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Results for "

ETA Antagonist

" in MedChemExpress (MCE) Product Catalog:

By Targets:	Angiotensin Receptor (1) Apoptosis (5) Drug Metabolite (1) Endothelin Receptor (51) Isotope-Labeled Compounds (2)
By Research Areas:	Cancer (14) Cardiovascular Disease (48) Endocrinology (26) Infection (1) Inflammation/Immunology (3) Metabolic Disease (2) Neurological Disease (2)

Inhibitors & Agonists

Peptides

Isotope-Labeled Compounds

Cat. No.	Product Name	Target	Research Areas	Chemical Structure

HY-118497

BMS 182874	Endothelin Receptor	Cardiovascular Disease Metabolic Disease
BMS 182874 is an orallyactive, highly selective endothelin receptor (ET_A receptor) antagonist, with IC₅₀ value of 0.150 μM, K_i 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-15403

Atrasentan 5 Publications Verification ABT-627; (+)-A 127722; A-147627	Endothelin Receptor	Cardiovascular Disease Endocrinology Cancer
Atrasentan (ABT-627) is an endothelin receptor antagonist with IC₅₀ of 0.0551 nM for ET_A .

HY-15403A

Atrasentan hydrochloride 5 Publications Verification ABT-627 hydrochloride; (+)-A 127722 hydrochloride; A-147627 hydrochloride	Endothelin Receptor	Cardiovascular Disease Endocrinology Cancer
Atrasentan hydrochloride (ABT-627 hydrochloride) is a selective endothelin A receptor antagonist with an IC₅₀ of 0.0551 nM for ET_A .

HY-112264

ETA antagonist 1	Endothelin Receptor	Cardiovascular Disease
ETA antagonist 1 is a *ETA* selective antagonist with an IC₅₀ of 0.08 μM.

HY-101262

SB234551	Endothelin Receptor	Neurological Disease
SB234551 is a selective endothelin *ETA* receptor antagonist. SB234551 can be used in the study of stroke model .

HY-103458

BMS 182874 hydrochloride	Endothelin Receptor	Cardiovascular Disease Metabolic Disease
BMS 182874 hydrochloride is an orallyactive, highly selective endothelin receptor (ET_A receptor) antagonist, with IC₅₀ value of 0.150 μM, K_i 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-114674A

Atrasentan sodium	Endothelin Receptor	Cardiovascular Disease Endocrinology Cancer
Atrasentan sodium is an endothelin receptor antagonist with IC₅₀ of 0.0551 nM for ET_A .

HY-19263

BMS-193884	Endothelin Receptor	Cardiovascular Disease
BMS-193884 is a selective, orally active, and competitive *ET_A* antagonist with 10000-fold greater affinity for the human ET_A receptor (K_i=1.4 nM) than for the ET_B receptor .

HY-76520

Sitaxsentan IPI 1040; TBC-11251	Endothelin Receptor	Cardiovascular Disease Endocrinology
Sitaxsentan (IPI 1040; TBC-11251) is a selective endothelin A (ETA) receptor antagonist.

HY-117644

L-749329 (Rac)-L-754142	Endothelin Receptor	Cardiovascular Disease
L-749329 ((Rac)-L-754142) is an *ET_A* and ET_B receptor antagonist, with K_is of 0.062 nM and 2.25 nM for ET_A and ET_B respectively. L-749329 inhibits ET-1-stimulated signaling .

HY-19274

ZD-1611	Endothelin Receptor	Cardiovascular Disease Endocrinology
ZD-1611 is a potent, orally active, selective ETA receptor antagonist, used for the research of ischemic stroke.

HY-15195

Avosentan Ro 67-0565; SPP-301	Endothelin Receptor	Cardiovascular Disease Endocrinology
Avosentan(Ro 67-0565; SPP-301) is a potent, selective endothelin receptor(ETA receptor) antagonist.

HY-118695

IRL-3630	Endothelin Receptor	Inflammation/Immunology
IRL-3630 (Compound 3) is an *ETA/ETB* antagonist (K_i: 1.9 and 1.2 nM) .

HY-105829

Sulfatroxazole Isosulfafurazole	Endothelin Receptor	Cardiovascular Disease
Sulfatroxazole (Isosulfafurazole) (compound 12) is a selective antagonist of *ETA* receptor (IC₅₀=0.26 μM) .

