Search Result
Results for "
Endothelin Receptor Antagonist
" in MedChemExpress (MCE) Product Catalog:
2
Isotope-Labeled Compounds
| Cat. No. |
Product Name |
Target |
Research Areas |
Chemical Structure |
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- HY-118497
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Endothelin Receptor
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Cardiovascular Disease
Metabolic Disease
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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 .
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- HY-B0323
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Sulfafurazole
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Endothelin Receptor
Bacterial
Antibiotic
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Infection
Endocrinology
Cancer
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Sulfisoxazole (Sulfafurazole) is an orally active endothelin receptor antagonist with IC50 values of 0.60 μM and 22 μM against endothelin receptor A and endothelin receptor B, respectively. Sulfisoxazole is a sulfonamide antibacterial agent with an oxazole substituent. Sulfisoxazole inhibits breast cancer exosome release by targeting endothelin receptor A .
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- HY-A0013
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- HY-A0013A
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- HY-103458
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Endothelin Receptor
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Cardiovascular Disease
Metabolic Disease
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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 .
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- HY-105168
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Endothelin Receptor
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Cardiovascular Disease
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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 .
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- HY-B0323A
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Sulfafurazole diethanolamine
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Endothelin Receptor
Antibiotic
Bacterial
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Infection
Endocrinology
Cancer
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Sulfisoxazole (Sulfafurazole) diethanolamine is an endothelin receptor antagonist with IC50 values of 0.60 μM and 22 μM against endothelin receptor A and endothelin receptor B, respectively. Sulfisoxazole diethanolamine is a sulfonamide antibacterial with an oxazole substituent. Sulfisoxazole diethanolamine inhibits breast cancer exosome release by targeting endothelin receptor A .
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- HY-P2057
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- HY-15402
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BMS 207940
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Endothelin Receptor
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Cardiovascular Disease
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Edonentan (BMS 207940) is an antagonist for endothelin receptor (ETA receptor), with a Ki of 10 pM. Edonentan is metabolic stable, exhibits good pharmakokinetic characters in rats. Edonentan regulates the endothelin system, blocks the big Endothelin-induced pressor response in rats model .
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- HY-114674A
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- HY-B0323R
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Endothelin Receptor
Bacterial
Antibiotic
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Infection
Endocrinology
Cancer
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Sulfisoxazole (Standard) is the analytical standard of Sulfisoxazole. This product is intended for research and analytical applications. Sulfisoxazole (Sulfafurazole) is an orally active endothelin receptor antagonist with IC50 values of 0.60 μM and 22 μM against endothelin receptor A and endothelin receptor B, respectively. Sulfisoxazole is a sulfonamide antibacterial agent with an oxazole substituent. Sulfisoxazole inhibits breast cancer exosome release by targeting endothelin receptor A .
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- HY-P1018
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- HY-15195
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- HY-76520
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- HY-123744
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- HY-135283
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A-216546
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Endothelin Receptor
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Cardiovascular Disease
Endocrinology
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ABT-546 (A-216546) is a potent, highly selective and active endothelin ETA receptor antagonist with a Ki of 0.46 nM for [ 125I]endothelin-1 binding to cloned human endothelin ETA. ABT-546 is >25,000-fold more selective for the ETA receptor than for the ETB receptor. ABT-546 blocks endothelin-1-induced arachidonic acid release and phosphatidylinositol hydrolysis with IC50 of 0.59 nM and 3 nM, respectively .
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- HY-11103
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- HY-15403
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- HY-119667
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- HY-115417
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- HY-15403A
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- HY-106994A
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YM598
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Endothelin Receptor
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Cardiovascular Disease
Inflammation/Immunology
Cancer
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Nebentan potassium (YM598) is a potent, selective and orally active non-peptide endothelin ETA receptor antagonist through the modification of Bosentan (HY-A0013). Nebentan potassium inhibits [ 125I] endothelin-1 binding to cloned human endothelin ETA and ETB receptor, with Ki of 0.697 nM and 569 nM, respectively . YM598 can ameliorate the progression of cor pulmonale and myocardial infarction in vivo .
