ET_A Antagonist

ET_A Antagonists (27):

Cat. No.	Product Name	Effect	Purity

HY-14184

Macitentan	Antagonist	99.95%
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-13209

Ambrisentan	Antagonist	99.95%
Ambrisentan is a selective ET type A receptor (ETAR) antagonist.

HY-12378

BQ-123	Antagonist	99.78%
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-B0323

Sulfisoxazole	Antagonist	99.90%
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.

HY-102092

FR139317	Antagonist
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-117634

WS009B	Antagonist
WS009B is a selective endothelin receptor antagonist (ET-1: IC₅₀=0.67 μM; ET-2: IC₅₀=0.8 μM). WS009B can be used in the study of cardiovascular diseases.

HY-122237

ATZ-1993	Antagonist
ATZ-1993 is an orally active, nonpeptide endothelin receptor subtype Aand endothelin receptor subtype B antagonist with pK_i 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.

HY-15895

Aprocitentan	Antagonist	99.98%
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-10088

Zibotentan	Antagonist	98.97%
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-120295

A-192621	Antagonist	99.85%
A-192621 is a potent, nonpeptide, orally active and selective endothelin B (ET_B) receptor antagonist with an IC₅₀ of 4.5 nM and a K_i of 8.8 nM. The selectivity of A-192621 is 636-fold higher than ET_A (IC₅₀ of 4280 nM and K_i 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.

HY-17351

Tezosentan	Antagonist	98.79%
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-103460

IRL 2500	Antagonist	≥99.0%
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-106994A

Nebentan potassium	Antagonist	99.53%
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-19431

Ro 46-8443	Antagonist	98.93%
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-106994

Nebentan	Antagonist	99.67%
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-118497

BMS 182874	Antagonist	99.85%
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-14184S

Macitentan-d₄	Antagonist	98.03%
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-19529

Ro 46-2005	Antagonist	98.32%
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-135283

ABT-546	Antagonist
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-13209C

Ambrisentan sodium	Antagonist
Ambrisentan (BSF 208075) sodium is a selective and orally active ET type A receptor (ETAR) antagonist.

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