HY-15404

Darusentan Lu-135252	Endothelin Receptor	Cardiovascular Disease Endocrinology
Darusentan (Lu-135252) is a selective endothelin receptor A (ET-A) receptor antagonist, which binds with a K_i of 1.4 nM to the ET-A receptor and a K_i 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 K_i of 13 nM .

HY-101598

PD-159020	Endothelin Receptor	Cardiovascular Disease Endocrinology
PD-159020 is a non-selective *ETA/ETB* antagonist, with IC₅₀s of 30 and 50 nM for hETA and hETB, respectively.

HY-A0013

Bosentan Maximum Cited Publications 23 Publications Verification	Endothelin Receptor	Cardiovascular Disease Endocrinology Cancer
Bosentan is a competitive and dual antagonist of endothelin-1 (ET) for the ET_A and ET_B receptors with K_i of 4.7 nM and 95 nM in human SMC, respectively.

HY-A0013A

Bosentan hydrate Maximum Cited Publications 23 Publications Verification	Endothelin Receptor	Cardiovascular Disease Endocrinology Cancer
Bosentan hydrate is a competitive and dual antagonist of endothelin-1 (ET) for the ET_A and ET_B receptors with K_i of 4.7 nM and 95 nM in human SMC, respectively.

HY-17351

Tezosentan RO 610612	Endothelin Receptor	Cardiovascular Disease Neurological Disease Endocrinology Cancer
Tezosentan (RO 610612) is an endothelin (ET) receptor antagonist, with pA₂s of 9.5, 7.7 for ET_A and ET_B receptors, respectively.

HY-135500

ACT-373898	Endothelin Receptor	Endocrinology
ACT-373898 is an inactive carboxylic acid metabolite of Macitentan. Macitentan is an orally active, non-peptide dual ETA and ETB (endothelin receptor) antagonist .

HY-15402D

Edonentan hydrate BMS 207940 hydrate	Endothelin Receptor	Cardiovascular Disease
Edonentan (BMS 207940) hydrate is a potent and selective antagonist of the *endothelin A (ETA) receptor, with a K_i* of 10 pM. In rats, Edonentan has superior (100%) oral bioavailbility .

HY-135283

ABT-546 A-216546	Endothelin Receptor	Cardiovascular Disease Endocrinology
ABT-546 (A-216546) is a potent, highly selective and active *endothelin ET_A* receptor** antagonist with a K_i of 0.46 nM for [ ¹²⁵I]endothelin-1 binding to cloned human endothelin ET_A. ABT-546 is >25,000-fold more selective for the ET_A receptor than for the ET_B receptor. ABT-546 blocks endothelin-1-induced arachidonic acid release and phosphatidylinositol hydrolysis with IC₅₀ of 0.59 nM and 3 nM, respectively .

HY-114674

A-127722	Endothelin Receptor	Cardiovascular Disease
A-127722 is A 2, 4-dialarylpyrrolidine-3-carboxylic acid ET_A selective endothelin receptor (ET receptor) antagonist with IC₅₀ value of 0.36 nM .

HY-115417

Bosentan-d4	Endothelin Receptor	Cardiovascular Disease Endocrinology
Bosentan-d4 is the deuterium labeled Bosentan. Bosentan is a competitive and dual antagonist of endothelin-1 (ET) for the ET_A and ET_B receptors with K_i of 4.7 nM and 95 nM in human SMC, respectively.

HY-106994A

Nebentan potassium YM598	Endothelin Receptor	Cardiovascular Disease Inflammation/Immunology Cancer
Nebentan potassium (YM598) is a potent, selective and orally active non-peptide *endothelin ET_A* 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 K_i of 0.697 nM and 569 nM, respectively . YM598 can ameliorate the progression of cor pulmonale and myocardial infarction in vivo .

HY-14184

Macitentan 10+ Cited Publications ACT-064992	Endothelin Receptor Apoptosis	Cardiovascular Disease Endocrinology Cancer
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) .

