
Cardiovascular Disease
|
|
KR31173 is an AT1 antagonist with an IC50 of 3.27 nM. KR31173 can be used as a positron emission tomography (PET) tracer after being labeled with 11C isotope. KR31173 shows promising biodistribution and pharmacological properties in mice. KR31173 selectively binds to organs known to contain a high density of AT1 angiotensin receptors in CD-1 mice .
|
-
- HY-B1505A
-
-
- HY-110001
-
|
|
5-HT Receptor
|
Neurological Disease
|
|
(S)-WAY 100135 dihydrochloride is a highly selective and potent antagonist of 5-HT 1A (IC50=33.9 nM). (S)-WAY 100135 dihydrochloride has anxiolytic activity in animal models .
|
-
- HY-148349A
-
-
- HY-105537
-
|
RS-100975
|
Adrenergic Receptor
|
Endocrinology
|
|
Ro 70-0004 (RS-100975) is a selective alpha1A-adrenoceptor antagonist with a pKi of 8.9. Ro 70‐0004 can be used in the study of prostatic hyperplasia .
|
-
- HY-106299
-
|
ZK98734
|
Progesterone Receptor
|
Metabolic Disease
|
|
Lilopristone (ZK98734) is a progesterone antagonist with a potential to induce menstruation, inhibit nidation, and terminate pregnancy. Lilopristone blocks progesterone action at the endometrium as well as decreases progesterone bioavailability, and can be utilized in antifertility research .
|
-
- HY-121008
-
-
- HY-P1193
-
|
|
Neurokinin Receptor
|
Neurological Disease
|
|
GR 82334 is a potent and specific reversible tachykinin NK1 receptor antagonist . GR 82334 inhibits substance P-induced sensitization by blocking SP NK1 receptors in naked mole-rats .
|
-
- HY-101630A
-
|
EGIS-3886 fumarate
|
5-HT Receptor
|
Others
|
|
Deramciclane fumarate is an antagonist of 5-HT Receptor. Deramciclane fumarate is an inverse agonist of 5-HT2C Receptor with an IC50 of 168 nM. Deramciclane fumarate also decreases basal phosphoinositide hydrolysis .
|
-
- HY-105962
-
|
Eresepine
|
Others
|
Others
|
|
Erizepine is an octopamine receptor class 3 (OAR3) antagonist with a Ki of 474 nM. Erizepine can be utilized in insect research .
|
-
- HY-W922811
-
|
|
iGluR
|
Neurological Disease
|
|
DL-Willardiine is an AMPA antagonist with an IC50 of 2 μM. DL-Willardiine can be utilized in psychotropic cccccc research .
|
-
- HY-122136
-
|
|
Melatonin Receptor
|
Neurological Disease
|
|
S26131 (compound 5) is a potent and selective MT1 melatoninergic ligand, and the Ki values are 0.5 and 112 nM for MT1 and MT2, respectively. S26131 behaves as an MT1 and MT2 antagonist .
|
-
- HY-119971
-
|
|
Nuclear Hormone Receptor 4A/NR4A
|
Metabolic Disease
Cancer
|
|
BIM5078 is a hepatocyte nuclear factor 4α (HNF4α) antagonist that can inhibit the expression of known HNF4α target genes. BIM5078 represses insulin promoter activity through HNF4α antagonism. BIM5078 can be used for the research of cancer and diabetes .
|
-
- HY-19427
-
|
|
P2X Receptor
|
Cancer
|
|
AZD9056 is a P2X7 purinergic receptor antagonist with anticancer activity. AZD9056 can inhibit the invasion and metastasis of cancer stem cells .
|
-
- HY-112219
-
-
- HY-150067
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Cannabinoid Receptor
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Metabolic Disease
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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 .
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- HY-109171R
-
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Neurokinin Receptor
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Cardiovascular Disease
Neurological Disease
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Elinzanetant (Standard) is the analytical standard of Elinzanetant. This product is intended for research and analytical applications. Elizanetant (NT-814) is an orally active, selective NK-1,3 receptor antagonist. Elizanetant can reduce the levels of estradiol and progesterone, and is used in the study of vascular motor symptoms and sleep disorders related to menopause in women .
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- HY-105138
-
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(6R)-BG9719; (6R)-CVT-124
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Adenosine Receptor
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Cardiovascular Disease
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(6R)-Naxifylline ((6R)-BG9719) (ENX R-enantiomer) is the R-enantiomer of Naxifylline (HY-19240). (6R)-Naxifylline is a A1-adenosine antagonist with saluretic activity. (6R)-Naxifylline induces relaxation of spontaneous tone in guinea pig trachea .
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- HY-103375
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CRFR
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Neurological Disease
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SN003 is a reversible antagonist of corticotropin releasing factor receptor 1 (CRFR 1) (IC50 = 241 nM) that displays more than 1000-fold selectivity over CRFR 2. SN003 suppresses CRF-induced ACTH release in vitro. SN003 attenuates depressive-like behavior in rat .
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- HY-107611
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-
- HY-105183
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Endothelin Receptor
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Others
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PD 145065 is a highly potent but non-selective endothelin receptor antagonist with an IC50 value of 4 nM for the ETA receptor for rabbit renal artery vascular smooth muscle cells .
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- HY-76711R
-
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Opioid Receptor
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Cancer
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Naltrexone (Standard) is the analytical standard of Naltrexone. This product is intended for research and analytical applications. Naltrexone is an antagonist of Opioid receptor. Naltrexone inhibits cell proliferation in vivo. Naltrexone reduces tumor growth by interfering with cell signalling and modifying the immune system .
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- HY-B1067B
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Phenazoline phosphate
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Histamine Receptor
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Neurological Disease
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Antazoline phosphate is an H1 receptor antagonist that affects the activity of the central nervous system, has a potent antiarrhythmic effect .
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- HY-167875
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HRP 913
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Dopamine Receptor
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Neurological Disease
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Neflumozide (HRP 913) is an orally active benzisoxazole derivative and a potent dopamine antagonist with antipsychotic activity. Neflumozide can be utilized in psychosis research .
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- HY-B1067A
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Phenazoline
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Histamine Receptor
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Neurological Disease
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Antazoline (Phenazoline) is an H1 receptor antagonist that affects the activity of the central nervous system, has a potent antiarrhythmic effect .
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- HY-P10619
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-
![[Tyr6,D-Phe7,D-His9]-Substance P (6-11)](//file.medchemexpress.com/product_pic/hy-p10619.gif)
- HY-169127
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5-HT Receptor
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Neurological Disease
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Seganserin is an orally active 5-HT receptor antagonist with a plasma half-life of 26.1 ± 12.9 (S.D.) h. Seganserin can be utilized in neurological research .
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- HY-107322A
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Mepirodipine; YM-09730-5 Free base
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Calcium Channel
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Cardiovascular Disease
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Barnidipine (Mepirodipine) is an L-type calcium antagonist (CaA) with high affinity for [ 3H] initrendipine binding sites (Ki = 0.21 nmol/L), has selective action against CaA receptors. Barnidipine is an orally effective antihypertensive agent that can reduce the level of platelet-derived growth factor B-chain mRNA and peripheral vascular resistance .
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- HY-106499A
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- HY-133533
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Cannabinoid Receptor
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Neurological Disease
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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 .
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- HY-120629
-
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CCR
|
Inflammation/Immunology
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BMS-639623 is a potent and orally activeCCR3 antagonist with an IC50 of 0.3 nM. BMS-639623 picomolar inhibition potency against eosinophil chemotaxis (IC50=38 pM). BMS-639623 can be used for the research of asthma .
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- HY-137388A
-
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p-Fluorohexahydrosiladifenidol hydrochloride
|
mAChR
|
Neurological Disease
|
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p-F-HHSiD (p-Fluorohexahydrosiladifenidol) hydrochloride is a selective M3 mAChR antagonist. p-F-HHSiD hydrochloride blocks Acetylcholine-mediated vasodilatation in human umbilical vein endothelial cells (HUVECs) .
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-
- HY-14405
-
|
GW679769
|
Neurokinin Receptor
Cytochrome P450
|
Neurological Disease
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Casopitant (GW679769) is a potent, selective, brain-penetrant and orally active neurokinin 1 (NK1) receptor antagonist. Casopitant antagonizes the emetic effects of Substance P (HY-P0201). Casopitant is also a substrate and weak to moderate inhibitor of CYP3A4. Casopitant is indicated for chemotherapy-induced nausea and vomiting (CINV) and postoperative nausea and vomiting (PONV) .
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- HY-12130
-
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CRFR
|
Neurological Disease
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CP 154526 is a potent, brain-penetrant and selective corticotropin-releasing factor receptor 1 (CRF1) antagonist with a Ki of 2.7 nM. CP 154526 shows selective for CRF1 over CRF2 (Ki = >10 μM). CP 154526 has anxiolytic activities .
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-
- HY-107557
-
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Histamine Receptor
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Neurological Disease
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Proxyfan is a potent histamine H3 receptor antagonist with Ki values of 2.9 nM and 2.7 nM for rat and human H3 receptor, respectively. Proxyfan is over 1000-fold more potent at H3 receptors than other histamine receptors .
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- HY-117634
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-
- HY-10011B
-
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CXCR
|
Inflammation/Immunology
Endocrinology
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(Rac)-SCH 563705 is a racemic mixture of SCH 563705 (HY-10011). SCH 563705 (compound 16) is a potent and orally active CXCR2 and CXCR1 antagonist with IC50 values of 1.3 nM and 7.3 nM and Ki values of 1 nM and 3 nM, respectively .
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-
- HY-12129
-
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CFTR
|
Neurological Disease
|
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CP 154526 hydrochloride is a potent, brain-penetrant and selective corticotropin-releasing factor receptor 1 (CRF1) antagonist with a Ki of 2.7 nM. CP 154526 hydrochloride shows selective for CRF1 over CRF2 (Ki = >10 μM). CP 154526 hydrochloride has anxiolytic activities .
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-
- HY-108432
-
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CCR
|
Inflammation/Immunology
|
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BMS-741672 is a selective and orally active CCR2 antagonist with an IC50 of 1.1 nM. BMS-741672 shows >700-fold selective for CCR2 than CCR5 .
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-
- HY-100382
-
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mGluR
|
Others
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FPTQ is potent mGluR1 antagonist with IC50 values of 6 nM and 1.4 nM for human and mouse mGluR1 respectively . FPTQ has anti-oxidant and anti-inflammatory effects in vitro and in vivo .
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-
- HY-162284
-
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ADAMTS
|
Cardiovascular Disease
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BAY-9835 is a potent and orally active ADAMTS7 and ADAMTS12 antagonist with IC50s of 6 nM and 30 nM, respectively. BAY-9835 is very selective against a range of off-targets and metalloproteases. BAY-9835 can be used for the atherogenesis research .
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-
- HY-123098
-
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Antifolate
Bacterial
DNA/RNA Synthesis
|
Cancer
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Tetrahydromethotrexate is a more potent folate antagonist than Methotrexate (HY-14519) in studies against certain bacteria (Streptococcus faecalis, Pediococcus erevisiae) and in animal models. Tetrahydromethotrexate is used in the research of cancer and autoimmune diseases .
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-
- HY-108480
-
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Neurokinin Receptor
|
Neurological Disease
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|
SDZ NKT 343 is a selective, orally active NK1 receptor antagonist with an IC50 of 0.62 nM against human NK1 receptor. SDZ NKT 343 has good analgesic activity .
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-
- HY-12819
-
-
- HY-107557A
-
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Histamine Receptor
|
Neurological Disease
|
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Proxyfan Oxalate is a potent histamine H3 receptor antagonist with Ki values of 2.9 nM and 2.7 nM for rat and human H3 receptor, respectively. Proxyfan Oxalate is over 1000-fold more potent at H3 receptors than other histamine receptors .
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-
- HY-124767
-
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Neuropeptide Y Receptor
|
Neurological Disease
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SR 142948A is a non-peptide neuropeptide neuropeptin (NT) receptor antagonist. SR 142948A is able to bind to neuropeptin receptors, especially with high affinity for NT1 and NT2 receptors. SR 142948A is mainly used to study the role of neuropeptide in the neurotransmitter system, especially the dopamine system .
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-
- HY-139899
-
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Taste Receptor
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Others
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S6821 is a TAS2R8 antagonist with IC50 value of 0.035 μM. S6821 is not found to be mutagenic or disruptive in vitro, nor is it found to induce micronucleus in bone marrow polychromatic erythrocytes in vivo .
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-
- HY-116601
-
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Cytochrome P450
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Others
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6-Hydroxywarfarin is a metabolite of (+) -warfarin. 6-Hydroxywarfarin is a weaker vitamin K antagonist. 6-Hydroxywarfarin is metabolized by the cytochrome P450 isomer 2C9 (CYP2C9) .
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-
- HY-107644
-
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mAChR
|
Cardiovascular Disease
|
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AQ-RA 741 is a potent and selective M 2 antagonist. AQ-RA 741 inhibits the vagally or agonist-induced bradycardia in rats, cats and guinea-pigs. AQ-RA 741 is used in bradycardiac disorders research .
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-
- HY-106056
-
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D 16726
|
Estrogen Receptor/ERR
|
Cancer
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Zindoxifene is a partial anti-estrogen. Zindoxifene works primarily by binding to estrogen receptors, thereby inhibiting the growth of estrogen-dependent tumor cells. Zindoxifene is able to exhibit the dual properties of estrogen agonists and antagonists and can be used in research and development to target estrogen-dependent tumors, such as prostate and breast cancer .
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-
- HY-100797
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(±)-CPP
|
iGluR
|
Neurological Disease
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(RS)-CPP ((±)-CPP) is a potent and selective NMDA antagonist. (RS)-CPP inhibits central neuron responses, and has anticonvulsant activity .
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-
- HY-N10397
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CCR
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Inflammation/Immunology
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Maceneolignan H (Compound 8) is a neolignane compound isolated from the arils of Myristica fragrans. Maceneolignan H is a selective CCR3 antagonist (EC50 = 1.4 μM). Maceneolignan H has the potential for the research of allergic diseases .
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-
- HY-107497
-
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Biochemical Assay Reagents
|
Cancer
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1-Methyl-3-amino-4-cyanopyrazole (compound 3) is a molecular compound that can be used in the synthesis of adenosine A3 receptor antagonists. 1-Methyl-3-amino-4-cyanopyrazole can be utilized in cancer research .
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-
- HY-120820
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5-HT Receptor
|
Neurological Disease
|
|
LY320954 is a selective 5-HT2A receptor antagonist, with a Ki of 96 nM. LY320954 potently inhibits Ca 2+ influx in the functional assay (EC50 of 35.5 nM). LY320954 inhibits 5-HT-induced paw swelling in rats, with ED50 of 4.8 mg/kg .
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-
- HY-118821
-
|
|
CRFR
|
Metabolic Disease
|
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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 .
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-
- HY-B0002B
-
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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 .
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- HY-116560
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-
- HY-116259
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PPAR
|
Metabolic Disease
|
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PT-S58, a GSK0660 derivative, is a PPARβ/δ full antagonist with an IC50 value of 98 nM. PT-S58 inhibits the agonist-induced transcriptional activity of PPARβ/δ in vitro .
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-
- HY-105122
-
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WIN 49596
|
Androgen Receptor
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Endocrinology
Cancer
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Zanoterone is an orally active antagonist of the androgen receptor (AR) with a Ki of 2.2 μM. Zanoterone blocks the binding of androgens such as testosterone and dihydrotestosterone (DHT), inhibiting the androgen signaling pathway, thereby reducing androgen-dependent prostate hyperplasia and prostate cancer growth .
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-
- HY-17417A
-
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Opioid Receptor
|
Neurological Disease
Cancer
|
|
Naloxone is an antagonist of Opioid receptor. Naloxone alleviates opioid-overdose-induced respiratory depression. Naloxone may cause pulmonary edema and cardiac arrhythmias .
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-
- HY-141609
-
|
AHR antagonist 5 free base
|
Aryl Hydrocarbon Receptor
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Cancer
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IK-175 is a selective and orally active aryl hydrocarbon receptor (AHR) inhibitor. IK-175 effectively blocks AHR from translocating from the cytoplasm to the nucleus. IK-175 is highly selective for AHR over other receptors, transporters, and kinases .
|
-
- HY-141411
-
|
(Rac)-MRI-1867
|
Cannabinoid Receptor
NO Synthase
|
Others
|
|
(Rac)-Zevaquenabant ((Rac)-MRI-1867, compound 6b) is a cannabinoid receptor type 1 (CB1R)/iNOS antagonist, with a Ki of 5.7 nM for CB1R. (Rac)-Zevaquenabant is potential for the research of liver fibrosis .
|
-
- HY-12735
-
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GCGR
|
Metabolic Disease
Endocrinology
|
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SCH 900822 is a potent and selective glucagon receptor (hGCGR) antagonist that blocks the binding of glucagon to its receptor, thereby reducing hepatic glycogenolysis and gluconeogenesis, thereby lowering blood glucose production. SCH 900822 can be used in the study of type 2 diabetes .
|
-
- HY-103357A
-
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Cholecystokinin Receptor
|
Neurological Disease
|
|
LY262691 is a selective CCK-B antagonist with antipsychotic properties. LY262691 decreases the number of spontaneously active A9 and A10 dopamine cells and can be utilized in antipsychotic research .
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-
- HY-106612
-
|
U-K52046; Albanoquil
|
Adrenergic Receptor
|
Cardiovascular Disease
|
|
Abanoquil (U-K52046), an potent and selective α-1 adrenoceptor antagonist, is an anti-arrhythmic agent. Abanoquil can be used for erectile dysfunction research .
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-
- HY-105790A
-
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Cholinesterase (ChE)
|
Cardiovascular Disease
|
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Piperilate (Pipethanate) hydrochloride is one of the mixtures of hetrazepine derivative PAF antagonists with anticholinergics, can be used for bronchial asthma research. Piperilate hydrochloride also causes hypotension and rescues mice poisoned by the organophosphates .
|
-
- HY-149854
-
|
|
Sigma Receptor
|
Neurological Disease
|
|
AB21 is a potent and selective S1R antagonist with Kis of 13, 102 nM for S1R and S2R. AB21 has the effect of reducing mechanical hypersensitivity .
|
-
- HY-149854B
-
|
|
Sigma Receptor
|
Neurological Disease
|
|
AB21 hydrochloride is a potent and selective S1R antagonist with Kis of 13, 102 nM for S1R and S2R. AB21 hydrochloride has the effect of reducing mechanical hypersensitivity .
|
-
- HY-105790
-
|
Pipethanate
|
Cholinesterase (ChE)
|
Cardiovascular Disease
|
|
Piperilate (Pipethanate) is one of the mixtures of hetrazepine derivative PAF antagonists with anticholinergics, can be used for bronchial asthma research. Piperilate also causes hypotension and rescues mice poisoned by the organophosphates .
|
-
- HY-120997
-
|
Berbamine p-nitrobenzoate
|
Calmodulin
|
Cancer
|
|
E6 Berbamine (Berbamine p-nitrobenzoate) is a potent calmodulin (CaM) antagonist. E6 Berbamine inhibits the activity of calmodulin (CaM)-dependent myosin light chain kinase (MLCK), with a Ki of 0.95 μM . E6 Berbamine also shows anti-leukemia activities, with an IC50 of 2.13 μM in K562 cells .
|
-
- 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-117176
-
|
|
iGluR
|
Neurological Disease
|
|
KRP-199 (compound 14h) is an α-amino-3-hydroxy-5-methylisoxazolepropionic acid receptor (AMPA-R) antagonist (Ki=16 nM) with high potency and selectivity for AMPA-R in vitro and good neuroprotective effects in vivo. KRP-199 can be used in the study of neurodegenerative diseases .
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-
- HY-100449A
-
|
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Prostaglandin Receptor
|
Endocrinology
|
|
(S)-AL 8810 is an 11β-fluoro analog of PGF2α that acts as a potent and selective antagonist at the FP receptor. (S)-AL 8810 is the C-15 epimer of AL 8810, having the
inverse, (S), or "natural" configuration at C-15 relative to AL 8810, which is 15-(R) .
|
-
- HY-W017933
-
|
Octahydro-1H-isoindole; Perhydroisoindole; Hexahydroisoindoline
|
Neurokinin Receptor
|
Neurological Disease
|
|
Octahydroisoindole (Perhydroisoindole) is a substance P antagonist that can cross the blood-brain barrier and is useful for the study of movement disorders associated with central nervous system diseases .