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- HY-106994
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YM598 free base
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Endothelin Receptor
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Cardiovascular Disease
Inflammation/Immunology
Cancer
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Nebentan (YM598 free base) is a potent, selective and orally active non-peptide endothelin ETA receptor antagonist through the modification of Bosentan (HY-A0013). Nebentan inhibits [ 125I] endothelin-1 binding to cloned human endothelin ETA and ETB receptor, with Ki of 0.697 nM and 569 nM, respectively . YM598 can ameliorate the progression of cor pulmonale and myocardial infarction in vivo .
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- HY-17351
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- HY-A0013R
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Endothelin Receptor
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Cardiovascular Disease
Endocrinology
Cancer
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Bosentan (Standard) is the analytical standard of Bosentan. This product is intended for research and analytical applications. Bosentan is a competitive and dual antagonist of endothelin-1 (ET) for the ETA and ETB receptors with Ki of 4.7 nM and 95 nM in human SMC, respectively.
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- HY-A0013AR
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Endothelin Receptor
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Cardiovascular Disease
Endocrinology
Cancer
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Bosentan (hydrate) (Standard) is the analytical standard of Bosentan (hydrate). This product is intended for research and analytical applications. Bosentan hydrate is a competitive and dual antagonist of endothelin-1 (ET) for the ETA and ETB receptors with Ki of 4.7 nM and 95 nM in human SMC, respectively.
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- HY-101262
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- HY-102092
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PD 147953
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Endothelin Receptor
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Cardiovascular Disease
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FR139317 (PD 147953) is a selective ETA receptor antagonist. FR139317 inhibits cerebral activation by intraventricular endothelin-1 in conscious rats. FR139317 also ameliorates cerebral vasospasm in dogs .
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- HY-122237
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Endothelin Receptor
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Cardiovascular Disease
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ATZ-1993 is an orally active, nonpeptide endothelin receptor subtype Aand endothelin receptor subtype B antagonist with pKi values of 8.69, 7.20, respectively. ATZ-1993 has the potential for the research of intimal hyperplasia after balloon denudation of the carotid artery .
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- HY-12378
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BQ-123
2 Publications Verification
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Endothelin Receptor
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Cardiovascular Disease
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BQ-123 is a potent and selective endothelin A (ETA) receptor antagonist with an IC50 of 7.3 nM and a Ki of 25 nM. BQ-123 inhibits endothelin-1-mediated proliferation of human pulmonary artery smooth muscle cells and lowers blood pressure in different rat models of hypertension .
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- HY-12378A
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Endothelin Receptor
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Cardiovascular Disease
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BQ-123 TFA is a potent and selective endothelin A (ETA) receptor antagonist with an IC50 of 7.3 nM and a Ki of 25 nM. BQ-123 TFA inhibits endothelin-1-mediated proliferation of human pulmonary artery smooth muscle cells and lowers blood pressure in different rat models of hypertension .
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- HY-P990089
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- HY-114674
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- HY-15404
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Lu-135252
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Endothelin Receptor
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Cardiovascular Disease
Endocrinology
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Darusentan (Lu-135252) is a selective endothelin receptor A (ET-A) receptor antagonist, which binds with a Ki of 1.4 nM to the ET-A receptor and a Ki of 184 nM to ET-B receptor, respectively with a 100-fold selectivity for ETA rather than ETB receptors . Darusentan competes for radiolabeled endothelin binding in rat aortic vascular smooth muscle cells (RAVSMs) membranes with single-site kinetics, exhibiting a Ki of 13 nM .
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- HY-17621
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- HY-135500
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Endothelin Receptor
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Endocrinology
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ACT-373898 is an inactive carboxylic acid metabolite of Macitentan. Macitentan is an orally active, non-peptide dual ETA and ETB (endothelin receptor) antagonist .
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- HY-15402D
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BMS 207940 hydrate
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Endothelin Receptor
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Cardiovascular Disease
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Edonentan (BMS 207940) hydrate is a potent and selective antagonist of the endothelin A (ETA) receptor, with a Ki of 10 pM. In rats, Edonentan has superior (100%) oral bioavailbility .
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- HY-120843
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Endothelin Receptor
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Cardiovascular Disease
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WS009A is an antagonist for endothelin receptor (ET Receptor) with IC50 of 5.8 and 6.9 μM for ET-1 receptor and ET-2 receptor. WS009A can be used in research of cardiovascular diseases .