HY-P10151

PD 156252	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-106994

Nebentan YM598 free base	Endothelin Receptor	Cardiovascular Disease Inflammation/Immunology Cancer
Nebentan (YM598 free base) is a potent, selective and orally active non-peptide *endothelin ET_A* receptor** antagonist through the modification of Bosentan (HY-A0013). Nebentan inhibits [ ¹²⁵I] endothelin-1 binding to cloned human endothelin ETA and ETB receptor, with K_i of 0.697 nM and 569 nM, respectively . YM598 can ameliorate the progression of cor pulmonale and myocardial infarction in vivo .

HY-17352

Clazosentan Ro 61-1790; VML 588; AXV-034343	Endothelin Receptor	Cardiovascular Disease
Clazosentan (Ro 61-1790) is a selective *endothelin A (ET_A)* receptor** antagonist. Clazosentan inhibits ET-1-mediated vasoconstriction. Clazosentan prevents cerebral vasospasm, vasospasm-related cerebral infarction .

HY-A0013R

Bosentan (Standard)	Endothelin Receptor	Cardiovascular Disease Endocrinology Cancer
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 ET_A and ET_B receptors with K_i of 4.7 nM and 95 nM in human SMC, respectively.

HY-A0013AR

Bosentan (hydrate) (Standard)	Endothelin Receptor	Cardiovascular Disease Endocrinology Cancer
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.

HY-19529

Ro 46-2005	Endothelin Receptor	Cardiovascular Disease Endocrinology
Ro 46-2005 is a novel synthetic non-peptide endothelin receptor antagonist, inhibits the specific binding of 125I-ET-1 to human vascular smooth muscle cells (ETA receptor) with IC50 of 220 nM.

HY-102092

FR139317 PD 147953	Endothelin Receptor	Cardiovascular Disease
FR139317 (PD 147953) is a selective ET_A receptor antagonist. FR139317 inhibits cerebral activation by intraventricular endothelin-1 in conscious rats. FR139317 also ameliorates cerebral vasospasm in dogs .

HY-14184A

Macitentan (n-butyl analogue)	Endothelin Receptor	Cardiovascular Disease Endocrinology
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).

HY-17352A

Clazosentan disodium Ro 61-1790 disodium; VML 588 disodium; AXV-034343 disodium	Endothelin Receptor	Cardiovascular Disease
Clazosentan disodium (Ro 61-1790) is a selective *endothelin A (ET_A)* receptor** antagonist. Clazosentan disodium inhibits ET-1-mediated vasoconstriction. Clazosentan disodium prevents cerebral vasospasm, vasospasm-related cerebral infarction .

HY-10088

Zibotentan ZD4054	Endothelin Receptor Apoptosis	Endocrinology Cancer
Zibotentan (ZD4054) is a potent, selective and orally active *endothelin A (ET_A)* receptor** antagonist with a K_i 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 .

HY-14184S

Macitentan-d4 ACT-064992-d₄	Isotope-Labeled Compounds Endothelin Receptor Apoptosis	Cardiovascular Disease
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].

HY-19431

Ro 46-8443	Endothelin Receptor	Cardiovascular Disease
Ro 46-8443 is the first non-peptide endothelin ET_B receptor selective antagonist. Ro 46-8443 displays an at least 100-fold selectivity for ET_B (IC₅₀: 34-69 nM) over ET_A receptors (IC₅₀: 6800 nM) .

HY-15402

Edonentan BMS 207940	Endothelin Receptor	Cardiovascular Disease
Edonentan (BMS 207940) is an antagonist for endothelin receptor (ET_A receptor), with a K_i 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 .

HY-114953

BMS-248360	Angiotensin Receptor Endothelin Receptor	Cardiovascular Disease
BMS-248360 is a potent and orally active dual antagonist of both angiotensin II receptor (AT1) and *endothelin A (ET_A)* receptor, with K_i**s of 10 nM and 1.9 nM for hAT1 and hETA receptor, respectively. BMS-248360 displays hypertensive effects .

HY-15895

Aprocitentan 2 Publications Verification ACT-132577	Endothelin Receptor	Cardiovascular Disease Endocrinology
Aprocitentan (ACT-132577) is the major and pharmacologically active metabolite of Macitentan. Aprocitentan is an orally active dual *ETA/ETB* antagonist with IC₅₀s of 3.4 nM and 987 nM, and pA₂ valus of 6.7 and 5.5, respectively. Aprocitentan is an antihypertensive agent .