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-
- HY-118615
-
|
|
Opioid Receptor
|
Neurological Disease
|
|
LY2048978 is a non-selective opioid receptor antagonist with Ki of 0.287, 0.471 and 1.05 nM for human mu, kappa and delta opioid receptors in vitro, respectively. LY2048978 can be used in the research of major depressive disorder and alcohol use disorder .
|
-
- HY-116386
-
|
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Histamine Receptor
|
Neurological Disease
|
|
GSK334429 is a selective and orally active non-imidazole histamine H3 receptor antagonist with a pKi of 9.49 against human H3 receptor. GSK334429 can be utilized in neurological research .
|
-
- HY-P0264A
-
|
Avexitide acetate
|
GLP Receptor
|
Metabolic Disease
|
|
Exendin(9-39) amide (Avexitide) acetate is a glucagon-like peptide-1 (GLP-1) antagonist that competes with endogenous GLP-1 for the GLP-1R, counteracting the effects of excessive GLP-1 secretion. Exendin(9-39) amide acetate can be utilized in Postbariatric hypoglycemia (PBH) research .
|
-
- HY-P0099
-
|
|
nAChR
|
Others
|
|
Pentapeptide-3 is a pentapeptide fragment of neurotoxin waglerin-1, it can be extracted from the venom of Temple Viper. Pentapeptide-3 is a competitive antagonist of nicotinic acetylcholine receptors (nAChRs), it can blocks nerves at the post-synaptic membrane. Pentapeptide-3 has anti-aging effects and it can be used together with other cosmetic peptides .
|
-
- HY-12709
-
-
- HY-110254
-
|
|
mGluR
|
Neurological Disease
|
|
AZD 9272 is a selective, orally active and brain penetrant mGluR5 antagonist with IC50s of 2.6 nM and 7.6 nM for rat and human receptors, respectively. AZD 9272 shows >3900-fold selectivity over other mGlu receptors 2].
|
-
- HY-100454
-
|
|
Dopamine Receptor
|
Neurological Disease
|
|
CGP 25454A is a selective presynaptic dopamine autoreceptor antagonist which induces the increase of dopamine and acetyl choline. CGP 25454A can be used for major depression research .
|
-
- HY-119635
-
|
|
Apoptosis
|
Cancer
|
|
Albicanol is a sesquiterpenoid with potent antioxidant and antagonistic activities against heavy metal toxicity. Albicanol shows cytotoxicity. Albicanol suppress profenofos (HY-B0832) induced genotoxicity in grass carp hepatocytes .
|
-
- HY-149854A
-
|
|
Sigma Receptor
|
Neurological Disease
|
|
AB21 oxalate is a potent and selective S1R antagonist with Kis of 13, 102 nM for S1R and S2R. AB21 oxalate has the effect of reducing mechanical hypersensitivity .
|
-
- HY-B1067BR
-
|
Phenazoline phosphate (Standard)
|
Reference Standards
Histamine Receptor
|
Neurological Disease
|
|
Antazoline (phosphate) (Standard) is the analytical standard of Antazoline (phosphate). This product is intended for research and analytical applications. Antazoline phosphate is an H1 receptor antagonist that affects the activity of the central nervous system, has a potent antiarrhythmic effect .
|
-
- HY-13204
-
|
KL 373 hydrochloride
|
mAChR
|
Neurological Disease
|
|
Biperiden (KL 373) hydrochloride is a non-selective muscarinic receptor antagonist that competitively binds to M1 muscarinic receptors, thereby inhibiting acetylcholine and enhancing dopamine signaling in the central nervous system. Biperiden hydrochloride has the potential for the research of Parkinson's disease and other related psychiatric disorders .
|
-
- HY-13204A
-
|
KL 373
|
mAChR
|
Neurological Disease
|
|
Biperiden (KL 373) is a non-selective muscarinic receptor antagonist that competitively binds to M1 muscarinic receptors, thereby inhibiting acetylcholine and enhancing dopamine signaling in the central nervous system. Biperiden has the potential for the research of Parkinson's disease and other related psychiatric disorders .
|
-
- HY-160900
-
|
|
TRP Channel
|
Others
|
|
RN-1665 is an orally active TRPV4 antagonist that exhibits excellent selectivity for related TRP receptors such as TRPV1, TRPV3 and TRPM8. RN-1665 is a TRPV4 probe for focus screens, with IC50s of 0.26 μM and 0.39 μM for hTRPV4 and rTRPV4 from human and rat, respectively .
|
-
- HY-14431A
-
|
SAM-531 hydrochloride; PF-05212365 hydrochloride
|
5-HT Receptor
|
Neurological Disease
|
|
Cerlapirdine hydrochloride is a selective and potent full antagonist of the 5-hydroxytryptamine 6 (5-HT6) receptor. Cerlapirdine hydrochloride has the potential for researching the Alzheimer's disease .
|
-
- HY-118410
-
|
|
Integrin
|
Cardiovascular Disease
|
|
L-738167 is an orally active fibrogen receptor antagonist that prevents the binding of fibrinogen to GP IIb/IIIa. L-738167 can be utilized in thrombus research .
|
-
- HY-B1067AR
-
|
|
Histamine Receptor
|
Neurological Disease
|
|
Antazoline (Standard) is the analytical standard of Antazoline. This product is intended for research and analytical applications. Antazoline (Phenazoline) is an H1 receptor antagonist that affects the activity of the central nervous system, has a potent antiarrhythmic effect .
|
-
- HY-161311
-
-
- HY-B0781
-
|
|
Histamine Receptor
mAChR
Adrenergic Receptor
|
Neurological Disease
Endocrinology
|
Promethazine hydrochloride is an orally active phenothiazine derivative with antihistaminic (H1), sedative, antiemetic, anticholinergic, and antimotion sickness properties. Promethazine hydrochloride is a potent H1 receptor antagonist and a mAChR antagonist. It also has a certain affinity for 5-HT2A and 5-HT2C receptors .
|
-
- HY-P5971
-
|
Mifomelatide
|
Melanocortin Receptor
|
Metabolic Disease
|
|
TCMCB07, a cyclic nonapeptide peptide, is an orally active and brain-penetrant melanocortin receptor 4 (MC4R) antagonist. TCMCB07 plays an important role in cachexia .
|
-
- HY-B1296
-
|
(±)-Promethazine
|
Histamine Receptor
|
Neurological Disease
Endocrinology
|
|
Promethazine is an orally active histamine receptor antagonist . Promethazine is first-generation antihistamine of the phenothiazine family, shows strong sedative and weak antipsychotic effects .
|
-
- HY-B0002BR
-
|
|
5-HT Receptor
|
Neurological Disease
Cancer
|
|
Ondansetron (Standard) is the analytical standard of Ondansetron. This product is intended for research and analytical applications. Ondansetron (GR 38032; SN 307) is a highly selective 5-HT3 receptor antagonist, with IC50 value of 103 pM. Ondansetron exerts antiemetic effects by antagonizing 5-HT receptor located on local neurons in the peripheral and central nervous system. Ondansetron suppresses nausea and vomiting caused by chemotherapy and radiation therapy. Ondansetron has orally bioactivity .
|
-
- HY-111256
-
|
|
mGluR
|
Neurological Disease
|
|
A-850002 is a metabotropic glutamate receptor (mGluR) antagonist (IC50=27 nM) that significantly attenuates spontaneous pain behavior after skin incision in rats. A-850002 can be used for analgesia research .
|
-
- 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-163101
-
|
|
Platelet-activating Factor Receptor (PAFR)
Leukotriene Receptor
|
Inflammation/Immunology
|
|
CP-96021 is a potent and orally available leukotriene D4 (LTD4 Ki=34 μM) / platelet activating factor (PAF Ki=37 μM) receptor antagonist. CP-96021 has antagonist capable of simultaneously targeting two different inflammatory mediators, LTD4 and PAF. CP-96021 shows high specificity for α1, α2, β, dopamine-2, adenosine 1, 5-HT1, H1, muscarine, μ opioid, and GABA receptors, all expressing IC50 values greater than 10 μM. CP-96021 can be used to study the pathogenesis of many inflammatory diseases such as asthma .
|
-
- HY-129636
-
|
(E)-GABAB receptor antagonist 1
|
GABA Receptor
ERK
|
Neurological Disease
|
|
CLH304a (compound 14) is a specific and noncompetitive GABAB receptor negative allosteric modulator (NAM). CLH304a decreases GABA-induced IP3 production with an IC50 of 37.9 μM. CLH304a has no effect on other GPCR Class C members such as mGluR1, mGluR2, and mGluR5. CLH304a acts on the heptahelical domain of GB2 subunits and non-competitively inhibits the effect of agonists with inverse agonist properties. CLH304a inhibits Baclofen (HY-B0007)-induced ERK1/2 phosphorylation in HEK293 cells overexpressing GABAB receptor .
|
-
- HY-118497
-
|
|
Endothelin Receptor
|
Cardiovascular Disease
Metabolic Disease
|
|
BMS 182874 is an orallyactive, highly selective endothelin receptor (ETA receptor) antagonist, with IC50 value of 0.150 μM, Ki of 0.055 μM. BMS 182874 reduces the arterial pressure of Deoxycorticosterone acetate (HY-B1472) induced hypertension model in rats, and can be used for cardiovascular disease research .
|
-
- HY-103458
-
|
|
Endothelin Receptor
|
Cardiovascular Disease
Metabolic Disease
|
|
BMS 182874 hydrochloride is an orallyactive, highly selective endothelin receptor (ETA receptor) antagonist, with IC50 value of 0.150 μM, Ki of 0.055 μM. BMS 182874 hydrochloride reduces the arterial pressure of Deoxycorticosterone acetate (HY-B1472) induced hypertension model in rats, and can be used for cardiovascular disease research .
|
-
- HY-149855
-
|
|
Sigma Receptor
|
Others
|
|
AB10 is a selective S1R antagonist. AB10 with Ki of 10, 165 nM for S1R and S2R, respectively. AB10 reverses the effect of Capsaicin (HY-10448) caused pain in model .
|
-
- HY-A0095B
-
|
BIMT-17 hydrochloride; BIMT-17BS hydrochloride
|
5-HT Receptor
Dopamine Receptor
|
Neurological Disease
|
|
Flibanserin hydrochloride (BIMT-17 hydrochloride) is an orally active 5-HT1A receptor agonist and 5-HT2A receptor antagonist with binding affinities Ki of 1 nM and 49 nM, respectively. Flibanserin hydrochloride also binds to dopamine D4 receptors with a Ki of 4-24 nM. Flibanserin hydrochloride has antidepressant and anxiolytic effects and can be used in the study of hypoactive sexual desire disorder (HSDD) .
|
-
- HY-161873
-
|
|
Sigma Receptor
|
Neurological Disease
|
|
PW507 is a potent, brain-penetrant and selective sigma 1 receptor (S1R) antagonist with a Ki of 7.5 nM for human S1R. PW507 displays a low binding affinity to S2R and hERG. PW507 can be used for the study of painful diabetic neuropathy (PDN) .
|
-
- HY-19240
-
|
BG9719; CVT-124
|
Adenosine Receptor
|
Cardiovascular Disease
|
|
Naxifylline (BG9719; CVT-124) is a potent and selective A1-adenosine antagonist with Ki values of 0.67 and 0.45 nM for rat and cloned human A1-receptors, respectively. Naxifylline is a potassium-sparing diuretic for the study of edema associated with congestive heart failure .
|
-
- HY-171253
-
-
- HY-P5971A
-
|
|
Melanocortin Receptor
|
Metabolic Disease
|
|
TCMCB07 TFA, a cyclic nonapeptide peptide, is an orally active and brain-penetrant melanocortin receptor 4 (MC4R) antagonist. TCMCB07 TFA plays an important role in cachexia .
|
-
- HY-19010
-
|
SKF 94482
|
Histamine Receptor
|
Neurological Disease
|
|
BMY-25368 (SKF 94482) is a histamine H2 receptor antagonist that acts as a gastric acid secretion inhibitor. BMY-25368 competitively antagonizes gastric secretion stimulated by histamine and also antagonizes gastric secretion stimulated by Pentagastrin (HY-A0261), Bethanechol (HY-B0406), and food .
|
-
- HY-16489
-
|
|
Potassium Channel
mAChR
Calcium Channel
|
Metabolic Disease
|
|
Terodiline, an antispasmodic agent, blocks hERG current with the IC50 of 375 nM. Terodiline has both anticholinergic and calcium antagonist properties, and effectively reduces abnormal bladder contractions caused by detrusor instability. Terodiline can be used for the research of urinary incontinence .
|
-
- HY-116088
-
|
|
LPL Receptor
|
Inflammation/Immunology
|
|
W123, a FTY720 analog, is a competitive sphingosine 1-phosphate type 1 (S1P1) receptor antagonist. W123 is measured by GTPγS activation, MAPK recruitment, cell migration, and ligand-induced receptor internalization .
|
-
- HY-139799
-
|
|
Neuropeptide Y Receptor
|
Metabolic Disease
|
|
Sch 202596 is a non-peptide antagonist of the galanin receptor subtype GalR1. Sch 202596 blocks the action of galanin by binding to GalR1, thereby reducing food intake. Sch 202596 can be used in the study of obesity and related eating disorders .
|
-
- HY-123560
-
|
|
Bradykinin Receptor
|
Cancer
|
|
BKM-570 is a nonpeptide bradykinin antagonist with anticancer effects. BKM-570 can be used in the study of lung cancer, prostate cancer and ovarian cancer .
|
-
- HY-111321
-
-
- HY-119127
-
|
|
Cholecystokinin Receptor
|
Metabolic Disease
|
|
TP-680 is a cholecystokinin receptor antagonist. TP-680 binds 1510 times more strongly to rat pancreatic CCKA receptors (IC50=1.2 nM) than to rat brain CCKB receptors (IC50=1812.5 nM). TP-680 can be used in the study of gastrointestinal diseases .
|
-
- HY-135456
-
|
|
5-HT Receptor
|
Neurological Disease
|
|
Ro4368554 is a brain-penetrant and selective 5-HT6 antagonist that reverses memory deficits induced by scopolamine and tryptophan depletion. Ro4368554 can be utilized in research related to memory deficits .
|
-
- HY-105689
-
|
|
RAR/RXR
|
Others
|
|
AGN 192870 is a RAR neutral antagonist with Kds of 147, 33, and 42 nM for RARα, RARβ, and RARγ, respectively. AGN 192870 shows IC50s of 87 and 32 nM for RARαand RARγ, respectively. AGN 192870 shows RARβ partial agonism . AGN 192870 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-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-120180
-
|
|
Calcium Channel
|
Cardiovascular Disease
|
|
BMS-188107 is a calcium antagonist that exerts anti-ischemic effects. BMS-188107 improves postischemic contractile function and reduces lactate dehydrogenase release. BMS-188107 can be utilized in cardiovascular research .
|
-
- HY-14431
-
|
SAM-531; PF-05212365
|
5-HT Receptor
|
Neurological Disease
|
|
Cerlapirdine (SAM-531, PF-05212365) is a selective and potent full antagonist of the 5-hydroxytryptamine 6 (5-HT6) receptor. Cerlapirdine has the potential for researching the Alzheimer's disease .
|
-
- 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-107322
-
|
Mepirodipine hydrochloride; YM-09730-5
|
Calcium Channel
|
Cardiovascular Disease
|
|
Barnidipine (Mepirodipine) hydrochloride is an L-type calcium antagonist (CaA) with high affinity for [ 3H] initrendipine binding sites (Ki = 0.21 nmol/L, has selective action against CaA receptors. Barnidipine hydrochloride is an orally active antihypertensive agent that can reduce the level of platelet-derived growth factor B-chain mRNA and peripheral vascular resistance .
|
-
- HY-13204AR
-
|
|
mAChR
|
Neurological Disease
|
|
Biperiden (Standard) is the analytical standard of Biperiden. This product is intended for research and analytical applications. Biperiden (KL 373) is a non-selective muscarinic receptor antagonist that competitively binds to M1 muscarinic receptors, thereby inhibiting acetylcholine and enhancing dopamine signaling in the central nervous system. Biperiden has the potential for the research of Parkinson's disease and other related psychiatric disorders .
|
-
- HY-16474
-
|
TAK-385
|
GnRH Receptor
|
Endocrinology
Cancer
|
|
Relugolix (TAK-385)?is a potent, orally active, nonpeptidic gonadotropin-releasing hormone (GnRH) antagonist. Relugolix possesses high affinity and potent antagonistic activity for human receptor (binding IC50=0.33 nM) and monkey receptor (IC50=0.32 nM) compared with TAK-013 (HY-100209) . Relugolix is used for the study of sex-hormone-dependent diseases, such as including endometriosis, uterine fibroids and prostate cancer et al .
|
-
- HY-B0781R
-
|
|
Reference Standards
Histamine Receptor
mAChR
Adrenergic Receptor
|
Neurological Disease
Endocrinology
|
Promethazine (hydrochloride) (Standard) is the analytical standard of Promethazine (hydrochloride). This product is intended for research and analytical applications. Promethazine hydrochloride is an orally active phenothiazine derivative with antihistaminic (H1), sedative, antiemetic, anticholinergic, and antimotion sickness properties. Promethazine hydrochloride is a potent H1 receptor antagonist and a mAChR antagonist. It also has a certain affinity for 5-HT2A and 5-HT2C receptors .
|
-
- HY-17417AR
-
|
|
Opioid Receptor
|
Neurological Disease
Cancer
|
|
Naloxone (Standard) is the analytical standard of Naloxone. This product is intended for research and analytical applications. Naloxone is an antagonist of Opioid receptor. Naloxone alleviates opioid-overdose-induced respiratory depression. Naloxone may cause pulmonary edema and cardiac arrhythmias .
|
-
- HY-169814
-
|
|
mAChR
|
Neurological Disease
|
|
Lu 25-077 is a brain-penetrant and pharmacologically active N-demethyl metabolite of Lu 25-109 (HY-101586), a partial M1 agonist and M2/M3 antagonist. Lu 25-077 can be utilized in neurological research .
|
-
- 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-14407
-
-
- HY-123460
-
|
|
Somatostatin Receptor
|
Cancer
|
|
BN-81674 is a somatostatin analogue and a selective antagonist of the non-peptide human somatostatin sst3 receptor (Ki=0.92 nM). In addition, BN-81674 reversed the inhibition of cyclic AMP accumulation induced by 1 nM somatostatin through the sst3 receptor with an IC50 value of 0.84 nM. BN-81674 can be used in cancer research .
|
-
- HY-19665
-
|
LY303870
|
Neurokinin Receptor
|
Neurological Disease
Inflammation/Immunology
|
|
Lanepitant (LY303870) is a selective neurokinin-1 (NK-1) receptor antagonist. Lanepitant blocks neurogenic inflammation and pain transmission by preventing the binding of substance P to NK-1 receptors on both neuronal and non-neuronal tissues. Lanepitant can be used to study osteoarthritis .
|
-
- HY-150790
-
-
- HY-114814
-
|
|
Adrenergic Receptor
|
Neurological Disease
|
|
ORM-10921 free base is a selective α-2C adrenergic receptor antagonist with a Ki of 1.4 nM. ORM-10921 free base displays potent antidepressant and antipsychotic-like effects .
|
-
- HY-P1321
-
|
1229U91; GW1229
|
Neuropeptide Y Receptor
|
Neurological Disease
|
|
GR231118, an analogue of the C-terminus of neuropeptide Y, is a potent , competitive and relative seletive antagonist at human neuropeptide Y Y receptor with a pKi of 10.4. GR231118 a potent agonist at the human neuropeptide Y Y4 receptor (pEC50=8.6; pKi=9.6) and a weak agonist at the human and rat neuropeptide YY2 and Y5 receptors. GR231118 also has high affinity for the mouse neuropeptide Y Y6 receptor (pKi= 8.8) .
|
-
- HY-P1321A
-
|
1229U91 TFA; GW1229 TFA
|
Neuropeptide Y Receptor
|
Neurological Disease
|
|
GR231118 TFA, an analogue of the C-terminus of neuropeptide Y, is a potent , competitive and relative seletive antagonist at human neuropeptide YY receptor with a pKi of 10.4. GR231118 a potent agonist at the human neuropeptide YY4 receptor (pEC50=8.6; pKi=9.6) and a weak agonist at the human and rat neuropeptide Y Y2 and Y5 receptors. GR231118 also has high affinity for the mouse neuropeptide YY6 receptor (pKi= 8.8) .
|
-
- HY-133112
-
|
3-Hydroxy-7-desmethyl agomelatine
|
Melatonin Receptor
5-HT Receptor
|
Neurological Disease
|
|
7-Desmethyl-3-hydroxyagomelatine (3-Hydroxy-7-desmethyl agomelatine), a metabolite of Agomelatine, has less activity than Agomelatine . Agomelatine is a melatonergic (MT1 and MT2) agonist and serotonergic (5HT2C) antagonist .
|
-
- HY-119087
-
-
- HY-118518
-
|
|
Calcium Channel
|
Cardiovascular Disease
Cancer
|
|
Ronipamil is a calcium ion antagonist. Ronipamil increases the specific binding and internalization of human 125I-LDL in human skin fibroblasts (HSF) and the human hepatoma cell line Hep G2 .