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- HY-19529
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- HY-P4201
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Vasopressin Receptor
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Cardiovascular Disease
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JKC 301 is a selective Endothelin A receptor antagonist. JKC 301 attenuates the pressor effects of nicotine in rats. JKC 301 can be used to study cardiovascular disease caused by smoking .
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- HY-114953
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Angiotensin Receptor
Endothelin Receptor
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Cardiovascular Disease
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BMS-248360 is a potent and orally active dual antagonist of both angiotensin II receptor (AT1) and endothelin A (ETA) receptor, with Kis of 10 nM and 1.9 nM for hAT1 and hETA receptor, respectively. BMS-248360 displays hypertensive effects .
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- HY-145516
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Ro 47-8634
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Others
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Metabolic Disease
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Desmethyl bosentan is an active metabolite of the endothelin receptor antagonist bosentan (HY-A0013).1 Desmethyl bosentan (25 μM) activates the pregnane X receptor (PXR) in CV-1 monkey kidney cells expressing the human receptor in a reporter assay.
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- HY-19431
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Endothelin Receptor
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Cardiovascular Disease
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Ro 46-8443 is the first non-peptide endothelin ETB receptor selective antagonist. Ro 46-8443 displays an at least 100-fold selectivity for ETB (IC50: 34-69 nM) over ETA receptors (IC50: 6800 nM) .
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- HY-14184
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- HY-P10151
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Endothelin Receptor
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Cardiovascular Disease
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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.
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- HY-17621S
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- HY-17352
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Ro 61-1790; VML 588; AXV-034343
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Endothelin Receptor
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Cardiovascular Disease
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Clazosentan (Ro 61-1790) is a selective endothelin A (ETA) receptor antagonist. Clazosentan inhibits ET-1-mediated vasoconstriction. Clazosentan prevents cerebral vasospasm, vasospasm-related cerebral infarction .
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- HY-135390
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Ro 64-1056
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Drug Metabolite
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Cardiovascular Disease
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Hydroxy desmethyl Bosentan (Ro 64-105) is a Bosentan metabolism produced by the cytochrome P450 enzymes CYP2C9 and CYP3A4 in the liver . Bosentan is a competitive and dual antagonist of endothelin-1 (ET) for the ETA and ETB receptors with Ki of 4.7 nM and 95 nM in human SMC, respectively. Bosentan can be used in treatment of pulmonary arterial hypertension .
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- HY-103460
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Endothelin Receptor
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Cardiovascular Disease
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IRL 2500 is a potent Endothelin receptor antagonist. IRL 2500 shows IC50?values of 1.3 and 94 nM for ETB?and ETA?receptors, respectively. IRL 2500 inhibits ETB?receptor-mediated blood pressure increase and renal vascular resistance in rats?in vivo .
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- HY-14184A
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Endothelin Receptor
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Cardiovascular Disease
Endocrinology
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Macitentan n-butyl analogue is a n-butyl analogue of Macitentan. Macitentan is an orally active, non-peptide dual endothelin ETA and ETB receptor antagonist for the potential treatment of idiopathic pulmonary fibrosis (IPF) and pulmonary arterial hypertension (PAH).
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- HY-17352A
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Ro 61-1790 disodium; VML 588 disodium; AXV-034343 disodium
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Endothelin Receptor
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Cardiovascular Disease
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Clazosentan disodium (Ro 61-1790) is a selective endothelin A (ETA) receptor antagonist. Clazosentan disodium inhibits ET-1-mediated vasoconstriction. Clazosentan disodium prevents cerebral vasospasm, vasospasm-related cerebral infarction .
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- HY-10088
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ZD4054
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Endothelin Receptor
Apoptosis
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Endocrinology
Cancer
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Zibotentan (ZD4054) is a potent, selective and orally active endothelin A (ETA) receptor antagonist with a Ki of 13 nM. Zibotentan has no inhibitory effect on ETB. Zibotentan has anticancer effects and can be used for castration-resistant prostate cancer (CRPC) research .
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- HY-14184S
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- HY-117634
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- HY-14184R
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Endothelin Receptor
Apoptosis
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Cardiovascular Disease
Endocrinology
Cancer
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Macitentan (Standard) is the analytical standard of Macitentan. This product is intended for research and analytical applications. Macitentan (ACT-064992) is an orally active, non-peptide dual ETA and ETB (endothelin receptor) antagonist. Macitentan has the potential for idiopathic pulmonary fibrosis (IPF) and pulmonary arterial hypertension (PAH) .