HY-15894A

BQ-788 5+ Cited Publications	Endothelin Receptor	Cardiovascular Disease Endocrinology Cancer
BQ-788 is a potent, selective ETB receptor antagonist with IC₅₀ of 1.2 nM for inhibition of ET-1 binding to human Girardi heart cells, poorly inhibiting the binding to ETA receptors in human neuroblastoma cell line SK-N-MC cells with IC₅₀ of 1300 nM .

HY-14184R

Macitentan (Standard)	Endothelin Receptor Apoptosis	Cardiovascular Disease Endocrinology Cancer
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) .

HY-103460

IRL 2500	Endothelin Receptor	Cardiovascular Disease
IRL 2500 is a potent Endothelin receptor antagonist. IRL 2500 shows IC₅₀?values of 1.3 and 94 nM for ET_B?and ET_A?receptors, respectively. IRL 2500 inhibits ETB?receptor-mediated blood pressure increase and renal vascular resistance in rats?in vivo .

HY-12378

BQ-123 2 Publications Verification	Endothelin Receptor	Cardiovascular Disease
BQ-123 is a potent and selective *endothelin A (ETA) receptor* antagonist with an IC₅₀ of 7.3 nM and a K_i 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 .

HY-15895S

Aprocitentan-d4 ACT-132577 d₄	Isotope-Labeled Compounds Endothelin Receptor	Cardiovascular Disease Endocrinology
Aprocitentan-d₄ is a deuterium labeled Aprocitentan. Aprocitentan is a major and pharmacologically active metabolite of Macitentan. Aprocitentan is an orally active dual ETA/ETB antagonist with IC50s of 3.4 nM and 987 nM, and pA2 valus of 6.7 and 5.5, respectively. Aprocitentan is an antihypertensive agent .

HY-12378A

BQ-123 TFA	Endothelin Receptor	Cardiovascular Disease
BQ-123 TFA is a potent and selective *endothelin A (ETA) receptor* antagonist with an IC₅₀ of 7.3 nM and a K_i 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 .

HY-15895R

Aprocitentan (Standard)	Endothelin Receptor	Cardiovascular Disease Endocrinology
Aprocitentan (Standard) is the analytical standard of Aprocitentan. This product is intended for research and analytical applications. Aprocitentan (ACT-132577) is the major and pharmacologically active metabolite of Macitentan. Aprocitentan is dual ETA/ETB antagonist with IC50s of 3.4 nM and 987 nM, and pA2 valus of 6.7 and 5.5, respectively .

HY-135390

Hydroxy desmethyl Bosentan Ro 64-1056	Drug Metabolite	Cardiovascular Disease
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 ET_A and ET_B receptors with K_i of 4.7 nM and 95 nM in human SMC, respectively. Bosentan can be used in treatment of pulmonary arterial hypertension .

HY-103459

CI-1020 PD156707	Endothelin Receptor	Cardiovascular Disease
CI-1020 (PD156707) is an orally active and selective antagonist targeting endothelin (ET_A) with an IC₅₀ value of 0.3 nM. CI-1020 blocks intimal hyperplasia in human saphenous veins completely in organ culture. CI 1020 inhibits hypoxic pulmonary hypertension and blocks ET-1-induced pressor responses following oral administration .

Cat. No.	Product Name	Target	Research Area

HY-12378

BQ-123 2 Publications Verification	Endothelin Receptor	Cardiovascular Disease
BQ-123 is a potent and selective *endothelin A (ETA) receptor* antagonist with an IC₅₀ of 7.3 nM and a K_i 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 .

HY-105183

PD 145065	Peptides	Others
PD 145065 is a highly potent but non-selective endothelin receptor antagonist with an IC₅₀ value of 4 nM for the ET_A receptor for rabbit renal artery vascular smooth muscle cells .

HY-P10151

PD 156252	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.

Cat. No.	Product Name	Chemical Structure

HY-14184S

Macitentan-d4
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].

HY-15895S

Aprocitentan-d4
Aprocitentan-d₄ is a deuterium labeled Aprocitentan. Aprocitentan is a major and pharmacologically active metabolite of Macitentan. Aprocitentan is an orally active dual ETA/ETB antagonist with IC50s of 3.4 nM and 987 nM, and pA2 valus of 6.7 and 5.5, respectively. Aprocitentan is an antihypertensive agent .

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