|
-
- HY-B1690
-
|
|
Antibiotic
Bacterial
Histamine Receptor
|
Infection
|
|
Methdilazine is an orally active antibiotic (histamine antagonist). Methdilazine can inhibit various mycobacterium with MIC values at 5-15 μg/mL in vitro and in vivo, which can be used for the research of infectious diseases .
|
-
- HY-B1690A
-
|
|
Antibiotic
Bacterial
Histamine Receptor
|
Infection
|
|
Methdilazine hydrochloride is an orally active antibiotic (histamine antagonist). Methdilazine hydrochloride can inhibit various mycobacterium with MIC values at 5-15 μg/mL in vitro and in vivo, which can be used for the research of infectious diseases .
|
-
- 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-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-50848
-
|
|
Prostaglandin Receptor
|
Cardiovascular Disease
|
|
BW A868C, a hydantoin compound, is a BW245C structural analogue. BW A868C is a selective and potent competitive prostaglandin D2 (PGD2) antagonist. BW A868C has no effect on other prostaglandin receptors (IP, EP1, EP2, TP and FP) .
|
-
- HY-112741
-
|
|
Leukotriene Receptor
|
Inflammation/Immunology
|
|
SB-209247 is a selective, high affinity and orally active leukotriene B4 (LTB4) receptor antagonist with a Ki of 0.78 nM. SB-209247 blocks LTB4-induced Ca 2+ mobilization with an IC50 of 6.6 nM. SB-209247 shows a potent anti-inflammatory activity .
|
-
- HY-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-P10571
-
|
|
Melanocortin Receptor
|
Endocrinology
|
|
GPS1573 is a noncompetitive antagonist of melanocortin type 2 receptor (MC2R) that dose-dependently antagonizes ACTH-stimulated MC2R activity (IC50=66 nM). GPS1573 can be used in the study of Cushing's disease due to its highly selective antagonism of MC2R .
|
-
- HY-15852
-
|
|
Drug Metabolite
|
Others
|
|
THRX-195518 is the major metabolite of Revefenacin (HY-15851), a lung-selective and long-acting muscarinic antagonist. THRX-195518 can be utilized in research related to chronic obstructive pulmonary disease .
|
-
- HY-107561
-
|
|
Histamine Receptor
|
Inflammation/Immunology
|
|
A-943931 (Compound 10) is a histamine H4 receptor antagonists. A-943931 has improved pharmacotropic and in vivo efficacy in models of pain and inflammation. A-943931 can be used in vivo anti-inflammatory and anti-nociception research .
|
-
- HY-16474R
-
|
|
GnRH Receptor
|
Endocrinology
Cancer
|
|
Relugolix (Standard) is the analytical standard of Relugolix. This product is intended for research and analytical applications. Relugolix (TAK-385) is a potent, orally active, nonpeptidic gonadotropin-releasing hormone (GnRH) antagonist. Relugolix possesses high affinity and potent antagonistic activity for human receptor (binding IC50=0.33 nM) and monkey receptor (IC50=0.32 nM) compared with TAK-013 (HY-100209) . Relugolix is used for the study of sex-hormone-dependent diseases, such as including endometriosis, uterine fibroids and prostate cancer et al .
|
-
- HY-10315
-
|
RWJ-53308
|
Integrin
|
Cardiovascular Disease
|
|
Elarofiban (RWJ-53308) is a nonpeptide, orally active antagonist for fibrinogen receptor αIIbβ3 (GPIIb/IIIa), with an IC50 of 0.15 nM. Elarofiban has the potential for platelet mediated thrombotic disorders research .
|
-
- HY-112874
-
|
|
CCR
|
Neurological Disease
Inflammation/Immunology
Cancer
|
|
BMS-681 is an orthosteric antagonist of CC chemokine receptor 2 (CCR2). BMS-681 restricts the movement of the extracellular end of TM6 by stabilizing TM7. TM7 and TM6 are the main components of the orthosteric binding site. BMS-681 can be used to study inflammatory neurodegenerative diseases and cancer .
|
-
- HY-106444A
-
|
MPV-1730 hydrochloride; JP-1730 hydrochloride
|
Adrenergic Receptor
|
Neurological Disease
|
|
Fipamezole hydrochloride is a potent and orally active α2-adrenergic receptor antagonist with Ki values of 9.2 nM, 17 nM, and 55 nM for human α2A, α2B, and α2C, receptors, respectively. Fipamezole hydrochloride is an anti-dyskinetic agent, and can be used for the study of Parkinson's disease .
|
-
- HY-119832B
-
|
(S)-EGIS-2062 free acid; (S)-EGYT-2062 free acid
|
Histamine Receptor
|
Inflammation/Immunology
|
|
(S)-Setastine ((S)-EGIS-2062 free acid) is a non-sedating, highly potent antagonist of H1 receptor-mediated responses. (S)-Setastine has a long-lasting antihistamine effect and good oral efficacy. (S)-Setastine can be used in the research of allergic diseases .
|
-
- HY-164083
-
|
|
5-HT Receptor
|
Neurological Disease
|
|
GR65630 is a potent and selective 5-hydroxytryptamine (5-HT) type 3 receptor antagonist. GR65630 can be used to study the expression patterns of 5-HT3 receptors in different brain regions and their possible functions in the central nervous system. GR65630 and its radiolabeled form [ 3H]GR65630 can be used to study the distribution, density and affinity of the receptors .
|
-
- HY-146413
-
|
|
CXCR
HIV
|
Infection
Cancer
|
|
HF50731 (compound 21) is a potent CXCR4 antagonist. HF50731 shows strong CXCR4 binding affinity, with IC50 of 19.8 nM. HF50731 effectively inhibits calcium mobilization, cell migration, and HIV-1 infection via CXCR4 coreceptor, with IC50 values of 119.2 nM, 621.4 nM and 1.5 μM .
|
-
- HY-108683
-
|
|
Orexin Receptor (OX Receptor)
|
Neurological Disease
|
|
ACT-335827 is a selective, orally active, brain-penetrant orexin type 1 receptor antagonist. ACT-33582 acts on OXR1 and OXR2 with IC50 values of 6 nM and 417 nM, respectively. ACT-33582 can be used in studies related to neurological disorders .
|
-
- HY-B1296S1
-
-
- HY-107626
-
|
|
MCHR1 (GPR24)
5-HT Receptor
|
Neurological Disease
|
|
ATC0065 is a potent, selective and orally active melanin-concentrating hormone (MCH) receptor 1 (MCHR1) antagonist with an IC50 of 15.7 nM for human MCHR1. ATC0065 does not exhibits significant activity for MCHR2. ATC0065 has anxiolytic and antidepressant activities .
|
-
- 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-107745
-
-
- HY-12397
-
|
|
VD/VDR
|
Endocrinology
|
|
ZK159222, a 25-carboxylic ester analogue of 1α,25-(OH)2D3, is a potent 1α,25-(OH)2D3 receptor (VDR) antagonist. The mechanism of ZK159222 antagonistic action is mediated by a lack of ligand-induced vitamin D receptor interaction with coactivators. ZK159222 has a partial agonistic character .
|
-
- HY-P10405
-
|
|
Dopamine Receptor
|
Neurological Disease
|
|
TAT-D1 peptide is a selective D1-D2 heterogeneous antagonist. TAT-D1 peptide destroys the heterodimer of the D1-D2 receptor by interacting with the specific domain of the D2 receptor through its unique amino acid sequence, in particular the two glutamate residues at the C terminal of the D1 receptor. TAT-D1 peptide can be used to study the role of D1-D2 receptor heterodimers in the regulation of depressive and anxiety-like behaviors .
|
-
- HY-106444
-
|
MPV 1730; JP-1730
|
Adrenergic Receptor
|
Neurological Disease
|
|
Fipamezole (MPV 1730; JP-1730) is a potent and orally active α2-adrenergic receptor antagonist with Ki values of 9.2 nM, 17 nM, and 55 nM for human α2A, α2B, and α2C, receptors, respectively. Fipamezole is an anti-dyskinetic agent, and can be used for the study of Parkinson's disease .
|
-
- HY-167855
-
|
|
P2Y Receptor
|
Inflammation/Immunology
|
|
MRS4833 (compound 15) is an orally active, potent, competitive P2Y14R antagonist with an of IC50 of 5.92 nM for hP2Y14R and an IC50 of 4.8 nM for mP2Y14R. MRS4833 reduces airway eosinophilia in a protease-mediated asthma model and reverses chronic neuropathic pain in a mouse CCI model .
|
-
- HY-149014
-
|
|
Orexin Receptor (OX Receptor)
|
Neurological Disease
|
|
OX2R-IN-1 (compound 15) is a low cytotoxicity profile OX2R-IN-1 antagonist (a potential OX2R binder) with an IC50 value of 484 μM. OX2R-IN-1 (compound 15) can cross the BBB into the brain with a short half-life .
|
-
- 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-N10132
-
|
|
nAChR
|
Infection
Neurological Disease
|
|
Microgrewiapine A is an antagonist of nAChR. Microgrewiapine A inhibits hα4β2 and hα3β4 activity with 60% and 70% inhibition, respectively. Microgrewiapine A has selective cytotoxic against HT-29 human colon cancer cells with an IC50 of 6.8 μM .
|
-
- HY-172808
-
|
|
Cannabinoid Receptor
Cytochrome P450
|
Metabolic Disease
|
|
BNS808 is an orally active and selective cannabinoid-1 receptor (CB1R) antagonist (IC50 = 0.8 nM) with notable CB2R selectivity and minimal brain penetration. BNS808 is studied in research on obesity and its associated metabolic complications, such as metabolic dysfunctional-associated steatotic liver disease (MASLD). BNS808 has reduced free drug availability for CNS entry, enhancing safety and minimizing drug-drug interactions through high plasma binding .
|
-
- 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-19374
-
|
|
GCGR
|
Metabolic Disease
|
|
BAY-27-9955 is an orally active non-peptide glucagon receptor antagonist. Bay 27-9955 competitively blocks the interaction of glucagon with the human glucagonreceptor at an IC50 value of 110 nM. BAY-27-9955 can be used for the study of type 2 diabetes .
|
-
- HY-P10550
-
|
|
VEGFR
|
Cancer
|
|
VGB4 is a VEGF-A and VEGF-B antagonist peptide that duplicates two binding domains of VEGF-B (loop 1 and loop3) and are linked together by the receptor-binding domain of VEGF-A (loop3). VGB4 has significant anti-angiogenic and anti-tumor activities and can regulate tumor growth and metastasis through multiple mechanisms. VGB4 could be used in anti-tumor research .
|
-
- HY-107626A
-
|
|
MCHR1 (GPR24)
5-HT Receptor
|
Neurological Disease
|
|
ATC0065 free base is a potent, selective and orally active melanin-concentrating hormone (MCH) receptor 1 (MCHR1) antagonist with an IC50 of 15.7 nM for human MCHR1. ATC0065 free base does not exhibits significant activity for MCHR2. ATC0065 free base has anxiolytic and antidepressant activities .
|
-
- HY-116248
-
|
|
RAR/RXR
Apoptosis
|
Cancer
|
|
Ro 41-5253 is an orally active selective retinoic acid receptor alpha (RARα) antagonist. Ro 41-5253 can bind RARα without inducing transcription or affecting RAR/RXR heterodimerization and DNA binding. Ro 41-5253 can inhibit cancer cell proliferation and induce apoptosis, has antitumor activity .
|
-
- HY-P3245
-
|
|
Apoptosis
|
Cancer
|
|
HXR9 is a cell-permeable peptide and a competitive antagonist of HOX/PBX interaction. HXR9 antagonizes the interaction between HOX and a second transcrip-tion factor (PBX), which binds to HOX proteins in paralogue groups1 to 8. HXR9 selectively decreases cell proliferation and promotes apoptosis in cells with a high level of expression of the HOXA/PBX3 genes, such as MLL-rearranged leukemic cells .
|
-
- HY-P3245A
-
|
|
Apoptosis
|
Cancer
|
|
HXR9 hydrochloride is a cell-permeable peptide and a competitive antagonist of HOX/PBX interaction. HXR9 hydrochloride antagonizes the interaction between HOX and a second transcrip-tion factor (PBX), which binds to HOX proteins in paralogue groups1 to 8. HXR9 hydrochloride selectively decreases cell proliferation and promotes apoptosis in cells with a high level of expression of the HOXA/PBX3 genes, such as MLL-rearranged leukemic cells .
|
-
- HY-109593
-
-
- HY-10315A
-
|
|
Integrin
|
Cardiovascular Disease
|
|
Elarofiban diTFA is the salt form of Elarofiban (HY-10315) with two TFA. Elarofiban diTFA is a nonpeptide, orally active antagonist for fibrinogen receptor αIIbβ3 (GPIIb/IIIa), with an IC50 of 0.15 nM. Elarofiban diTFA has the potential for platelet mediated thrombotic disorders research .
|
-
- HY-122171
-
|
|
Histamine Receptor
|
Neurological Disease
|
|
A-317920 is a selective and potent rat histamine H3 receptor (H3R) antagonist with pKi value of 9.2 and 7.0 for full-length rat and full-length human H3R, respectively. A-317920 exhibits over 130 fold selective affinity for the rat over the human H3R. A-317920 enhances cognition via H3R blockade .
|
-
- HY-106874A
-
|
RS-15385-197 hydrochloride
|
Adrenergic Receptor
|
Neurological Disease
|
|
Delequamine (RS-15385-197) hydrochloride is an orally active and selective α2-adrenergic receptor antagonist with a pKi of 9.5 for α2-adrenoceptors in rat cortex. Delequamine hydrochloride shows >1000 fold selectivity against 5-HT1A receptors and α1-adrenoceptors. Delequamine hydrochloride can be used for the study of erectile dysfunction .
|
-
- HY-106874
-
|
RS-15385-197
|
Adrenergic Receptor
|
Neurological Disease
|
|
Delequamine (RS-15385-197) is an orally active and selective α2-adrenergic receptor antagonist with a pKi of 9.5 for α2-adrenoceptors in rat cortex. Delequamine shows >1000 fold selectivity against 5-HT1A receptors and α1-adrenoceptors. Delequamine can be used for the study of erectile dysfunction .
|
-
- HY-14407AR
-
|
|
Neurokinin Receptor
|
Neurological Disease
Endocrinology
Cancer
|
|
Fosaprepitant (dimeglumine) (Standard) is the analytical standard of Fosaprepitant (dimeglumine). This product is intended for research and analytical applications. Fosaprepitant dimeglumine (MK-0517) is a proagent of Aprepitant (HY-10052). Fosaprepitant dimeglumine is a neurokinin-1 receptor antagonist, which is development for the prevention of chemotherapy-induced nausea and vomiting (CINV) .
|
-
- HY-103208
-
|
|
Adrenergic Receptor
|
Metabolic Disease
|
|
Benalfocin is a novel selective alpha-2 adrenergic receptor antagonist. Benalfocin reduces blood pressure and heart rate. Benalfocin can be used in the study of cardiovascular effects .
|
-
- HY-117053
-
|
|
Neurokinin Receptor
|
Neurological Disease
|
|
ZM 253270 is a species-selective non-peptide NK-2 receptor (NK-2R) antagonist. ZM 253270 competitively inhibits the binding of [ 3H]NKA to native or cloned NK-2R from hamster bladder (Ki=2 nM), but has a weaker inhibitory effect (48-fold) on the binding of [ 3H]NKA to cloned human NK-2R .
|
-
- HY-P10373
-
|
|
JAK
|
Infection
|
|
pJAK2(1001-1013) is a SOCS1/3 antagonist. pJAK2(1001–1013) plays a positive role in antiviral immune response by inhibiting the negative regulatory effect of SOCS proteins and enhancing the JAK/STAT signaling pathway
|
-
- HY-116908
-
|
|
5-HT Receptor
|
Neurological Disease
|
|
SB-272183 is a selective 5-HT1A, 5-HT1B and 5-HT1D receptor antagonist. In addition, SB-272183 is also a potent and selective ligand for 5-HT1A, 5-HT1B and 5-HT1D receptors in human recombinant and native tissues with pKi values of 8.0, 8.1 and 8.7, respectively. SB-272183 can be used in antidepressant research .
|
-
- HY-14128
-
|
SB-723620
|
CRFR
|
Neurological Disease
|
|
NBI-34041 (SB-723620) is a selective and orally active nonpeptide CRF1 receptor antagonist with an IC50 of 58.9 nM and a Ki of 4.0 nM for human CRF1 receptor. NBI-34041 has no inhibitory effect on the CRF2 receptor. NBI-34041 can be used for depression and anxiety disorders research.
|
-
- HY-100821
-
|
|
Bacterial
|
Infection
|
|
2,4-Dihydroxyphenylacetylasparagine is a potent and selective antagonist of glutamate. 2,4-Dihydroxyphenylacetylasparagine inhibits glutamate binding to rat brain synaptic membranes .
|
-
- HY-19409
-
|
|
Calcium Channel
|
Neurological Disease
|
|
AJG049 is a novel antagonist of the Ca 2+ channel with an IC50 value of 79 nM. AJG049 can be used to reduce the contraction of intestinal smooth muscle .
|
-
- HY-118944
-
|
|
Adrenergic Receptor
|
Endocrinology
|
|
L-748328 is a potent and selective human β3-adrenergic receptor antagonist. L-748328 has a Ki of 3.7 nM against human cloned β3-AR expressed in Chinese hamster ovary (CHO) cells. In addition, L-748328 inhibits the lipolytic response induced by the β3-AR agonist L-742791 in isolated non-human primate adipocytes .
|
-
- HY-19057
-
|
MK-467; L-659066
|
Adrenergic Receptor
|
Cardiovascular Disease
Neurological Disease
|
|
Vatinoxan (MK-467) is an alpha 2-adrenergic receptor antagonist. The peripheral selectivity of Vatinoxan determines that it has limited penetration across the blood-brain barrier and therefore has low concentrations in the central nervous system. Vatinoxan antagonizes alpha 2-adrenergic receptor receptors by binding to them, thereby reducing or preventing cardiovascular effects caused by α2-adrenergic agonists. Vatinoxan can be used in studies of cardiovascular effects, sedation and analgesia .
|
-
- HY-106684A
-
|
|
Adrenergic Receptor
|
Cardiovascular Disease
|
|
Ridazolol hydrochloride is a β-adrenergic receptor (βAR) antagonist. Ridazolol hydrochloride exhibits a high degree of selectivity for β-1 adrenergic receptor (β1AR) and possesses moderate intrinsic sympathomimetic activity (ISA). Ridazolol hydrochloride can competitively antagonize the relaxation effects induced by isoproterenol. Ridazolol hydrochloride is utilized in the research of cardiovascular diseases .
|
-
- HY-106684
-
|
|
Adrenergic Receptor
|
Cardiovascular Disease
|
|
Ridazolol is a β-adrenergic receptor (βAR) antagonist. Ridazolol exhibits a high degree of selectivity for β-1 adrenergic receptor (β1AR) and possesses moderate intrinsic sympathomimetic activity (ISA). Ridazolol can competitively antagonize the relaxation effects induced by isoproterenol. Ridazolol is utilized in the research of cardiovascular diseases .
|
-
- HY-110056
-
|
|
CRFR
|
Neurological Disease
|
|
NBI 35965 hydrochloride is a selective, orally active and brain-penetrant corticotropin-releasing factor receptor 1 (CRF1) antagonist with a Ki value of 4 nM and a pKi value of 8.5. NBI 35965 hydrochloride does not inhibit CRF2. NBI 35965 hydrochloride reduces CRF or stress-induced adrenocorticotropic hormone (ACTH) production in vivo with pIC50 values of 7.1 and 6.9, respectively. NBI 35965 hydrochloride shows anxiolytic effects .
|
-
- HY-12079
-
|
|
CCR
|
Inflammation/Immunology
|
|
CP-481715 is a potent, reversible and selective CCR1 antagonist with a Kd of 9.2 nM for human CCR1. CP-481715 is >100-fold selective for CCR1 as compared with a panel of G-protein-coupled receptors including related chemokine receptors. CP-481715 has the potential for rheumatoid arthritis and other inflammatory diseases research .
|
-
- HY-123012
-
|
LY-488756
|
Adrenergic Receptor
|
Others
|
|
Lubabegron is a potent modulator of β-adrenergic receptor (β-AR). Lubabegron demonstrates antagonistic behavior at the β1 and β 2 receptor subtypes and agonistic behavior at the β 3 receptor subtype in cattle. Lubabegron reduces NH3 gas emissions from an animal or its waste. Lubabegron is available as an animal supplement .
|
-
- HY-131479A
-
|
|
Drug Metabolite
|
Neurological Disease
|
|
Threo-dihydrobupropion is a major metabolite of Bupropion, formed via oxidation and reduction exhibit pharmacological activity. Bupropion, a dual dopamine-norepinephrine uptake inhibitor and a nicotine receptor antagonist, is widely used in the management of depression and as a smoking cessation aid .