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- HY-121300
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(-)-TAN2162
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Antibiotic
Bacterial
Endothelin Receptor
CGRP Receptor
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Infection
Cancer
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Kendomycin ((−)-TAN 2162) is a polyketide antibiotic with remarkable antibacterial and cancer cells cytotoxic activities. Kendomycin tends to be bacteriostatic rather than bactericidal and inhibits the growth of the methicillin-resistant Staphylococcus aureus (MRSA) strain COL at a low concentration (MIC of 5 μg/mL). Kendomycin is a potent antagonist of the endothelin receptor and a calcitonin receptor agonist which plays its role as an anti-osteoporotic agent .
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- HY-W781265
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L-755,805
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Others
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Infection
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BE 24566B is a polyketide fungal metabolite originally isolated from S. violaceusniger. It is active against B. subtilis, B. cereus, S. aureus, M. luteus, E. faecalis, and S. thermophilus (MICs=1.56, 1.56, 1.56, 1.56, 3.13, and 3.13 μg/mL, respectively). BE 24566B is an endothelin (ET) receptor antagonist (IC50s=11 and 3.9 μM for ETA and ETB receptors, respectively).
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- HY-120295
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Endothelin Receptor
Apoptosis
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Cardiovascular Disease
Endocrinology
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A-192621 is a potent, nonpeptide, orally active and selective endothelin B (ETB) receptor antagonist with an IC50 of 4.5 nM and a Ki of 8.8 nM. The selectivity of A-192621 is 636-fold higher than ETA (IC50 of 4280 nM and Ki of 5600 nM). A-192621 promotes apoptosis in PASMCs. A-192621 alos causes elevation of arterial blood pressure and an elevation in the plasma ET-1 level .
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- HY-19210
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Endothelin Receptor
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Cardiovascular Disease
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SB-209670 is an extremely potent and highly specific non-peptide, subnanomolar endothelin (ET) receptor antagonist. SB 209670 selectively inhibits binding of 125I-labeled ET-1 to cloned human ET receptor subtypes ETA and ETB (Ki=0.2 and 18 nM, respectively). SB 209670 produces a dose-dependent reduction in blood pressure in hypertensive rats, protects from ischemia-induced neuronal degeneration in a gerbil stroke model, and attenuates neointima formation following rat carotid artery balloon angioplasty .
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| Cat. No. |
Product Name |
Target |
Research Area |
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- HY-12378
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BQ-123
2 Publications Verification
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Endothelin Receptor
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Cardiovascular Disease
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BQ-123 is a potent and selective endothelin A (ETA) receptor antagonist with an IC50 of 7.3 nM and a Ki of 25 nM. BQ-123 inhibits endothelin-1-mediated proliferation of human pulmonary artery smooth muscle cells and lowers blood pressure in different rat models of hypertension .
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- HY-105183
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Peptides
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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-105168
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Endothelin Receptor
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Cardiovascular Disease
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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 .
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- HY-P2057
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- HY-P1018
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- HY-P4201
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Vasopressin Receptor
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Cardiovascular Disease
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JKC 301 is a selective Endothelin A receptor antagonist. JKC 301 attenuates the pressor effects of nicotine in rats. JKC 301 can be used to study cardiovascular disease caused by smoking .
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- HY-P10151
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Endothelin Receptor
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Cardiovascular Disease
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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.
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| Cat. No. |
Product Name |
Target |
Research Area |
| Cat. No. |
Product Name |
Category |
Target |
Chemical Structure |
| Cat. No. |
Product Name |
Chemical Structure |
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- HY-14184S
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Macitentan-d4 is a deuterium labeled Sulfamethoxazole. Macitentan is an orally active, non-peptide dual ETA and ETB (endothelin) receptor antagonist. Macitentan has the potential for idiopathic pulmonary fibrosis (IPF) and pulmonary arterial hypertension (PAH)[1].
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- HY-17621S
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Sparsentan-d5 is deuterium labeled Sparsentan. Sparsentan (RE-021) is a highly potent dual angiotensin II and endothelin A receptor antagonist with Kis of 0.8 and 9.3 nM, respectively[1].
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