|
-
- HY-124637
-
|
|
Trk Receptor
|
Neurological Disease
|
|
ALE-0540, a nonpeptidic small molecule, is a nerve growth factor receptor antagonist. ALE-0540 inhibits the binding of NGF to tyrosine kinase (Trk) A or both p75 and TrkA with IC50 values of 5.88 μM and 3.72 μM, respectively. ALE-0540 can be used to examine mechanisms leading to the development of agents for the treatment of pain .
|
-
- HY-117903A
-
|
|
Smo
Hedgehog
|
Cancer
|
|
MRT-92 is a Smoothened (Smo) antagonist (Ki=0.7 nM) with anticancer activity. MRT-92 inhibits Hedgehog signaling pathway and rodent cerebellar granule cell proliferation by blocking overlapping binding sites in the transmembrane domain of the Smoothened receptor (IC50=0.4 nM). MRT-92 can be used in the study of cerebellar glioma .
|
-
- HY-103454B
-
|
|
Estrogen Receptor/ERR
Apoptosis
|
Endocrinology
Cancer
|
|
MPP hydrochloride is a potent and selective ER (estrogen receptor) modulator. MPP hydrochloride induces significant apoptosis in the endometrial cancer and oLE cell lines. MPP hydrochloride reverses the the positive effects of beta-estradiol. MPP hydrochloride has mixed agonist/antagonist action on murine uterine ERalpha in vivo .
|
-
- HY-135783
-
AT 1001
1 Publications Verification
|
nAChR
|
Neurological Disease
|
|
AT 1001 is a high-affinity and selective antagonist of the α3β4 nicotinic acetylcholine receptor (α3β4 nAChR) (Ki=2.64 nM). AT 1001 reversibly blocks inward currents induced by Epibatidine (HY-101078) in HEK cells transfected with α3β4 nAChR. AT-1001 dose-dependently inhibits nicotine self-administration behavior in rats without affecting food-reinforced responding. AT 1001 can be utilized in the research of nicotine addiction and smoking cessation therapies .
|
-
- HY-118918
-
|
|
Vasopressin Receptor
|
Endocrinology
|
|
YM218 free base is an orally active non-peptide vasopressin (AVP) receptor antagonist. YM218 free base has a high affinity for rat liver V1A receptors with a Ki value of 0.50 nM; it has a lower affinity for rat pituitary V1B, kidney V2, and uterine oxytocin receptors with Ki values of 1510 nM, 72.2 nM, and 150 nM, respectively. YM218 free base can be used in the study of diabetes and kidney disease .
|
-
- HY-103378
-
|
|
CRFR
|
Neurological Disease
|
|
NBI 35965 methanesulfonate is a selective, orally active and brain-penetrant corticotropin-releasing factor receptor 1 (CRF1) antagonist with a Ki value of 4 nM and a pKi value of 8.5. NBI 35965 methanesulfonate does not inhibit CRF2. NBI 35965 methanesulfonate reduces CRF or stress-induced adrenocorticotropic hormone (ACTH) production in vivo with pIC50 values of 7.1 and 6.9, respectively. NBI 35965 methanesulfonate shows anxiolytic effects .
|
-
- HY-121156
-
|
LF 16-0687; XY-2405
|
Bradykinin Receptor
|
Neurological Disease
|
|
Anatibant (LF 16-0687; XY-2405) is a selective non-peptide bradykinin B2 receptor antagonist. Anatibant binds to the human, rat and guinea-pig recombinant B2 receptor with Ki values of 0.67 nM, 1.74 nM and 1.37 nM, respectively. Anatibant crosses the blood-brain barrier (BBB). Anatibant can be used in research on brain damage diseases .
|
-
- HY-121156A
-
|
LF 16-0687 hydrochloride; XY-2405 hydrochloride
|
Bradykinin Receptor
|
Neurological Disease
|
|
Anatibant (LF 16-0687; XY-2405) hydrochloride is a selective non-peptide bradykinin B2 receptor antagonist. Anatibant hydrochloride binds to the human, rat and guinea-pig recombinant B2 receptor with Ki values of 0.67 nM, 1.74 nM and 1.37 nM, respectively. Anatibant hydrochloride crosses the blood-brain barrier (BBB). Anatibant hydrochloride can be used in research on brain damage diseases .
|
-
- HY-14117
-
-
- HY-P10138
-
|
|
Insulin Receptor
|
Metabolic Disease
|
|
Human GIP(3-30), amide is a high affinity antagonist of the human GIP receptor in vitro. Human GIP(3-30), amide has potential anti-obesity and anti-diabetic effects .
|
-
- HY-100928
-
|
|
Calcium Channel
|
Neurological Disease
|
|
YS 035 hydrochloride is a Ca 2+ antagonist on cellular uptake and mitochondrial efflux of calcium ions. YS 035 hydrochloride inhibits Ca 2+ uptake by muscle cells and inhibits Na +/Ca 2+ exchange (Ki=28 µM). YS 035 hydrochloride is a useful tool for research on the mitochondrial Ca 2+ transport .
|
-
- HY-159686
-
|
|
Adrenergic Receptor
|
Inflammation/Immunology
Endocrinology
|
|
Aclidinium is a long-acting muscarinic antagonist and long-acting β2-adrenoceptor (β2-AR) agonist with bronchodilator activity. Aclidinium can reduce hyperinflation of the lungs and increase lung function and exercise endurance time. Aclidinium is used in research on chronic obstructive pulmonary disease (COPD) .
|
-
- HY-19646
-
|
480156-S
|
Bradykinin Receptor
Prostaglandin Receptor
|
Neurological Disease
|
|
Zoliprofen (480156-S), a new non-steroidal anti-inflammatory agent, has potent pain suppressing effect. Zoliprofen has strong antagonistic action against bradykinin, markedly inhibiting all bradykinin-induced edema and pain reactions. Zoliprofen weakly inhibits Arachidonic acid (HY-109590)-induced edema and pain reactions but also inhibits PGE2 synthesis of bovine vesicular gland microsomes .
|
-
- HY-10657
-
|
|
Urotensin Receptor
|
Cardiovascular Disease
Others
|
|
SB-706375 is an antagonist of the Urotensin II (UII) receptor. By blocking the Urotensin II receptor, SB-706375 reduces the kidney's response to UII and Urotensin-related peptide (URP) and significantly increases the Glomerular Filtration Rate (GFR). SB-706375 can be used in research on kidney diseases and hypertension .
|
-
- HY-106890
-
|
57G709
|
Angiotensin Receptor
PDGFR
|
Cardiovascular Disease
|
|
E4177 (57G709) is an orally active angiotensin II receptor antagonist. E4177 can inhibit the growth of vascular smooth muscle cells (HASMC) and the increase of cell surface area. In addition, E4177 can also increase the expression of platelet-derived growth factor (PDGF) receptor. E4177 can be used in the study of vascular diseases .
|
-
- HY-150751
-
|
ODN A151
|
Toll-like Receptor (TLR)
AIM2
|
Inflammation/Immunology
|
|
ODN TTAGGG (A151), inhibitory oligonucleotide (ODN), is a TLR9, AIM2 and cGAS antagonist. ODN TTAGGG is immunosuppressive and inhibits AIM2 inflammasome activation, as well as cGAS activation, by competing with DNA. ODN TTAGGG can be used in the study of lupus erythematosus and other related autoimmune diseases. ODN TTAGGG sequence: 5'-T-T-A-G-G-G-T-T-A-G-G-G-T-T-A-G-G-G-T-T-A-G-G-G-3' .
|
-
- HY-150751C
-
|
ODN A151 sodium
|
AIM2
Toll-like Receptor (TLR)
|
Inflammation/Immunology
|
|
ODN TTAGGG sodium, inhibitory oligonucleotide (ODN), is a TLR9, AIM2 and cGAS antagonist. ODN TTAGGG sodium is immunosuppressive and inhibits AIM2 inflammasome activation, as well as cGAS activation, by competing with DNA. ODN TTAGGG sodium can be used in the study of lupus erythematosus and other related autoimmune diseases. ODN TTAGGG sequence: 5'-T-T-A-G-G-G-T-T-A-G-G-G-T-T-A-G-G-G-T-T-A-G-G-G-3' .
|
-
- HY-162957
-
|
|
Bacterial
Antibiotic
|
Infection
|
|
LasR-IN-5 (compound 3C) is a LasR antagonist with an IC50 of 1.37 μM, demonstrating a 77% inhibition of biofilm formation in Pseudomonas aeruginosa. LasR-IN-5 also exhibits quorum sensing (QS) inhibition activity and has potential applications in Pseudomonas aeruginosa infection research .
|
-
- HY-17038
-
|
S-20098
|
Melatonin Receptor
5-HT Receptor
Endogenous Metabolite
|
Neurological Disease
|
|
Agomelatine (S-20098) is a specific agonist of MT1 and MT2 receptors with Kis of 0.1, 0.06, 0.12, and 0.27 nM for CHO-hMT1, HEK-hMT1, CHO-hMT2, and HEK-hMT2, respectively . Agomelatine is a selective 5-HT2C receptor antagonist with pKis of 6.4 and 6.2 at native (porcine) and cloned, human 5-HT2C receptors, respectively .
|
-
- HY-17038A
-
|
S-20098 hydrochloride
|
Melatonin Receptor
5-HT Receptor
Endogenous Metabolite
|
Neurological Disease
|
|
Agomelatine hydrochloride (S-20098 hydrochloride) is a specific agonist of MT1 and MT2 receptors with Kis of 0.1, 0.06, 0.12, and 0.27 nM for CHO-hMT1, HEK-hMT1, CHO-hMT2, and HEK-hMT2, respectively . Agomelatine hydrochloride is a selective 5-HT2C receptor antagonist with pKis of 6.4 and 6.2 at native (porcine) and cloned, human 5-HT2C receptors, respectively .
|
-
- HY-134268
-
|
8-Bromo-7-deazaadenosine-5'-O-diphosphoribose
|
TRP Channel
|
Cardiovascular Disease
Neurological Disease
Metabolic Disease
|
|
8-Br-7-CH-ADPR (8-Bromo-7-deazaadenosine-5'-O-diphosphoribose) is a specific TRPM2 antagonist that inhibits TRPM2 activation by binding to the NUDT9 homology domain of the TRPM2 channel, thereby controlling the influx of cations through the cell membrane channel. 8-Br-7-CH-ADPR can be used to study the role of TRPM2 in pathological processes such as cell death, neurodegenerative diseases, myocardial infarction, and diabetes .
|
-
- HY-120427
-
|
NSC 658586
|
CCR
CXCR
HIV
HSV
|
Infection
Inflammation/Immunology
|
|
Cosalane (NSC 658586) is a CCR7 (IC50 = 2.43 μM) and CXCR2 antagonist (IC50 = 0.66 μM). Cosalane is an inhibitor of HIV replication with a wide range of activity against HIV-1 isolates, HIV-2, Rauscher murine leukemia virus, HSV-1, HSV-2 and human cytomegalovirus. Cosalane inhibits both attachment of gp120 to CD4. Cosalane inhibits human and murine CCR7 in response to both CCL19 and CCL21 agonists. Cosalane can be studied in research for HIV or attenuating acute graft-versus-host disease (aGVHD) in allogeneic hematopoietic stem cell transplantation (HSCT) .
|
-
- HY-107744
-
-
- HY-118409
-
|
|
Androgen Receptor
|
Endocrinology
Cancer
|
|
VPC-3033 is an androgen receptor antagonist. VPC-3033 has a strong androgen DHT replacement potency (IC50: 0.625-2.5 μM), can effectively inhibit androgen receptor transcriptional activity (IC50=0.3 μM), and has a strong androgen receptor degradation ability. In addition, VPC-3033 exhibits significant anti-androgen receptor activity against prostate cancer cells resistant to Enzalutamide (HY-70002) .
|
-
- HY-B1690AR
-
|
|
Antibiotic
Bacterial
Histamine Receptor
|
Infection
|
|
Thioridazine (Standard) is the analytical standard of Thioridazine. This product is intended for research and analytical applications. Thioridazine, an antagonist of the dopamine receptor D2 family proteins, exhibits potent anti-psychotic and anti-anxiety activities. Thioridazine is also a potent inhibitor of PI3K-Akt-mTOR signaling pathways with anti-angiogenic effect. Thioridazine shows antiproliferative and apoptosis induction effects in various types of cancer cells, with specificity on targeting cancer stem cells (CSCs) .
|
-
- HY-17038B
-
|
S-20098 L(+)-Tartaric acid
|
Melatonin Receptor
5-HT Receptor
Endogenous Metabolite
|
Neurological Disease
|
|
Agomelatine L(+)-Tartaric acid (S-20098 L(+)-Tartaric acid) is a specific agonist of MT1 and MT2 receptors with Kis of 0.1, 0.06, 0.12, and 0.27 nM for CHO-hMT1, HEK-hMT1, CHO-hMT2, and HEK-hMT2, respectively . Agomelatine L(+)-Tartaric acid is a selective 5-HT2C receptor antagonist with pKis of 6.4 and 6.2 at native (porcine) and cloned, human 5-HT2C receptors, respectively .
|
-
- HY-146450
-
|
|
Bacterial
Antibiotic
|
Infection
|
|
PXYC2 is a ribosomal protein S1 (RpsA) antagonist with Kds of 6.35 and 5.11 μM for RpsA-CTD and RpsA-CTD Δ438A, respectively. RpsA plays an important role in the trans-translation process of Mycobacterium Tuberculosis (Mtb) .
|
-
- HY-146447
-
|
|
Bacterial
Antibiotic
|
Infection
|
|
PXYC13 is a ribosomal protein S1 (RpsA) antagonist with Kds of 7.61 and 8.50 μM for RpsA-CTD and RpsA-CTD Δ438A, respectively. RpsA plays an important role in the trans-translation process of Mycobacterium Tuberculosis (Mtb) .
|
-
- HY-146446
-
|
|
Bacterial
Antibiotic
|
Infection
|
|
PXYC1 is a ribosomal protein S1 (RpsA) antagonist with Kds of 0.81 and 0.31 μM for RpsA-CTD and RpsA-CTD Δ438A, respectively. RpsA plays an important role in the trans-translation process of Mycobacterium Tuberculosis (Mtb) .
|
-
- HY-146451
-
|
|
Bacterial
Antibiotic
|
Infection
|
|
PXYC12 is a ribosomal protein S1 (RpsA) antagonist with Kds of 2.67 and 4.67 μM for RpsA-CTD and RpsA-CTD Δ438A, respectively. RpsA plays an important role in the trans-translation process of Mycobacterium Tuberculosis (Mtb) .
|
-
- HY-146449
-
|
|
Bacterial
Antibiotic
|
Infection
|
|
PXYD4 is a ribosomal protein S1 (RpsA) antagonist with Kds of 3.24 and 1.64 μM for RpsA-CTD and RpsA-CTD Δ438A, respectively. RpsA plays an important role in the trans-translation process of Mycobacterium Tuberculosis (Mtb) .
|
-
- HY-17038R
-
|
S-20098 (Standard)
|
Reference Standards
Melatonin Receptor
5-HT Receptor
Endogenous Metabolite
|
Neurological Disease
|
|
Agomelatine (Standard) is the analytical standard of Agomelatine. This product is intended for research and analytical applications. Agomelatine (S-20098) is a specific agonist of MT1 and MT2 receptors with Kis of 0.1, 0.06, 0.12, and 0.27 nM for CHO-hMT1, HEK-hMT1, CHO-hMT2, and HEK-hMT2, respectively . Agomelatine is a selective 5-HT2C receptor antagonist with pKis of 6.4 and 6.2 at native (porcine) and cloned, human 5-HT2C receptors, respectively .
|
-
- HY-101198
-
|
|
Histamine Receptor
Apoptosis
|
Neurological Disease
Cancer
|
|
Clobenpropit dihydrobromide is a potent histamine H3R antagonist/inverse agonist with a pEC50 of 8.07 for histamine H3LR . Clobenpropit dihydrobromide acts as partial agonist at histamine H4 receptors (Ki 13 nM). Clobenpropit dihydrobromide also binds to serotonin 5-HT3 receptors (Ki 7.4 nM) and α2A/α2C adrenoceptors (Ki 17.4/7.8 nM) . Clobenpropit dihydrobromide increases apoptosis .
|
-
- HY-14863
-
|
CTA-018
|
VD/VDR
Cytochrome P450
|
Others
Endocrinology
|
|
Lunacalcipol (CTA-018), as a vitamin D analogue, has a dual role in the pathogenesis of Chronic Kidney Disease (CKD), as an agonist of vitamin D receptor and an antagonist of cytochrome P450 enzyme 24-hydroxylase. Lunacalcipol binds to VDR and regulates transcriptional activity of VDR by influencing ligand binding affinity, ligand-dependent coactivator recruitment or inhibitory factor dissociation, efficiency of ligand entry into target cells, tissue specificity and different metabolism of ligand. Lunacalcipol can be used in the study of CKD, especially Secondary Hyperparathyroidism (sHPT) .
|
-
- HY-137955
-
|
|
P2Y Receptor
|
Cardiovascular Disease
Others
Neurological Disease
|
|
MRS 2211 sodium hydrate is a competitive P2Y13 receptor antagonist (pIC50= 5.97). MRS 2211 sodium hydrate is highly selective to the P2Y13 receptor, showing more than 20-fold selectivity compared to the P2Y1 and P2Y12 receptors. MRS 2211 sodium hydrate can be used to further investigate the role of the P2Y13 receptor in different physiological and pathological processes, such as its function in blood cells, the nervous system and the immune system .
|
-
- HY-P991049
-
|
ATM-001
|
TNF Receptor
|
Inflammation/Immunology
|
|
Atrosimab (ATM-001) is a Fv-Fc1κ fusion protein with strong binding to human TNFR1 with an EC50 value of 0.37 nM. Atrosimab potently inhibits TNF-induced activation of TNFR1. Atrosimab has the potential for the study of chronic inflammatory diseases .
|
-
- HY-19037
-
-
- HY-145258
-
|
|
GABA Receptor
|
Neurological Disease
|
|
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 .
|
-
- HY-108608
-
|
|
Calcium Channel
|
Others
|
|
o-3M3FBS is the negative control of m-3M3FBS. o-3M3FBS inhibits inward and outward currents via mechanisms independent of PLC acting in an antagonistic manner. In contrast, o-3M3FBS also causes an increase in [Ca 2+]i in an agonistic manner .
|
-
- HY-120767
-
|
KLH-2109 choline; OBE-2109 choline
|
GnRH Receptor
|
Inflammation/Immunology
Cancer
|
|
Linzagolix choline (KLH-2109 choline) is a non-peptide gonadotropin-releasing hormone (GnRH) antagonist with oral activity. Linzagolix choline inhibits the release of endogenous gonadotropins such as luteinizing hormone LH and follicle-stimulating hormone FSH by binding to the GnRH receptor within the pituitary gland. This inhibition results in a reduction in the production of sex hormones such as estrogen and progesterone, which in turn affects the course of sex hormone-dependent diseases. Linzagolix choline can be used in the study of sex hormone-dependent diseases such as endometriosis and uterine fibroids .
|
-
- HY-136702
-
|
|
Adenosine Receptor
|
Inflammation/Immunology
|
|
L-97-1 is a A1 adenosine receptor (A1AR) antagonist. L-97-1 is a water-soluble small molecule compound with high affinity and high selectivity against human A1 adenosine receptors. L-97-1 works by blocking A1 adenosine receptors. In patients with asthma, adenosine is an important signaling molecule capable of causing bronchoconstriction by activating A1AR. L-97-1 reduces airway hyperreactivity (BHR) by competitively binding to A1AR, thereby alleviating or blocking adenosine-induced bronchoconstriction and inflammation .
|
-
- HY-12709A
-
|
|
Adrenergic Receptor
|
Cardiovascular Disease
Inflammation/Immunology
|
|
ARC 239 dihydrochloride is a selective α2B/2C adrenoceptor antagonist (pKd values are 5.95, 7.41 and 7.56 at α2A, α2B, and α2C receptors respectively). ARC 239 dihydrochloride binds to CHO cell membranes expressing human recombinant a2A-, a2B- or a2C-adrenoceptor subtypes with pKis of 5.6, 8.4, and 7.08, respectively .
|
-
- HY-147560
-
|
|
Sigma Receptor
Opioid Receptor
|
Neurological Disease
|
|
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 .
|
-
- HY-110099
-
|
|
CXCR
|
Inflammation/Immunology
|
|
(±)-NBI-74330 is a potent and selective CXCR3 antagonist. (±)-NBI-74330 not only reduces tactile and thermal hypersensitivity but also enhances the analgesic properties of morphine. (±)-NBI-74330 can reduce microglial cell activation, increase astroglial cell activation, and downregulate the expression of some CXCR3 ligands in a rat neuropathic pain model .
|
-
- HY-P10388
-
|
|
CD47
TGF-β Receptor
|
Cancer
|
|
TAX2 peptide is a dodecapeptide based on molecular docking and simulation design, derived from the cell surface receptor CD47 sequence. TAX2 peptide acts as a selective antagonist of TSP-1 (thromboxin-1) interacting with CD47. TAX2 peptide can promote the binding of TSP-1 to CD36, which leads to the destruction of VEGFR2 (vascular endothelial growth factor receptor 2) activation, thereby blocking downstream NO (nitric oxide) signaling, demonstrating anti-angiogenic properties. TAX2 peptide can be used to study angiogenesis and tumor cell interactions in the tumor microenvironment .
|
-
- HY-173640
-
|
|
Androgen Receptor
Phosphodiesterase (PDE)
|
Cancer
|
|
ID11916 is an orally active androgen receptor (AR) antagonist and a phosphodiesterase 5 (PDE5) inhibitor. ID11916 blocks androgen binding to AR, nuclear translocation, and androgen-dependent transcriptional activity of AR, while increasing intracellular cGMP levels and activating PKG via inhibition. ID11916 shows potent anti-cancer effect in prostate cancer cell lines VCaP and 22Rv1 and in AR-positive breast cancer cell lines SK-BR-3 .
|
-
- HY-P10138A
-
|
|
Insulin Receptor
|
Metabolic Disease
|
|
Human GIP(3-30), amide TFA is the TFA salt form of human GIP(3-30), amide (HY-P10138). Human GIP(3-30), amide TFA is a high affinity antagonist of the human GIP receptor in vitro. Human GIP(3-30), amide TFA has potential anti-obesity and anti-diabetic effects .
|
-
- HY-P3248
-
|
Myelin basic protein (85-99) antagonist
|
Biochemical Assay Reagents
|
Inflammation/Immunology
|
|
J5 peptide is an MBP inhibitor that competitively inhibits the binding of MBP85-99 to HLA-DR2. J5 peptide alleviates PLP139-151/MBP85-99-induced experimental autoimmune encephalomyelitis (EAE) in mice. J5 peptide can be used in research on inflammatory and immune diseases .
|
-
- HY-N6932
-
|
|
Cannabinoid Receptor
P-glycoprotein
PI3K
Akt
mTOR
Apoptosis
Autophagy
EGFR
|
Metabolic Disease
Cancer
|
|
Voacamine is an indole alkaloid with cannabinoid 1 (CB1) antagonistic activity. Voacamine can inhibit nuclear translocation. Voacamine is effective in enhancing the effect of Doxorubicin (HY-15142A) as it interferes with the P-glycoprotein (P-gp) function. Voacamine promotes apoptosis-independent autophagic cell death in human osteosarcoma cells. Voacamine activates mitochondrial-associated apoptosis signaling pathway and inhibition of PI3K/Akt/mTOR signaling pathway to suppress breast cancer progression. Voacamine inhibits EGFR to exert oncogenic activity against colorectal cancer .
|
-
- HY-101283
-
HCH6-1
3 Publications Verification
|
Formyl Peptide Receptor (FPR)
|
Inflammation/Immunology
|
|
HCH6-1 is a potent and competitive dipeptide antagonist of Formyl peptide receptor 1 (FPR1). HCH6-1 inhibits chemotaxis, superoxide anion generation, and elastase release in human neutrophils specifically activated by fMLF (an FPR1 agonist). HCH6-1 has protective effects against acute lung injury (ALI) in vivo and can be used for the research of FPR1-involved inflammatory lung diseases .
|
-
- HY-148494
-
|
FLX475
|
CCR
|
Inflammation/Immunology
Cancer
|
|
Tivumecirnon (FLX475) is an orally active, selective CCR4 antagonist. Tivumecirnon blocks the binding of CCR4 to its ligands, CCL17 and CCL22, thereby reducing Treg infiltration into the tumor microenvironment. Tivumecirnon has antitumor activity .
|
-
- HY-P3678
-
|
|
Neuropeptide Y Receptor
|
Cardiovascular Disease
Neurological Disease
|
|
Neuropeptide Y (18-36) (porcine) is a competitive neuropeptide Y (NPY) cardiac receptor antagonist. Neuropeptide Y (18-36) (porcine) inhibits the binding of I-NPY to cardiac ventricular membranes in a concentration-dependent manner with an IC50 value of 158 nM and an Ki value of 140 nM. Neuropeptide Y (18-36) (porcine) can be used for the research of congestive heart failure .
|
-
- HY-115450
-
|
|
LPL Receptor
|
Endocrinology
Cancer
|
|
ONO-0300302 is an orally active and potent LPA1 (lysophosphatidic acid receptor 1) antagonist, with an IC50 of 0.086 μM. ONO-0300302 is a slow tight binding inhibitor, and its binding affinity increases with time, with Kd of 0.34 nM (37 °C, 2 h). ONO-0300302 can be used for benign prostatic hyperplasia (BPH) research .
|
-
- HY-105168
-
|
|
Endothelin Receptor
|
Cardiovascular Disease
|
|
TAK 044 is an antagonist of Endothelin Receptor. TAK 044 strongly inhibits ET-induced deterioration in various animal models. TAK 044 can be used in study ET-related diseases such as acute myocardial infarction,acute renal failure, acute hepatic malfunction, and subarachnoid hemorrhage .
|
-
- HY-100920
-
-
- HY-145906
-
|
|
Dopamine Receptor
|
Neurological Disease
|
|
D4R antagonist-2 is a potent and selective D4R antagonist with an IC50 of 6.52 µM. D4R antagonist-2 displays very favorable in vitro PK parameters and has good brain penetration. D4R antagonist-2 has the potential for the research of Parkinson’s disease .
|
-
- HY-155406
-
|
|
Estrogen Receptor/ERR
Caspase
Bcl-2 Family
|
Cancer
|
|
Estrogen receptor modulator 10 (compound G-5b) is an estrogen receptor (ER) antagonist (IC50=6.7 nM) and degrader (DC50=0.4 nM). Estrogen receptor modulator 10 is developed based on the Fulvestrant (HY-13636) molecule and can rapidly degrade ER receptors through the proteasome pathway. Estrogen receptor modulator 10 can induce cell apoptosis and block cells in the G1/G0 phase and can be used in cancer research .
|
-
- HY-P99483
-
|
AT 004; VT 007
|
CD20
Adenosine Receptor
|
Cancer
|
|
Blontuvetmab (AT 004) is a caninized CD20 monoclonal antibody and is also a potent, selective, highly potent antagonist of A2aR receptor. Blontuvetmab behaves as Nociceptin (HY-P0183)/Orphanin (HY-P0183) FQ receptor (NOP) agonists displaying weak NOP affinity. Blontuvetmab inhibits 5'-N-Ethylcarboxamidoadenosine (NECA)-mediated A2aR activation and significantly reverses the ability of adenosine to suppress CD8 T cell activation, increasing levels of cytokines such as IFN-γ. Blontuvetmab Blontuvetmab can be used for the research of Canine B-cell lymphoma .
|
-
- HY-117132
-
|
|
mGluR
|
Neurological Disease
|
|
YM-202074 is a selective, allosteric metabotropic glutamate receptor type 1 (mGluR1) antagonist with high affinity. YM-202074 binds to the allosteric site of rat mGluR1 with a Ki of 4.8 nM. YM-202074 fumarate also inhibits mGluR1-mediated inositol phosphate production in rat cerebellar granule cells with an IC50 of 8.6 nM. YM-202074 has potent neuroprotective effects in transient MCA (tMCA) occlusion rat models .
|
-
- HY-103556
-
|
|
mGluR
|
Neurological Disease
|
|
YM-202074 fumarate is a selective, allosteric metabotropic glutamate receptor type 1 (mGluR1) antagonist with high affinity. YM-202074 fumarate binds to the allosteric site of rat mGluR1 with a Ki of 4.8 nM. YM-202074 fumarate also inhibits mGluR1-mediated inositol phosphate production in rat cerebellar granule cells with an IC50 of 8.6 nM. YM-202074 fumarate has potent neuroprotective effects in transient MCA (tMCA) occlusion rat models .
|
-
- HY-119873
-
|
REV 5320
|
NO Synthase
Adrenergic Receptor
|
Cardiovascular Disease
|
|
Celiprolol (REV 5320) is a potent, cardioselective and orally active β1-andrenoceptor r antagonist with partial β2 agonist activity, with Ki values of 0.14-8.3 μM. Celiprolol has antihypertensive and antianginal activity, and can be used for the research of cardiovascular disease such as high blood pressure .
|
-
- HY-B1264
-
|
|
NO Synthase
Adrenergic Receptor
|
Cardiovascular Disease
|
|
Celiprolol (REV 5320) is a potent, cardioselective and orally active β1-andrenoceptor r antagonist with partial β2 agonist activity, with Ki values of 0.14-8.3 μM. Celiprolol has antihypertensive and antianginal activity, and can be used for the research of cardiovascular disease such as high blood pressure .
|
-
- HY-W007511
-
|
Isohexanol; Isohexyl alcohol
|
Biochemical Assay Reagents
|
Neurological Disease
|
|
4-Methyl-1-pentanol is a volatile aroma component of red wine, which is often used in the production and blending of wine. 4-Methyl-1-pentanol can also be used as an alcohol antagonist to antagonize the effects of ethanol and 1-butanol on cell-cell adhesion, and is used in the study of fetal alcohol syndrome .
|
-
- HY-117694
-
|
|
CGRP Receptor
|
Neurological Disease
Inflammation/Immunology
|
|
MK-8825 is an orally active, potent and selective CGRP receptor antagonist, which shows concentration-dependent inhibition of Capsaicin (HY-10448)-evoked dermal blood flow with an EC50 value of about 7.4 μM. MK-8825 inhibits CGRP-induced spontaneous nociceptive facial grooming behaviors, neuronal activation in the trigeminal nucleus, and systemic release of pro-inflammatory cytokines in a mouse model of acute orofacial masseteric muscle pain. MK-8825 is promising for research of acute migraine .
|
-
- HY-P5175
-
|
|
mAChR
|
Neurological Disease
|
|
Muscarinic toxin 7 is a peptide toxin with selective and noncompetitive antagonism at the muscarinic M1 receptor .
|
-
- 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-12882
-
|
NP-120; RC-61-91
|
iGluR
Adrenergic Receptor
Potassium Channel
Calcium Channel
Influenza Virus
|
Infection
Neurological Disease
|
|
Ifenprodil (NP-120), a cerebral vasodilator, is a noncompetitive NMDA receptor antagonist. Ifenprodil exerts high affinity at NR1A/NR2B receptors (IC50=0.34 μM) over 400-fold than at NR1A/NR2A receptors (IC50=146 μM) . Ifenprodil is an α1 adrenergic receptor antagonist. Ifenprodil inhibits GIRK (Kir3), reduces inward currents through the basal GIRK activity. Ifenprodil has reliable inhibitory effects against A/H1N1 strains (EC50 of 6.6 µM). Ifenprodil has neuroprotective, anticonvulsant and antinociceptive effects. Ifenprodil can be used for the study of cerebrovascular diseases and peripheral arterial obliterative disease .
|
-
- HY-B1264R
-
|
|
NO Synthase
Adrenergic Receptor
|
Cardiovascular Disease
|
|
Celiprolol (hydrochloride) (Standard) is the analytical standard of Celiprolol (hydrochloride). This product is intended for research and analytical applications. Celiprolol (REV 5320) is a potent, cardioselective and orally active β1-andrenoceptor r antagonist with partial β2 agonist activity, with Ki values of 0.14-8.3 μM. Celiprolol has antihypertensive and antianginal activity, and can be used for the research of cardiovascular disease such as high blood pressure .
|
-
- HY-N3478
-
|
Hydroxycoriatin
|
GABA Receptor
|
Neurological Disease
|
|
Isohyenanchin (Hydroxycoriatin) is an RDLac homo-oligomers antagonist. Isohyenanchin also is a weak antagonist of ionotropic GABA receptors .
|
-
- HY-110209
-
|
|
TRP Channel
|
Others
|
|
AC4 is a trans antagonist upon voltageactivation of TRPV1 and as cis antagonist of TRPV1 currents upon stimulation with Capsaicin (HY-10448). AC4 demonstrates that a photoswitchable antagonist and an agonist can be used in concert .
|
-
- HY-12882A
-
|
NP-120 tartrate; RC-61-91 tartrate
|
iGluR
Adrenergic Receptor
Potassium Channel
Calcium Channel
Influenza Virus
|
Infection
Neurological Disease
|
|
Ifenprodil (NP-120) tartrate, a cerebral vasodilator, is a noncompetitive NMDA receptor antagonist. Ifenprodil tartrate exerts high affinity at NR1A/NR2B receptors (IC50=0.34 μM) over 400-fold than at NR1A/NR2A receptors (IC50=146 μM) . Ifenprodil tartrate is an α1 adrenergic receptor antagonist. Ifenprodil tartrate inhibits GIRK (Kir3), reduces inward currents through the basal GIRK activity. Ifenprodil tartrate has reliable inhibitory effects against A/H1N1 strains (EC50 of 6.6 µM). Ifenprodil tartrate has neuroprotective, anticonvulsant and antinociceptive effects. Ifenprodil tartrate can be used for the study of cerebrovascular diseases and peripheral arterial obliterative disease .
|
-
- HY-A0033
-
|
UK-88525
|
mAChR
p38 MAPK
Akt
|
Neurological Disease
Metabolic Disease
Cancer
|
|
Darifenacin (UK-88525) is a selective and orally active M3 muscarinic receptor (M3R) antagonist with a pKi of 8.9. Darifenacin binds >20-fold more specifically to M3R than to other muscarinic receptors. Darifenacin can be used in the study of urinary incontinence and other symptoms of overactive bladder. Darifenacin inhibits tumor growth in colorectal cancer cells and has anti-tumor effects .
|
-
- HY-125046
-
|
|
LPL Receptor
|
Others
|
|
CYM50374 is a potent antagonist sphingosine-1-phosphate 4 (S1P4) antagonists, with the IC50 of 34 nM .
|
-
- HY-103134
-
|
|
5-HT Receptor
|
Inflammation/Immunology
|
|
5-HT4 antagonist 3 hydrochloride is a highly selective 5-hydroxytryptamine receptor (5-HT4) antagonist. 5-HT4 antagonist 3 (hydrochloride) blocks muscarine receptors and sodium channels. 5-HT4 antagonist 3 (hydrochloride) can be used to evaluate function of 5-HT4 receptor .
|
-
- HY-110206
-
|
|
Cannabinoid Receptor
|
Metabolic Disease
|
|
AM6545 is a highly selective, brain-free (peripherally active) CB1 receptor antagonist (Ki=1.7 nM). AM6545 inhibits endocannabinoid signaling by competitively antagonizing CB1 receptors, inhibiting CB1-mediated appetite stimulation and inflammatory responses without affecting cAMP levels. AM6545 significantly reduces food intake and body weight in mice, while improving metabolic syndrome-related renal impairment (such as proteinuria, fibrosis) and insulin resistance. AM6545 can be used in the study of obesity and its complications .
|
-
- HY-A0012
-
|
UK-88525 hydrobromide
|
mAChR
p38 MAPK
Akt
|
Neurological Disease
Metabolic Disease
Cancer
|
|
Darifenacin (UK-88525) hydrobromide is a selective and orally active M3 muscarinic receptor (M3R) antagonist with a pKi of 8.9. Darifenacin hydrobromide binds >20-fold more specifically to M3R than to other muscarinic receptors. Darifenacin hydrobromide can be used in the study of urinary incontinence and other symptoms of overactive bladder. Darifenacin hydrobromide inhibits tumor growth in colorectal cancer cells and has anti-tumor effects .
|
-
- HY-15540
-
-
- HY-22437S
-
-
- HY-N10754
-
|
|
mTOR
Cytochrome P450
|
Infection
Cardiovascular Disease
Cancer
|
|
Aschantin, a bisepoxylignan, can be isolated from Magnolia biondii. Aschantin has antiplasmodial, Ca 2+-antagonistic, platelet activating factor-antagonistic, and chemopreventive activities. Aschantin is a mTOR kinase inhibitor. Aschantin is also an inhibitor of Cytochrome P450 and UGT enzyme .
|
-
- HY-22437S1
-
-
- HY-17403
-
|
CV-4093
|
Calcium Channel
NF-κB
|
Infection
Cardiovascular Disease
Metabolic Disease
Inflammation/Immunology
|
|
Manidipine dihydrochloride is a third-generation, lipophilic, orally active and highly vasoselective calcium channel antagonist (IC50 = 2.6 nM in guinea-pig ventricular cells) and acts as an antihypertensive agent. Manidipine effectively reduces blood pressure as well as improving insulin sensitivity, renal protection, and antiatherosclerotic activity. Manidipine also exerts anti-inflammatory activity mediated by NF-κB and antiviral activity against many flavivirus and negative-strand RNA viruses through the inhibition of calcium channel. Manidipine is widely applied to research of cardiovascular, metabolic disease and infection .
|
-
- HY-120926
-
|
|
Calcium Channel
|
Others
|
|
BBR 2160 is a compound with cardiac electrophysiological effects and is a dihydropyridine calcium antagonist that can reduce myocardial contractility and action potential duration and has calcium antagonist properties.
|
-
- HY-14656S
-
|
|
Calcium Channel
|
Cardiovascular Disease
|
|
Diltiazem-d3 (hydrochloride) is the deuterium labeled Diltiazem hydrochloride. Diltiazem hydrochloride is a Ca2+ influx inhibitor (slow channel blocker or calcium antagonist)[1][2].
|
-
- HY-107716
-
|
|
iGluR
|
Neurological Disease
|
|
Ro 8-4304 hydrochloride is a potent NMDA receptor antagonist. Ro 8-4304 hydrochloride is a NR2B selective, non-competitive, voltage-independent antagonist .
|
-
- HY-147280
-
|
GP-2250
|
Apoptosis
|
Cancer
|
|
Misetionamide is an orally oxathiazin-like compound. Misetionamide is a glyceraldehyde-3-phosphate dehydrogenase (GAPDH) inhibitor with antineoplastic activity. Misetionamide can be used for the research of cancer .
|
-
- HY-156876
-
|
|
Cytochrome P450
|
Metabolic Disease
|
|
20-HETE inhibitor-2 is an orally active 20-HETE inhibitor. 20-HETE inhibitor-2 can inhibit the activities of CYP4F2 and CYP4A11, thereby suppressing the production of 20-HETE. 20-HETE inhibitor-2 has the effect of improving blood glucose and can be used for the research of various diseases related to 20-HETE such as obesity .
|
-
- HY-134983
-
-
- HY-10341
-
|
HA-1077 Hydrochloride; AT-877 Hydrochloride
|
ROCK
Calcium Channel
Autophagy
PKA
PKC
HIV
|
Cancer
|
|
Fasudil (HA-1077; AT877) Hydrochloride is a nonspecific RhoA/ROCK inhibitor and also has inhibitory effect on protein kinases, with an Ki of 0.33 μM for ROCK1, IC50s of 0.158 μM and 4.58 μM, 12.30 μM, 1.650 μM for ROCK2 and PKA, PKC, PKG, respectively. Fasudil Hydrochloride is also a potent Ca 2+ channel antagonist and vasodilator .
|
-
- HY-10341C
-
|
HA-1077 dihydrochloride; AT-877 dihydrochloride
|
Calcium Channel
ROCK
PKA
PKC
Autophagy
HIV
|
Cancer
|
|
Fasudil (HA-1077; AT877) dihydrochloride is a nonspecific RhoA/ROCK inhibitor and also has inhibitory effect on protein kinases, with an Ki of 0.33 μM for ROCK1, IC50s of 0.158 μM and 4.58 μM, 12.30 μM, 1.650 μM for ROCK2 and PKA, PKC, PKG, respectively. Fasudil dihydrochloride is also a potent Ca 2+ channel antagonist and vasodilator .
|
-
- HY-10341A
-
|
HA-1077; AT877
|
ROCK
Calcium Channel
Autophagy
PKA
PKC
|
Cancer
|
|
Fasudil (HA-1077; AT877) is a nonspecific RhoA/ROCK inhibitor and also has inhibitory effect on protein kinases, with an Ki of 0.33 μM for ROCK1, IC50s of 0.158 μM and 4.58 μM, 12.30 μM, 1.650 μM for ROCK2 and PKA, PKC, PKG, respectively. Fasudil is also a potent Ca 2+ channel antagonist and vasodilator .
|
-
- HY-15277
-
-
- HY-14656S1
-
-
- HY-101685A
-
-
- HY-100248
-
-
- HY-U00067
-
-
- HY-101685
-
-
- HY-114427
-
NS-102
1 Publications Verification
|
iGluR
|
Neurological Disease
|
|
NS-102 is a selective kainate (GluK2) receptor antagonist. NS-102 is a potent GluR6/7 receptor antagonist .
|
-
- HY-19705
-
-
- HY-12195
-
-
- HY-A0012R
-
|
UK-88525 (hydrobromide) (Standard)
|
mAChR
p38 MAPK
Akt
|
Neurological Disease
Metabolic Disease
Cancer
|
|
Darifenacin (hydrobromide) (Standard) is the analytical standard of Darifenacin (hydrobromide). This product is intended for research and analytical applications. Darifenacin (hydrobromide) is a selective and orally active M3 muscarinic receptor (M3R) antagonist with a pKi of 8.9. Darifenacin (hydrobromide) binds >20-fold more specifically to M3R than to other muscarinic receptors. Darifenacin (hydrobromide) can be used in the study of urinary incontinence and other symptoms of overactive bladder. Darifenacin (hydrobromide) inhibits tumor growth in colorectal cancer cells and has anti-tumor effects .
|
-
- HY-10341B
-
|
HA-1077 hydrochloride semihydrate; AT877 hydrochloride semihydrate
|
ROCK
Calcium Channel
Autophagy
HIV
PKA
PKC
|
Cancer
|
|
Fasudil (HA-1077; AT877) hydrochloride semihydrate is a nonspecific RhoA/ROCK inhibitor and also has inhibitory effect on protein kinases, with an Ki of 0.33 μM for ROCK1, IC50s of 0.158 μM and 4.58 μM, 12.30 μM, 1.650 μM for ROCK2 and PKA, PKC, PKG, respectively. Fasudil hydrochloride semihydrate is also a potent Ca 2+ channel antagonist and vasodilator .
|
-
- HY-19818A
-
-
- HY-10308
-
|
|
Others
|
Metabolic Disease
|
|
Lefradafiban is an orally active glycoprotein IIb/IIIa receptor antagonist. Lefradafiban can be metabolized to its active form, Fradafiban, a non-peptide GP IIb/IIIa receptor antagonist .
|
-
- HY-P10588
-
|
|
Neurokinin Receptor
|
Others
|
|
WIN 66306 is a cyclic heptapeptide that can be isolated from an Aspergillus species. WIN 66306 is a neurokinin antagonist with antagonistic effects on both NK1 and NK2 receptors .
|
-
- HY-19705B
-
-
- HY-19223
-
-
- HY-112067
-
-
- HY-147273
-
-
- HY-172433
-
-
- HY-B1547A
-
-
- HY-100266
-
-
- HY-109196
-
-
- HY-101658A
-
-
- HY-101817
-
-
- HY-U00017
-
-
- HY-112067A
-
-
- HY-14277A
-
|
R 50547 hydrochloride
|
Histamine Receptor
Neurotensin Receptor
Integrin
|
Inflammation/Immunology
|
|
Levocabastine (R 50547) hydrochloride is a potent and selective histamine H1-receptor antagonist. Levocabastine hydrochloride is also a selective, high affinity neurotensin receptor subtype 2 (NTR2) antagonist, with a Ki of 17 nM for mNTR2. Levocabastine hydrochloride can act as a VLA-4 antagonist, interferes with conjunctival eosinophil infiltration in allergic conjunctivitis (AC) .
|
-
- HY-14277
-
|
R 50547
|
Histamine Receptor
Neurotensin Receptor
Integrin
|
Inflammation/Immunology
|
|
Levocabastine (R 50547) is a potent and selective histamine H1-receptor antagonist. Levocabastine hydrochloride is also a selective, high affinity neurotensin receptor subtype 2 (NTR2) antagonist, with a Ki of 17 nM for mNTR2. Levocabastine can act as a VLA-4 antagonist, interferes with conjunctival eosinophil infiltration in allergic conjunctivitis (AC) .
|
-
- HY-A0019
-
|
9-Hydroxyrisperidone
|
Drug Metabolite
Dopamine Receptor
5-HT Receptor
Adrenergic Receptor
|
Neurological Disease
|
|
Paliperidone (9-Hydroxyrisperidone), the major active metabolite of Risperidone, is a dopamine D2 antagonist and 5-HT2A antagonist. Paliperidone is also active as an antagonist at α1 and α2 adrenergic receptors and H1-histaminergic receptors. Paliperidone, a antipsychotic agent, shows efficacy against schizophrenia .
|
-
- HY-B1808
-
|
|
Histamine Receptor
|
Infection
|
|
Triprolidine is an orally active H1R Antagonist antagonist. Triprolidine has the function of spinal cord motor and sensory block. Triprolidine can be used for the research of allergic rhinitis .
|
-
- 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-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-145611
-
-
- HY-13242
-
|
LY2940680
|
Smo
|
Cancer
|
|
Taladegib (LY2940680) is an antagonist of the smoothened receptor.
|
-
- HY-147294
-
-
- HY-15372
-
-
- HY-106910
-
-
- HY-100280
-
-
- HY-P10227
-
-
- HY-15070
-
-
- HY-B1589A
-
-
- HY-101574
-
-
- HY-101594
-
-
- HY-U00062
-
-
- HY-101675
-
-
- HY-101707
-
-
- HY-105117
-
-
- HY-121146
-
-
- HY-B0561
-
|
SC9420
|
Mineralocorticoid Receptor
Androgen Receptor
Autophagy
Calcium Channel
|
Cardiovascular Disease
Metabolic Disease
Endocrinology
Cancer
|
|
Spironolactone is an aldosterone antagonist that acts on the aldosterone mineralocorticoid receptor (IC50=24 nM) and androgen receptor (IC50=77 nM), promotes podocyte autophagy and regulates pain. Spironolactone improves hypertension-related vascular hypertrophy and remodeling by reducing angiotensin II (Ang II)-induced inflammation, reduces aldosterone-induced vascular and soft tissue calcification through PIT1-dependent signaling, and alleviates vascular dysfunction in type II diabetic mice by reducing oxidative stress and restoring NO/GC signaling; at low concentrations, it and its metabolites can interfere with aldosterone biosynthesis in the adrenal cortex and inhibit voltage-dependent Ca 2+ channels to exert antihypertensive effects .
|
-
- HY-10341R
-
|
|
ROCK
Calcium Channel
Autophagy
PKA
PKC
HIV
|
Cancer
|
|
Fasudil (Hydrochloride) (Standard) is the analytical standard of Fasudil (Hydrochloride). This product is intended for research and analytical applications. Fasudil (HA-1077; AT877) Hydrochloride is a nonspecific RhoA/ROCK inhibitor and also has inhibitory effect on protein kinases, with an Ki of 0.33 μM for ROCK1, IC50s of 0.158 μM and 4.58 μM, 12.30 μM, 1.650 μM for ROCK2 and PKA, PKC, PKG, respectively. Fasudil Hydrochloride is also a potent Ca 2+ channel antagonist and vasodilator .
|
-
- HY-N2304A
-
|
|
Opioid Receptor
|
Inflammation/Immunology
|
|
Methyl-6-alpha-Naltrexol is a metabolite of Methylnaltrexone (MNTX). Methylnaltrexone is a selective mu-opioid receptor antagonist and functions as a peripherally acting receptor antagonist in tissues of the gastrointestinal tract .
|
-
- HY-102086
-
|
|
Adenosine Receptor
|
Neurological Disease
|
|
MSX3 is a potent antagonist of adenosine A2A that can reverse the effects of the dopamine antagonist Haloperidol (HY-14538) on effort-related decision making in a T-maze cost/benefit procedure .
|
-
- HY-106415
-
|
|
Calcium Channel
|
Neurological Disease
|
|
Terflavoxate is a flavone derivative with spasmolytic properties. Terflavoxate has Ca 2+-antagonistic effect is mainly responsible for Terflavoxate smooth muscle relaxant properties. Terflavoxate has the potential for overactive detrusor research .
|
-
- HY-107748A
-
|
5'-GNTI TFA
|
Endogenous Metabolite
|
Neurological Disease
|
|
5'-Guanidinonaltrindole TFA is a selective kappa-opioid receptor antagonist with significant opioid antagonist activity. 5'-Guanidinonaltrindole TFA exhibits 5 times the antagonistic potency of the prototypical kappa-opioid receptor antagonist norbinatorphimine in smooth muscle preparations, with a selectivity ratio exceeding 500 times. Binding and functional studies of 5'-Guanidinonaltrindole TFA showed pA(2) values comparable to smooth muscle data. 5'-Guanidinonaltrindole TFA is regarded as a potentially valuable pharmacological tool for studying opioids due to its high selectivity and potency .
|
-
- HY-106561
-
-
- HY-U00245
-
-
- HY-101534
-
-
- HY-156614
-
-
- HY-U00247
-
-
- HY-B0768A
-
-
- HY-145610
-
-
- HY-156907
-
-
- HY-13202
-
|
|
PPAR
|
Cancer
|
|
T0070907 is a potent PPARγ antagonist with a Ki of 1 nM.
|
-
- HY-U00202
-
-
- HY-B1589
-
-
- HY-100173
-
-
- HY-100903
-
|
nor-Binaltorphimine dihydrochloride; nor-BNI dihydrochloride
|
Opioid Receptor
|
Neurological Disease
|
|
Norbinaltorphimine dihydrochloride is a potent and selective κ opioid receptor antagonist.
|
-
- HY-172244
-
-
- HY-172434
-
-
- HY-B1165
-
-
- HY-P2057
-
-
- HY-U00110
-
-
- HY-105257
-
-
- HY-N14304
-
-
- HY-P0257
-
-
- HY-103531
-
-
- HY-B0325
-
-
- HY-U00119
-
-
- HY-101691
-
-
- HY-B0768
-
-
- HY-B1303A
-
-
- HY-13209
-
-
- HY-B2154
-
-
- HY-P2612A
-
|
|
TNF Receptor
|
Others
Cancer
|
|
WP9QY, TNF-a Antagonist, TNF-a Antagonist is a biological active peptide. (This cyclic peptide is designed to mimic the most critical tumor necrosis factor (TNF) recognition loop on TNF receptor I. It prevents interactions of TNF with its receptor. This TNF antagonist is a useful template for the development of small molecular inhibitors to prevent both inflammatory bone destruction and systemic bone loss in rheumatoid arthritis.)
|
-
- HY-P2612
-
|
|
TNF Receptor
|
Others
|
|
WP9QY, TNF-a Antagonist, TNF-a Antagonist is a biological active peptide. (This cyclic peptide is designed to mimic the most critical tumor necrosis factor (TNF) recognition loop on TNF receptor I. It prevents interactions of TNF with its receptor. This TNF antagonist is a useful template for the development of small molecular inhibitors to prevent both inflammatory bone destruction and systemic bone loss in rheumatoid arthritis.)
|
-
- HY-100798
-
|
|
GABA Receptor
|
Neurological Disease
|
|
Phaclofen is a selective GABAB receptor antagonist. Phaclofen is a peripheral and central baclofen antagonist. Phaclofen maybe a potential compound in determining the physiological significance of central and peripheral bicuculline-insensitive receptors with which GABA and (-)-baclofen interact .
|
-
- HY-113730
-
|
|
CXCR
|
Others
|
|
VUF5834 is a non-peptide chemokine receptor CXCR3 antagonist with non-competitive antagonistic and inverse agonistic activities. VUF5834 blocks the effects of CXCL10 and CXCL11 on human CXCR3, exhibits non-competitive antagonistic and inverse agonistic properties to CXCR3, and, except for TAK-779, has a slightly lower affinity for rodent CXCR3 than for primate CXCR3.
|
-
- 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-157312
-
|
|
Cannabinoid Receptor
|
Metabolic Disease
|
|
CB1 antagonist 4 is a inverse agonist of cannabinoid receptor 1 (CB1) with an IC50 of 0.4 nM. CB1 antagonist 4 can reduce body weight, improve plasma inflammatory markers and glucose homeostasis .
|
-
- HY-112730
-
PEO-IAA
5 Publications Verification
2-(1H-Indol-3-yl)-4-oxo-4-phenyl-butyric acid
|
Others
|
Others
|
|
PEO-IAA is an indole-3-acetic acid (IAA) antagonist. PEO-IAA is an auxin antagonist that binds to transport inhibitor response 1/auxin signaling F-box proteins (TIR1/AFBs).
|
-
- HY-134081
-
|
|
mAChR
|
Others
|
|
Desiodomethyl 4-DAMP is a muscarinic receptor antagonist .
|
-
- HY-12377
-
-
- HY-159842
-
-
- HY-B1438
-
-
- HY-N2079
-
-
- HY-118314
-
-
- HY-N6628
-
-
- HY-U00056
-
-
- HY-U00234
-
-
- HY-100255
-
-
- HY-110110
-
-
- HY-U00139
-
-
- HY-145553
-
-
- HY-152856
-
-
- HY-U00350
-
-
- HY-A0250
-
-
- HY-B2168
-
-
- HY-112620
-
-
- HY-100814
-
-
- HY-159832
-
-
- HY-100966
-
-
- HY-107602
-
-
- HY-B1303
-
-
- HY-100668
-
-
- HY-D0965
-
-
- HY-129231
-
-
- HY-100535
-
|
Cyclopamine-KAAD
|
Smo
|
Cancer
|
|
KAAD-Cyclopamine, a hedgehog signaling inhibitor, is a smoothened antagonist .
|
-
- HY-100292
-
-
- HY-15539
-
-
- HY-101745
-
-
- HY-101743
-
-
- HY-19652A
-
|
Esoxybutynin hydrochloride
|
mAChR
|
Neurological Disease
|
|
(S)-Oxybutynin (Esoxybutynin) hydrochloride is a potent muscarinic receptor antagonist .
|
-
- HY-100191
-
-
- HY-124157
-
-
- HY-402545
-
-
- HY-121186
-
-
- HY-101207
-
|
|
GABA Receptor
|
Neurological Disease
|
|
NCS-382 is a potent GABA receptor antagonist and also a GHBR receptor antagonist. NCS-382 has anticonvulsant and antisedative activity. NCS-382 is used in the related research of hereditary nervous system diseases .
|
-
- HY-A0019S
-
|
|
Dopamine Receptor
5-HT Receptor
Adrenergic Receptor
|
Neurological Disease
|
|
Paliperidone-d4 is the deuterium labeled Paliperidone. Paliperidone (9-Hydroxyrisperidone), the major active metabolite of Risperidone, is a dopamine D2 antagonist and 5-HT2A antagonist. Paliperidone is also active as an antagonist at α1 and α2 adrenergic receptors and H1-histaminergic receptors. Paliperidone, a antipsychotic agent, shows efficacy against schizophrenia .
|
-
- HY-108555
-
|
|
Protease Activated Receptor (PAR)
|
Cardiovascular Disease
|
|
FR171113 is a specific and non-peptide thrombin receptor antagonist. FR171113 exhibits the antithrombotic effects of a PAR1 antagonist. FR171113 inhibits thrombin-induced platelet aggregation with an IC50 of 0.29 μM. .
|
-
- 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-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-120182
-
-
- HY-19973
-
-
- HY-117500
-
-
- HY-121692A
-
-
- HY-110097
-
|
CNS 1102
|
iGluR
|
Neurological Disease
|
|
Aptiganel hydrochloride (Cerestat) is a non-competitive NMDA receptor antagonist with neuroprotective effect.
|
-
- HY-121019
-
-
- HY-P4785
-
-
- HY-115874
-
|
|
CCR
|
Others
|
|
BMS-753426 is a potent and orally bioavailable antagonist of CCR2.
|
-
- HY-118844
-
-
- HY-15085
-
-
- HY-114674A
-
-
- HY-100122
-
-
- HY-121906
-
-
- HY-19732
-
-
- HY-16763
-
-
- HY-119950
-
-
- HY-B0009
-
-
- HY-19818
-
-
- HY-110240
-
|
|
Smo
|
Others
|
|
IHR-1 is a cell membrane impermeable Smo antagonist .
|
-
- HY-167668
-
-
- HY-101944
-
-
- HY-10164
-
-
- HY-101632
-
-
- HY-U00019
-
-
- HY-101600
-
-
- HY-101602
-
-
- HY-101618
-
-
- HY-15073
-
-
- HY-117981
-
-
- HY-165622
-
-
- HY-18101A
-
-
- HY-U00040
-
-
- HY-14277AR
-
|
|
Histamine Receptor
Neurotensin Receptor
Integrin
|
Inflammation/Immunology
|
|
Levocabastine (hydrochloride) (Standard) is the analytical standard of Levocabastine (hydrochloride). This product is intended for research and analytical applications. Levocabastine (R 50547) hydrochloride is a potent and selective histamine H1-receptor antagonist. Levocabastine hydrochloride is also a selective, high affinity neurotensin receptor subtype 2 (NTR2) antagonist, with a Ki of 17 nM for mNTR2. Levocabastine hydrochloride can act as a VLA-4 antagonist, interferes with conjunctival eosinophil infiltration in allergic conjunctivitis (AC) .
|
-
- HY-115827
-
|
|
Prostaglandin Receptor
|
Others
|
|
AH22921 is an EP4 prostaglandin receptor antagonist with the activity of antagonizing the activation of adenylate cyclase by prostaglandins in CHO cells. AH22921 can shift the PGE2 concentration-response curve to the right in CHO cells. It is a non-competitive antagonist that is selective for EP4 receptors and has an antagonistic effect on EP4 receptors in CHO cells, but does not affect the PGE2 concentration-response curve in NPE cells containing EP2 receptors.
|
-
- HY-A0019R
-
|
9-Hydroxyrisperidone (Standard)
|
Drug Metabolite
Reference Standards
Dopamine Receptor
5-HT Receptor
Adrenergic Receptor
|
Neurological Disease
|
|
Paliperidone (Standard) is the analytical standard of Paliperidone. This product is intended for research and analytical applications. Paliperidone (9-Hydroxyrisperidone), the major active metabolite of Risperidone, is a dopamine D2 antagonist and 5-HT2A antagonist. Paliperidone is also active as an antagonist at α1 and α2 adrenergic receptors and H1-histaminergic receptors. Paliperidone, a antipsychotic agent, shows efficacy against schizophrenia .
|
-
- HY-N0096
-
|
(-)-Tetrahydropalmatine; L-Tetrahydropalmatine
|
5-HT Receptor
Dopamine Receptor
|
Neurological Disease
|
|
Rotundine is an antagonist of dopamine D1, D2 and D3 receptors with IC50s of 166 nM, 1.4 μM and 3.3 μM, respectively. Rotundine is also an antagonist of 5-HT1A with an IC50 of 370 nM.
|
-
- HY-126068
-
|
Esamisulpride; SEP-4199
|
Dopamine Receptor
5-HT Receptor
|
Neurological Disease
|
|
(S)-Amisulpride (Esamisulpride) is a potent dopamine D2/D3 receptor antagonist. (S)-Amisulpride is an antagonist at the 5-HT7 receptor with a KI of 900 nM. (S)-Amisulpride has antipsychotic and antidepressant effects .
|
-
- HY-13706A
-
|
TM30089
|
Prostaglandin Receptor
|
Inflammation/Immunology
|
|
CAY10471 (TM30089) is a potent, selective, and orally active prostaglandin D2 receptor CRTH2 antagonist. CAY10471 attenuates the progression of tubulointerstitial fibrosis and chronic contact hypersensitivity (CHS) in animal model .
|
-
- HY-107607
-
|
|
Leukotriene Receptor
|
Inflammation/Immunology
|
|
FPL-55712 free base is a leukotriene receptor antagonist. FPL-55712 free base is also an antagonist of slow reacting substance of anaphylaxis (SRS-A). FPL-55712 free base inhibits leukotriene-induced bronchoconstriction .
|
-
- HY-100405
-
|
|
mGluR
|
Neurological Disease
|
|
FTIDC is an orally active, noncompetitive, selective allosteric metabotropic glutamate receptor (mGluR) 1 antagonist with an IC50 of 5.8 nM for human mGluR1a. FTIDC has no species differences in its antagonistic activity on recombinant human, mouse, and rat mGluR1 .
|
-
- HY-123490
-
|
INS50589
|
P2Y Receptor
|
Inflammation/Immunology
|
|
Regrelor disodium (INS 50589) is a platelet P2Y12 receptor antagonist. Regrelor disodium is a well-tolerated, reversible ADP competitive antagonist. Regrelor disodium inhibits cell proliferation. Regrelor disodium can be used in inflammation-related research .
|
-
- HY-105201A
-
|
FK1052
|
5-HT Receptor
|
Neurological Disease
Cancer
|
|
Fabesetron (FK1052) hydrochloride is an orally active 5-HT3 receptor antagonist with 5-HT4 receptor antagonistic activity. Fabesetron hydrochloride can be used in the study for both acute and delayed emesis induced by cancer chemotherapy .
|
-
- HY-B1416A
-
-
- HY-P3854
-
|
|
Neurokinin Receptor
|
Neurological Disease
|
|
GR 83074 is a potent and selective NK-2 (Neurokinin Receptor) antagonist with a pKB of 8.23. GR 83074 is inactive as an NK-3 antagonist and exhibits a 340-fold NK-2/NK-1 selectivity .
|
-
- HY-12881
-
|
SL-820715
|
iGluR
|
Neurological Disease
|
|
Eliprodil(SL-820715) is a non-competitive NR2B-NMDA receptor antagonist(IC50=1 uM), less potent for NR2A- and NR2C-containing receptors(IC50> 100 uM).
|
-
- HY-B0561S1
-
-
- HY-B0561S
-
-
- HY-B0549A
-
|
Rec-7-0040; DW61
|
Phosphodiesterase (PDE)
Calcium Channel
mAChR
|
Neurological Disease
|
|
Flavoxate hydrochloride is a potent and competitive phosphodiesterase (PDE) inhibitor. Flavoxate hydrochloride is an antispasmodic agent and muscarinic mAChR antagonist. Flavoxate hydrochloride shows moderate calcium antagonistic activity and local anesthetic effect. Flavoxate hydrochloride can be used for the research of overactive bladder (OAB) and lower urinary tract infections .
|
-
- HY-111616
-
|
|
PPAR
Angiotensin Receptor
|
Cardiovascular Disease
Others
|
|
GSK1820795A, as a telmisartan analog, is a selective hGPR132a antagonist. GSK1820795A blocks activation of yeast cells expressing hGPR132a by N-acylamides . GSK1820795A is also a angiotensin II antagonists and partial PPARγ agonists (compound 38) .
|
-
- HY-N0607
-
|
Polysciasaponin P3; Chikusetsusaponin 5; Chikusetsusaponin V
|
Calcium Channel
Prostaglandin Receptor
|
Cardiovascular Disease
Endocrinology
|
|
Ginsenoside Ro (Polysciasaponin P3; Chikusetsusaponin 5; Chikusetsusaponin V) exhibits a Ca 2+-antagonistic antiplatelet effect with an IC50 of 155 μM. Ginsenoside Ro reduces the production of TXA2 more than it reduces the activities of COX-1 and TXAS.
|
-
- HY-B1439B
-
-
- HY-P0061B
-
|
RC160 diacetate; BMY 41606 diacetate
|
Neurokinin Receptor
|
Cancer
|
|
Vapreotide diacetate is a neurokinin-1 (NK1) receptor antagonist, with an IC50 of 330 nM.
|
-
- HY-42849
-
-
- HY-22437
-
|
(±)-UK-88525
|
mAChR
|
Neurological Disease
Cancer
|
|
(±)-Darifenacin is the racemate of Darifenacin. Darifenacin is a selective M3 muscarinic receptor antagonist .
|
-
- HY-17382C
-
-
- HY-15487
-
-
- HY-13021
-
-
- HY-118780
-
-
- HY-17582
-
-
- HY-B1506
-
-
- HY-P2075
-
|
|
Renin
|
Endocrinology
|
|
EMD 55068 is a renin antagonist. EMD 55068 inhibits the uptake of taurocholate .
|
-
- HY-15001
-
-
- HY-100925
-
-
- HY-109147
-
-
- HY-169820
-
-
- HY-B1506A
-
|
Acetopromazine maleate; Acetylpromazine maleate
|
Adrenergic Receptor
|
Neurological Disease
|
|
Acepromazine (Acetopromazine) maleate is a phenothiazine tranquilizer and is alpha-adrenoceptor antagonist [2.
|
-
- HY-10304
-
-
- HY-110110A
-
-
- HY-122126
-
-
- HY-125145
-
-
- HY-19737A
-
|
|
PPAR
|
Cancer
|
|
DG172 dihydrochloride is a selective PPARβ/δ antagonist, with an IC50 of 27 nM.
|
-
- HY-101502A
-
-
- HY-110170
-
-
- HY-12710A
-
-
- HY-16509
-
-
- HY-10304A
-
-
- HY-118455
-
-
- HY-14538A
-
-
- HY-P0061
-
-
- HY-13439
-
-
- HY-P1994
-
-
- HY-12114
-
-
- HY-50663
-
MK 0893
5 Publications Verification
|
GCGR
|
Metabolic Disease
|
|
MK 0893 is a potent and selective glucagon receptor antagonist with an IC50 of 6.6 nM.
|
-
- HY-42849A
-
-
- HY-172427
-
-
- HY-120585
-
-
- HY-P1018
-
-
- HY-101797
-
-
- HY-15758
-
-
- HY-P1782
-
-
- HY-U00018
-
-
- HY-19243
-
-
- HY-101668
-
-
- HY-19163
-
-
- HY-103099
-
-
- HY-136969
-
-
- HY-14284
-
-
- HY-14656
-
-
- HY-14538
-
-
- HY-15066
-
|
FG9065
|
iGluR
|
Neurological Disease
|
|
CNQX (FG9065) is a potent and competitive AMPA/kainate receptor antagonist with IC50s of 0.3 μM and 1.5 μM, respectively. CNQX is a competitive non-NMDA receptor antagonist . CNQX blocks the expression of fear-potentiated startle in rats .
|
-
- HY-B0561S2
-
-
- HY-101229
-
|
|
iGluR
|
Neurological Disease
|
|
(2R,3R)-Chlorpheg is a week antagonist of L-homocysteic acid (L-HCA) induced depolarization.(2R,3R)-Chlorpheg also is a weak N-methyl-D-aspartate (NMDA) antagonist .
|
-
- HY-B0549
-
|
Rec-7-0040 free base; DW61 free base
|
Phosphodiesterase (PDE)
Calcium Channel
mAChR
|
Neurological Disease
|
|
Flavoxate is a potent and competitive phosphodiesterase (PDE) inhibitor. Flavoxate is an antispasmodic agent and muscarinic mAChR antagonist. Flavoxate shows moderate calcium antagonistic activity and local anesthetic effect. Flavoxate can be used for the research of overactive bladder (OAB) and lower urinary tract infections .
|
-
- HY-14757
-
|
SL-650472
|
5-HT Receptor
|
Neurological Disease
|
|
Trelanserin (SL-650472) is a 5-HT receptor antagonist and also an effective in vitro smooth muscle contraction antagonist, competing against the contractions induced by sumatriptan (HY-B0121B) with a pA2 of 8.17±0.36 .
|
-
- HY-13222
-
|
|
Opioid Receptor
|
Neurological Disease
Cancer
|
|
BAN ORL 24 is a nociceptin/orphanin FQ (N/OFQ) peptide receptor (NOP) antagonist. BAN ORL 24 has antagonistic effect for nociceptin (NOP) receptor with KI value of 0.24 nM in CHO cell. BAN ORL 24 can be used for the research of cancer and analgesic .
|
-
- HY-105201
-
|
FK1052 free base
|
5-HT Receptor
|
Neurological Disease
Cancer
|
|
Fabesetron (FK1052) is an orally active 5-HT3 receptor antagonist with 5-HT4 receptor antagonistic activity. Fabesetron (FK1052) can be used in the study for both acute and delayed emesis induced by cancer chemotherapy .
|
-
- HY-148350
-
|
|
PTHR
|
Cancer
|
|
DS69910557 is a potent, selective and orally activehuman parathyroid hormone receptor 1 (hPTHR1) antagonist. DS69910557 has antagonistic activity for PTHR1 with an IC50 value of 0.08 μM. DS69910557 can be used for the research of hyperparathyroidism, hypercalcemia of malignancy and osteoporosis .
|
-
- HY-B0569
-
|
|
nAChR
Apoptosis
|
Cardiovascular Disease
Neurological Disease
|
|
Hexamethonium Bromide is a non-selective ganglionic nicotinic-receptor antagonist (nAChR) antagonist, with mixed competitive and noncompetitive activity. Hexamethonium Bromide has anti-hypertensive activity. Hexamethonium Bromide attenuates sympathetic activity and blood pressure in spontaneously hypertensive animal models .
|
-
- HY-18697
-
-
- HY-114928
-
|
L 3937; Dideiodo Amiodarone
|
Drug Intermediate
|
Others
|
|
Deiodoamiodarone (L 3937; Dideiodo Amiodarone) is an intermediate of amiodarone. Amiodarone is a potent calmodulin antagonist .
|
-
- HY-143518
-
-
- HY-123557
-
|
|
iGluR
|
Others
|
Dasolampanel etibutil is an ion-type glutamate receptor 5 (iGluR5) antagonist .
|
-
- HY-15702
-
HJC0350
2 Publications Verification
|
Ras
|
Cancer
|
|
HJC0350 is a potent and specific EPAC2 antagonist with an IC50 of 0.3 μM.
|
-
- HY-100914
-
|
Ophobolin A
|
Calmodulin
|
Cancer
|
|
A-7 hydrochloride (Ophobolin A) is a calmodulin antagonist and can be used for the research of cancer .
|
-
- HY-121545
-
-
- HY-108458
-
-
- HY-145716
-
|
Nafoxidene
|
Estrogen Receptor/ERR
|
Cancer
|
|
Nafoxidine, a nonsteroidal estrogen antagonist, is shown to possess antitumor activity against breast cancer.
|
-
- HY-B0918
-
|
Chlophenadione; Indaliton; G-25766
|
VD/VDR
|
Cardiovascular Disease
|
|
Chlorindione (Chlophenadione) is a potent anticoagulant. Chlorindione also is a vitamin K1 antagonist .
|
-
- HY-109543A
-
-
- HY-76520
-
-
- HY-15709
-
-
- HY-100850
-
-
- HY-14901
-
|
|
Progesterone Receptor
|
Cancer
|
|
Telapristone is a Progesterone antagonist. Telapristone can be used in the study of uterine fibroids and endometriosis .
|
-
- HY-110095
-
-
- HY-106231
-
|
JB95008 free acid
|
Cholecystokinin Receptor
|
Others
|
|
Gastrazole (JB95008) free acid is a gastrin receptor antagonist with activity against pancreatic cancer.
|
-
- HY-112604
-
-
- HY-101713
-
-
- HY-N7574
-
-
- HY-110037
-
-
- HY-A0229A
-
-
- HY-102093
-
-
- HY-109074
-
-
- HY-123744
-
-
- HY-P5359
-
-
- HY-W700638A
-
-
- HY-142868
-
-
- HY-B0953A
-
-
- HY-137148
-
|
|
Chloride Channel
|
Cancer
|
|
DIOA is a potent acid-sensitive outwardly rectifying (ASOR) anion channel antagonist .
|
-
- HY-125449
-
|
|
Calmodulin
|
Others
|
|
Fasciculic acid C is a calmodulin antagonist that can be isolated from mushroom Naematoloma fasciculare .
|
-
- HY-16732
-
-
- HY-112703
-
-
- HY-U00363
-
-
- HY-A0075
-
-
- HY-106499
-
-
- HY-A0145
-
|
|
VD/VDR
|
Others
Cancer
|
|
Phenprocoumon is a coumarin derivative that acts as a long acting oral anticoagulant and an antagonist of vitamin K.
|
-
- HY-B2073A
-
-
- HY-16701
-
|
|
IAP
|
Cancer
|
|
BV6 is an antagonist of cIAP1 and XIAP, members of the inhibitors of apoptosis (IAP) family.
|
-
- HY-136842
-
-
- HY-109543
-
|
|
5-HT Receptor
|
|
|
Indisetron is a 5-HT3 receptor antagonist with anti-emetic activity.
|
-
- HY-12510
-
-
- HY-101164
-
-
- HY-15574A
-
-
- HY-106416
-
-
- HY-W013200
-
|
|
VD/VDR
|
Metabolic Disease
|
|
Coumachlor is an orally active antieoagulant agent. Coumachlor is a vitamin K antagonist .
|
-
- HY-U00086
-
-
- HY-U00026
-
-
- HY-B2073
-
-
- HY-19684
-
-
- HY-14390
-
-
- HY-101706
-
-
- HY-101830
-
-
- HY-50912
-
-
- HY-P0209
-
-
- HY-B0286A
-
-
- HY-134125
-
-
- HY-U00283
-
-
- HY-G0012
-
-
- HY-17417AS
-
|
|
Opioid Receptor
|
Others
|
|
Naloxone D5 is deuterium labeled Naloxone. Naloxone is a a potent opioid receptor antagonist.
|
-
- HY-172413
-
|
|
PPAR
|
Cancer
|
|
Amezalpat is the antagonist for PPARα with IC50 of 58 nM. Amezalpat exhibits antineoplastic activity .
|
-
- HY-U00404
-
-
- HY-159507
-
-
- HY-100153
-
-
- HY-U00188
-
-
- HY-U00207
-
-
- HY-50691
-
-
- HY-103335
-
-
- HY-103360
-
|
|
CCR
|
Inflammation/Immunology
|
|
J-113863 is a potent and selective CCR1 antagonist with IC50 values of 0.9 nM and 5.8 nM for human and mouse CCR1 receptors, respectively. J-113863 is also a potent antagonist of the human CCR3 (IC50 of 0.58 nM) , but a weak antagonist of the mouse CCR3 (IC50 of 460 nM). J-113863 is inactive against CCR2, CCR4 and CCR5, as well as the LTB4 or TNF-α receptors. Anti-inflammatory effect .
|
-
- HY-32329
-
|
Org-8282
|
5-HT Receptor
Adrenergic Receptor
|
Neurological Disease
|
|
Setiptiline (Org-8282) is a serotonin receptor antagonist. Setiptiline is a tetracyclic antidepressant (TeCA) which acts as a noradrenergic and specific serotonergic antidepressant (NaSSA). Setiptiline acts as a norepinephrine reuptake inhibitor, α2-adrenergic receptor antagonist, and serotonin receptor antagonist, likely at the 5-HT2A, 5-HT2C, and/or 5-HT3 subtypes, as well as an H1 receptor inverse agonist/antihistamine.
|
-
- HY-159923
-
|
|
Opioid Receptor
|
Neurological Disease
|
|
BPRMU191 is a μ-opioid receptor (MOR) modulator that converts small-molecule morphinan antagonists into G protein-biased MOR agonists, thereby inducing MOR-dependent activation and analgesic effects. Co-administration of BPRMU191 with morphinan antagonists provides analgesia while reducing side effects such as gastrointestinal dysfunction, antinociceptive tolerance, and dependency-related adverse effects. BPRMU191, in combination with morphinan antagonists, offers a potential strategy for studying severe pain management and G protein-coupled receptor modulation .
|
-
- HY-P3397A
-
|
|
GHSR
|
Cancer
|
|
JV-1-36 acetate is a growth hormone-releasing hormone (GHRH) antagonist. JV-1-36 acetate inhibits the production of reactive oxygen species in A549 lung cancer cells. JV-1-36 can be used to study the effect of GHRH antagonists in vitro .
|
-
- HY-116066
-
|
|
Endogenous Metabolite
|
Endocrinology
|
|
YM471 free base is a non-peptide antagonist of vasopressin V1A and V2 receptors with potent and persistent antagonistic activity. YM471 exhibits high affinity for rat V1A and V2 receptors with K values of 0.16 and 0.77 nM, respectively .
|
-
- HY-B0561R
-
|
SC9420 (Standard)
|
Reference Standards
Mineralocorticoid Receptor
Androgen Receptor
Autophagy
|
Metabolic Disease
Cancer
|
|
Spironolactone (Standard) is the analytical standard of Spironolactone. This product is intended for research and analytical applications. Spironolactone (SC9420) is an orally active aldosterone mineralocorticoid receptor antagonist with an IC50 of 24 nM. Spironolactone is also a potent antagonist of androgen receptor with an IC50 of 77 nM. Spironolactone promotes autophagy in podocytes .
|
-
- HY-P3397
-
|
|
GHSR
|
Cancer
|
|
JV-1-36 is a growth hormone-releasing hormone (GHRH) antagonist. JV-1-36 inhibits the production of reactive oxygen species in A549 lung cancer cells. JV-1-36 can be used to study the effect of GHRH antagonists in vitro .
|
-
- HY-G0014AR
-
|
Quetiapine S-oxide dihydrochloride (Standard)
|
Drug Metabolite
|
Neurological Disease
|
|
Quetiapine sulfoxide (dihydrochloride) (Standard) is the analytical standard of Quetiapine sulfoxide (dihydrochloride). This product is intended for research and analytical applications. Quetiapine sulfoxide dihydrochloride (Quetiapine S-oxide dihydrochloride) is a main metabolite of Quetiapinem. Quetiapine is a second-generation antipsychotic[1]. Quetiapine is a 5-HT receptors agonist and a dopamine receptor antagonist[2].
|
-
- HY-P10473
-
|
|
Neuromedin U Receptor (NMUR)
|
Inflammation/Immunology
|
|
CPN-351 (compound 9a), a pentapeptide, is a selective antagonist of human NMUR1 with a pA2 of 7.35. The antagonistic effect of CPN-351 on human NMUR1 is 10 times higher than that on NMUR2. CPN-351 can be used in the study of inflammation .
|
-
- HY-114452
-
|
BTRX-246040
|
Opioid Receptor
|
Neurological Disease
|
|
LY2940094 (BTRX-246040) is a potent, selective and orally available nociceptin receptor (NOP receptor) antagonist with high affinity (Ki=0.105 nM) and antagonist potency (Kb=0.166 nM). LY2940094 reduces ethanol self-administration in animal models .
|
-
- HY-15129
-
|
L-Serine O-phosphate; L-SOP
|
mGluR
Endogenous Metabolite
|
Neurological Disease
|
|
O-Phospho-L-serine is the immediate precursor to L-cystein in the serine synthesis pathway, and an agonist at the group III mGluR receptors (mGluR4, mGluR6, mGluR7, and mGluR8); O-Phospho-L-serine also acts as a weak antagonist for mGluR1 and a potent antagonist for mGluR2 .
|
-
- HY-19638A
-
|
AR-C69931MX tetrasodium
|
P2Y Receptor
|
Cardiovascular Disease
Inflammation/Immunology
|
|
Cangrelor tetrasodium, an adenosine triphosphate analogue, is a reversible and selective platelet P2Y12 antagonist, with prompt and potent antiplatelet effects. Cangrelor tetrasodium directly blocks adenosine diphosphate (ADP)-induced activation and aggregation of platelets. Cangrelor tetrasodium is also a nonspecific GPR17 antagonist .
|
-
- HY-120927
-
|
|
Opioid Receptor
|
Neurological Disease
|
|
Alvimopan metabolite is a μ opioid receptor antagonist with activity that selectively interacts with μ peripheral receptors. Alvimopan metabolite can be used as a potential inhibitory drug to alleviate the side effects caused by opioids. Alvimopan metabolite was identified as a highly selective μ opioid receptor antagonist during research and development .
|
-
- HY-101527
-
20-HEDE
2 Publications Verification
WIT 002
|
Cytochrome P450
|
Cancer
|
|
20-HEDE (WIT 002) is an antagonist of 20-hydroxyeicosatetraenoic acid (20-HETE).
|
-
- HY-U00212
-
-
- HY-107631
-
-
- HY-145353
-
-
- HY-15640
-
|
|
TRP Channel
Apoptosis
|
Cancer
|
|
Capsazepine is a synthetic analogue of the sensory neurone excitotoxin, and an antagonist of TRPV1 receptor with an IC50 of 562 nM.
|
-
- HY-103495
-
-
- HY-103408
-
-
- HY-15403
-
-
- HY-106766
-
-
- HY-P3450
-
-
- HY-155879
-
-
- HY-15412
-
|
|
Smo
|
Cancer
|
|
HhAntag is a specific, potent and orally active small molecule SMO antagonist of the Hh pathway .
|
-
- HY-112667
-
-
- HY-U00263
-
-
- HY-135552
-
-
- HY-B0355
-
-
- HY-10259
-
-
- HY-120564
-
|
|
CRFR
|
Neurological Disease
|
|
BMS-763534 is a CRF1 antagonist that inhibits neurological disorders such as depression and anxiety. .
|
-
- HY-12426A
-
|
|
mAChR
|
Neurological Disease
|
|
mAChR-IN-1 hydrochloride is a potent muscarinic cholinergic receptor (mAChR) antagonist, with an IC50 of 17 nM .
|
-
- HY-107186
-
-
- HY-13541
-
|
|
Cadherin
|
Cancer
|
|
ADH-1, an N-cadherin antagonist, inhibits N-cadherin mediated cell adhesion.
|
-
- HY-14423
-
-
- HY-P2669
-
-
- HY-12426
-
|
|
mAChR
|
Neurological Disease
|
|
mAChR-IN-1 is a potent muscarinic cholinergic receptor (mAChR) antagonist, with an IC50 of 17 nM .
|
-
- HY-B0500
-
-
- HY-108997A
-
-
- HY-101233
-
-
- HY-11103
-
-
- HY-169137
-
-
- HY-18611A
-
-
- HY-W013113
-
|
|
nAChR
|
Neurological Disease
|
|
BTMPS is a nicotine receptor (nAChR) antagonist that can lessen the negative effects of morphine on rats .
|
-
- HY-14770
-
-
- HY-107765
-
-
- HY-108324
-
-
- HY-50669
-
-
- HY-10259A
-
-
- HY-G0011
-
-
- HY-167699
-
|
|
mAChR
|
Others
|
|
Cyclodrine is a cholinergic receptor antagonist that exhibits biological activity by influencing both muscarinic and nicotinic receptors.
|
-
- HY-16027
-
|
|
GnRH Receptor
|
Endocrinology
|
|
Acyline, a GnRH peptide analogue, is a GnRH antagonist that inhibits gonadotropin and testosterone (T) levels .
|
-
- HY-103499
-
|
|
GABA Receptor
|
Neurological Disease
|
ZK 93426 (hydrochloride) is a benzodiazepine antagonist. ZK 93426 (hydrochloride) can be used for the research of neurological disease .
|
-
- HY-P2028
-
|
|
GnRH Receptor
|
Cancer
|
|
BIM 21009 is a LHRH and GnRH receptor antagonist. BIM 21009 inhibits tumor growth .
|
-
- HY-107672
-
|
Stilonium iodide
|
nAChR
|
Neurological Disease
|
|
MG624 is a potent and selective neuronal α7 nAChR antagonist with a Ki of 106 nM .
|
-
- HY-152850
-
|
|
Androgen Receptor
|
Endocrinology
Cancer
|
|
Gumelutamide is a tetrahydropyridopyrimidine compound, acting as an antiandrogen, antineoplastic agent. Gumelutamide is an androgen antagonist .
|
-
- HY-B0205S
-
|
CV-11974-d4
|
Angiotensin Receptor
|
Others
|
|
Candesartan-d4 is the deuterium labeled Candesartan, which is an angiotensin II receptor antagonist.
|
-
- HY-N1378
-
-
- HY-B0500B
-
-
- HY-U00335
-
-
- HY-43711
-
|
|
mAChR
|
Neurological Disease
|
|
Nor-benzetimide is a major metabolite of Benzetimide. Benzetimide is a mAChR antagonist with anticholinergic activity .
|
-
- HY-19924
-
-
- HY-18611
-
-
- HY-B0500A
-
-
- HY-19670
-
-
- HY-14129
-
-
- HY-19855
-
-
- HY-15853
-
-
- HY-14367
-
-
- HY-107710
-
-
- HY-13004
-
-
- HY-B0547
-
|
|
mAChR
|
Neurological Disease
|
|
Homatropine is an orally active muscarinic acetylcholine receptor antagonist and can be used as an anticholinergic agent .
|
-
- HY-U00257
-
-
- HY-13796
-
-
- HY-108997
-
-
- HY-106785
-
-
- HY-125879
-
-
- HY-103533
-
-
- HY-14432
-
-
- HY-101407
-
-
- HY-111186
-
|
WL 108366
|
Glucocorticoid Receptor
MMP
VKOR
|
Others
|
|
Flocoumafen (WL 108366) is an orally active vitamin K epoxide reductase inhibitor and a multi-target ligand, which includes prostaglandin F synthase, serum albumin, glucocorticoid receptor 2, and MMP-9. Flocoumafen is a second-generation anticoagulant rodenticide (ARs) with a half-life of 177.4 hours and has deadly anticoagulant effects .
|
-
- HY-111186R
-
|
|
VKOR
Glucocorticoid Receptor
MMP
|
Others
|
|
Flocoumafen (Standard) is the analytical standard of Flocoumafen. This product is intended for research and analytical applications. Flocoumafen (WL 108366) is an orally active vitamin K epoxide reductase inhibitor and a multi-target ligand, which includes prostaglandin F synthase, serum albumin, glucocorticoid receptor 2, and MMP-9. Flocoumafen is a second-generation anticoagulant rodenticide (ARs) with a half-life of 177.4 hours and has deadly anticoagulant effects .
|
-
- HY-B1517B
-
|
|
5-HT Receptor
|
Cardiovascular Disease
Cancer
|
|
Alprenolol benzoate is an orally active non-selective β-adrenoceptor antagonist and an antagonist of 5-HT1A and 5-HT1B receptors. Alprenolol benzoate is used as an anti-hypertensive, anti-anginal and anti-arrhythmic agent .
|
-
- HY-15066A
-
|
FG9065 disodium
|
iGluR
|
Neurological Disease
|
|
CNQX disodium (FG9065 disodium) is a potent and competitive AMPA/kainate receptor antagonist with IC50s of 0.3 μM and 1.5 μM, respectively. CNQX disodium is a competitive non-NMDA receptor antagonist . CNQX disodium blocks the expression of fear-potentiated startle in rats .
|
-
- HY-16978
-
-
- HY-32329A
-
|
MO-8282
|
5-HT Receptor
|
Neurological Disease
|
|
Setiptiline maleate (MO-8282 maleate) is a serotonin receptor antagonist. Setiptiline maleate is a tetracyclic antidepressant (TeCA) which acts as a noradrenergic and specific serotonergic antidepressant (NaSSA). Setiptiline maleate acts as a norepinephrine reuptake inhibitor, α2-adrenergic receptor antagonist, and serotonin receptor antagonist, likely at the 5-HT2A, 5-HT2C, and/or 5-HT3 subtypes, as well as an H1 receptor inverse agonist/antihistamine .
|
-
- HY-A0295
-
-
- HY-107743
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NalBzoH
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Opioid Receptor
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Neurological Disease
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Naloxone benzoylhydrazone (NalBzoH) is a mixed agonist/antagonist. Naloxone benzoylhydrazone is a prototypic κ3-opioid receptor agonist, and a partial agonist at the cloned μ and δ opioid receptors, and an antagonist at opioid-like NOP receptors. Naloxone benzoylhydrazone has potently analgesia effect .
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- HY-U00121A
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5-HT Receptor
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Metabolic Disease
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Lintopride hydrochloride, a benzamide, is a potent 5HT-4 antagonist with moderate 5HT-3 antagonist properties. Lintopride hydrochloride increases gastric emptying, stimulates antral and duodenal motility and accelerates intestinal transit in animal. Lintopride hydrochloride significantly increases the lower oesophageal sphincter (LOS) basal tone .
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- HY-W424730
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iGluR
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Others
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HA-966 hydrochloride is a glycine site antagonist of the NMDA receptor, exhibiting non-competitive antagonism on NMDA responses. HA-966 hydrochloride effectively blocks the enhancement of NMDA responses by glycine in a competitive manner. HA-966 hydrochloride plays a significant role in mediating the antagonist action at the glycine modulatory site of the NMDA receptor.
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- HY-U00121
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5-HT Receptor
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Metabolic Disease
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Lintopride, a benzamide, is a potent 5HT-4 antagonist with moderate 5HT-3 antagonist properties. Lintopride increases gastric emptying, stimulates antral and duodenal motility and accelerates intestinal transit in animal. Lintopride significantly increases the lower oesophageal sphincter (LOS) basal tone .
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- HY-P2285
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- HY-10560
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-
- HY-123788
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-
- HY-109718
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- HY-10052
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- HY-173072
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Orphan Receptor
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Others
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SJPYT-310 is a selective PXR antagonist. SJPYT-310 shows no significant cytotoxicity .
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- HY-P4452
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- HY-103113
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- HY-112558
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- HY-106397
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- HY-13541A
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Cadherin
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Cancer
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ADH-1 trifluoroacetate is an N-cadherin antagonist, which inhibits N-cadherin mediated cell adhesion.
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- HY-N0184
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- HY-P0171
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BKT140 (4-fluorobenzoyl); BL-8040; TF14016
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CXCR
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Endocrinology
Cancer
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Motixafortide (BKT140 4-fluorobenzoyl) is a novel CXCR4 antagonist with an IC50 vakue of ～1 nM.
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- HY-50669A
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- HY-136791
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- HY-123287
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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-W708197
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mAChR
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Neurological Disease
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Tolterodine dimer is the impurity of Tolterodine (HY-A0024). Tolterodine is a potent muscarinic receptor antagonist.
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- HY-106397A
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- HY-119010
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- HY-111295
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Adenosine Receptor
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Others
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LAS38096 is a potent, selective, and efficacious A2B Adenosine Receptor antagonist, with a Ki of 17 nM .
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- HY-111155
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- HY-118535
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- HY-105771
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mAChR
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Neurological Disease
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Parapenzolate bromide, an antispasmodic, is an orally active mAChR antagonist. Parapenzolate bromide is an anticholinergic agent .
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- HY-106239
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- HY-U00253
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- HY-B1589AS
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- HY-U00106
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- HY-B0460
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BA-679 BR monohydrate
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mAChR
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Neurological Disease
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Tiotropium bromide (BA-679 BR) monohydrate is a long-acting muscarinic receptor antagonist .
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- HY-100471
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- HY-109167
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- HY-146404
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- HY-108972
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- HY-16027A
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GnRH Receptor
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Endocrinology
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Acyline TFA, a GnRH peptide analogue, is a GnRH antagonist that inhibits gonadotropin and testosterone (T) levels .
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- HY-19632
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- HY-15403A
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- HY-19193
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- HY-100152
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SX 810
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mAChR
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Inflammation/Immunology
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Beperidium iodide shows a competitive antagonistic effect against acetylcholine receptor with a pA2 of 7.93.
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- HY-107749
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- HY-19391
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- HY-104061
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TRP Channel
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Others
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AMG8788 is a potent, selective, orally active antagonist of TRPM8 with an IC50 of 63.2 nM .
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- HY-117256
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- HY-104062
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TRP Channel
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Others
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AMG9678 is a potent, selective, orally active antagonist of TRPM8 with an IC50 of 31.2 nM .
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- HY-167850
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-
- HY-U00252
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-
- HY-105198
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- HY-119219
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Bacterial
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Infection
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Detoxin C1 is an active principle of detoxin complex. Detoxin complex is an antagonist of Blasticidin S .
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- HY-110132
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- HY-B1510
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- HY-15488A
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- HY-17001A
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- HY-10560A
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- HY-19654
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- HY-105436
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- HY-109511
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CCR
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Others
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AZD-1678 is a potent CCR4 receptor antagonist, with a pIC50 of 8.6 .
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- HY-119076
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- HY-101683
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- HY-101620
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iGluR
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Neurological Disease
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MRZ 2-514 is an antagonist of the strychnine-insensitive modulatory site of the NMDA receptor (glycineB), with Ki of 33 μM.
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- HY-101700
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- HY-101669
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- HY-B0547A
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mAChR
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Neurological Disease
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Homatropine Bromide is an orally active muscarinic acetylcholine receptor antagonist and can be used as an anticholinergic agent .
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- HY-19580
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CM 57755A
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Histamine Receptor
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Endocrinology
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Ramisotidine is a histamine H2 receptor antagonist that can inhibit gastric acid secretion stimulated by pentagastrin .
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- HY-101718
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- HY-13209C
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- HY-117793
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- HY-112736
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- HY-110136
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- HY-12371
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mGluR
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Neurological Disease
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VU0431316 is a potent and selective non-competitive antagonist of mGlu5 with an IC50 value of 24 nM .
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- HY-106334
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- HY-U00360
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(Rac)-Netazepide; (Rac)-YF 476; (Rac)-YM-220
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Cholecystokinin Receptor
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Metabolic Disease
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(Rac)-Sograzepide is an antagonist of cholecystokinin B (CCK-B) receptor, and has the potential of reducing the secretion of gastric acid.
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- HY-N0340
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Hyoscine butylbromide; (-)-Scopolamine butylbromide; Butylscopolamine bromide
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mAChR
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Neurological Disease
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Scopolamine butylbromide is a competitive antagonist of muscarinic acetylcholine receptor (mAChR) with an IC50 of 55.3 ± 4.3 nM.
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- HY-15319B
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CXCR
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Others
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AMG 487 S-enantiomer is the S enantiomer of AMG 487. AMG 487 is an antagonist of the chemokine receptor CXCR3.
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- HY-P5128
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Satoreotide tetraxetan
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Radionuclide-Drug Conjugates (RDCs)
Somatostatin Receptor
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Cancer
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DOTA-JR11 is a somatostatin receptor 2 （SSTR2）antagonist. DOTA-JR11 can be labeled by 68Ga, used for paired imaging in neuroendocrine tumors (NETs) research . DOTA-JR11 can be used for the synthesis/research of Radionuclide-Drug Conjugates (RDCs).
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- HY-117799
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5-HT Receptor
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Endocrinology
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LY426965 is a potent arylpiperazine compound known for its role as a full antagonist of the serotonin 1A receptor, lacking partial agonist activity. It is identified as a selective 5-HT1A antagonist, showing promise in preclinical studies for treating conditions associated with serotonin dysregulation, such as smoking cessation and depression-related disorders .
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- HY-B1517A
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(RS)-Alprenolol hydrochloride; dl-Alprenolol hydrochloride
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5-HT Receptor
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Cardiovascular Disease
Cancer
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Alprenolol ((RS)-Alprenolol; dl-Alprenolol) hydrochloride is an orally active non-selective β-adrenoceptor antagonist and an antagonist of 5-HT1A and 5-HT1B receptors. Alprenolol hydrochloride is used as an anti-hypertensive, anti-anginal and anti-arrhythmic agent .
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- HY-B1487R
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iGluR
mAChR
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Neurological Disease
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Procyclidine (hydrochloride) (Standard) is the analytical standard of Procyclidine (hydrochloride). This product is intended for research and analytical applications. Procyclidine (Tricyclamol, (±)-Procyclidine) hydrochloride , an anticholinergic agent, is a muscarinic receptor antagonist that also has the properties of an N-methyl-D-aspartate (NMDA) antagonist. Procyclidine hydrochloride can be used in studies of Parkinson's disease and related psychiatric disorders such as Soman-induced epilepsy .
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- HY-108483
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Neurokinin Receptor
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Neurological Disease
Inflammation/Immunology
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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 .
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- HY-13222A
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Opioid Receptor
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Cancer
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BAN ORL 24 free base is a nociceptin/orphanin FQ (N/OFQ) peptide receptor (NOP) antagonist. BAN ORL 24 free base has antagonistic effect for nociceptin (NOP) receptor with KI value of 0.24 nM in CHO cell. BAN ORL 24 free base can be used for the research of cancer and analgesic .
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- HY-115487
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Prostaglandin Receptor
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Inflammation/Immunology
Cancer
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MF-766 is a highly potent, selective and orally active EP4 antagonist with a Ki of 0.23 nM. MF-766 behaves as a full antagonist with an IC50 of 1.4 nM (shifted to 1.8 nM in the presence of 10% HS) in the functional assay. MF-766 can be used for cancer and inflammation diseases research .
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- HY-B1517
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(RS)-Alprenolol; dl-Alprenolol
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5-HT Receptor
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Cardiovascular Disease
Cancer
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Alprenolol ((RS)-Alprenolol; dl-Alprenolol) is an orally active non-selective β-adrenoceptor antagonist and an antagonist of 5-HT1A and 5-HT1B receptors. Alprenolol is used as an anti-hypertensive, anti-anginal and anti-arrhythmic agent .
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- HY-P10473A
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Neuromedin U Receptor (NMUR)
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Inflammation/Immunology
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CPN-351 TFA (compound 9a), a pentapeptide, is a selective antagonist of human NMUR1 with a pA2 of 7.35. The antagonistic effect of CPN-351 TFA on human NMUR1 is 10 times higher than that on NMUR2. CPN-351 TFA can be used in the study of inflammation .
X
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-
- HY-19638
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AR-C69931MX
|
P2Y Receptor
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Cardiovascular Disease
Inflammation/Immunology
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Cangrelor (AR-C69931MX), an adenosine triphosphate analogue, is an intravenous, reversible and selective platelet P2Y12 antagonist, with prompt and potent antiplatelet effects. Cangrelor directly blocks adenosine diphosphate (ADP)-induced activation and aggregation of platelets. Cangrelor is also a nonspecific GPR17 antagonist .
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- HY-121186R
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Adrenergic Receptor
Calcium Channel
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Neurological Disease
Metabolic Disease
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Bevantolol (hydrochloride) (Standard) is the analytical standard of Bevantolol (hydrochloride). This product is intended for research and analytical applications. Bevantolol hydrochloride is a selective β1 and α1-adrenergic receptor antagonist with pKi values of 7.83, 6.9 in rat cerebral cortex, respectively. Bevantolol hydrochloride is a potent Ca 2+ antagonist .
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- HY-B0982
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-
- HY-120792
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mAChR
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Others
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DAU 5884 is a muscarinic receptor antagonist with activity that discriminates between different muscarinic receptor subtypes. DAU 5884 discriminates between M4 and M2 receptor sites and is a highly potent M1-selective antagonist with specific activity at different muscarinic receptors characterized by radioligand binding studies and functional assays.
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- HY-149434
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Androgen Receptor
Apoptosis
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Cancer
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PROTAC AR-NTD antagonist 1 (compound 18) is a small molecule protein-targeting chimera (PROTACs) targeting the Androgen Receptor AR-V7. PROTAC AR-NTD antagonist 1 antagonizes the N-terminal domain of AR (AR-NTD), degrades AR-V7 protein, and induces apoptosis in prostate cancer (PC) cells. The efficiencies of PROTAC AR-NTD antagonist 1 in degrading AR-V7 in VCaP cells were 62.2% (1 μM) and 71.1% (5 μM), respectively .
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- HY-10064
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-
- HY-B1510S
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-
- HY-112629
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-
- HY-107696
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-
- HY-P2067
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GnRH Receptor
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Endocrinology
Cancer
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Argtide is a luteinizing hormone-releasing hormone (LHRH) antagonist. Argtide is used in endometriosis and cancer-related research .
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- HY-103201
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-
- HY-10664
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-
- HY-B0538A
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- HY-152850A
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Androgen Receptor
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Endocrinology
Cancer
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Gumelutamide (monosuccinate) is a tetrahydropyridopyrimidine compound, acting as an antiandrogen, antineoplastic agent. Gumelutamide (monosuccinate) is an androgen antagonist .
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-
- HY-139572
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BAY-2327949
|
Vasopressin Receptor
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Metabolic Disease
|
|
Enuvaptan (BAY-2327949) is a vasopressin receptor antagonist and has the potential for research into renal and cardiovascular diseases .
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-
- HY-123655
-
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iGluR
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Neurological Disease
|
|
Fenazinel dihydrochloride, an N-methyl-D-aspartate (NMDA) receptor antagonist, shows promise as a potential treatment for ischemic stroke.
|
-
- HY-100318
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-
- HY-16502
-
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Transcrocetin disodium; trans-Crocetin disodium
|
iGluR
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Cancer
|
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Crocetin (Transcrocetin) disodium, extracted from saffron (Crocus sativus L.), acts as an NMDA receptor antagonist with high affinity.
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-
- HY-105221
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-
- HY-14538S
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-
- HY-19658
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-
- HY-123142
-
-
- HY-120689
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-
- HY-17512
-
-
- HY-15195
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-
- HY-P5171
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|
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Wnt
|
Cancer
|
|
MDGCEL is a WNT5A peptide, that acts as a WNT5A mimicks and exhibits WNT5A antagonistic activity .
|
-
- HY-W018061
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CP101,606
|
iGluR
|
Neurological Disease
|
|
Traxoprodil (CP101,606) is a potent and selective NMDA antagonist and protect hippocampal neurons with an IC50 of 10 nM.
|
-
- HY-12635
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-
- HY-13059B
-
|
|
iGluR
|
Neurological Disease
|
|
SDZ 220-581 hydrochloride is an orally active, potent, competitive NMDA receptor antagonist with pKi value of 7.7 .
|
-
- HY-101542
-
-
- HY-U00356
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-
- HY-15462
-
-
- HY-19768
-
-
- HY-U00392
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-
- HY-W701635
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-
- HY-19736
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-
- HY-125463
-
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|
nAChR
|
Neurological Disease
|
|
ANQ9040 is a steroidal relaxant. ANQ9040 is a relatively low-affinity and non-depolarizing nicotinic antagonist .
|
-
- HY-19057A
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-
- HY-B1435
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-
- HY-B1225A
-
|
Romtiazin; Ampazine; Berophen
|
Dopamine Receptor
|
Neurological Disease
|
|
Promazine (Romtiazin) is an antipsychotic and a dopamine receptor D2 antagonist. Promazine inhibits dopaminergic neurotransmission .
|
-
- HY-125701
-
|
|
GnRH Receptor
|
Endocrinology
|
|
A-76154, an octapeptide, is a potent reduced-size luteinizing hormone-releasing hormone (LHRH) antagonist .
|
-
- HY-142214
-
|
|
TRP Channel
|
Others
|
|
TRPA1-IN-1 is a potent, selective, and orally bioavailable TRPA1 small molecule antagonist.
|
-
- HY-76511
-
-
- HY-118420
-
|
|
RAR/RXR
|
Cancer
|
|
BMS-185411 is a selective retinoic acid receptor alpha (RARα) antagonist, with an IC50 value of 140 nM .
|
-
- HY-13059
-
![[Tyr6,D-Phe7,D-His9]-Substance P (6-11)](http://file.medchemexpress.com/product_pic/hy-p10619.gif)
