Home > Inhibitors & Agonists > GPCR > Endothelin Receptor
Cat. No. Product name CAS No.
DCAPI1496 Ambrisentan Featured

A nonpeptide endothelin ETA receptor antagonist. Antihypertensive.

177036-94-1
DC8191 Sparsentan(PS433540)

acting as both an Endothelin Receptor Antagonist (ERA) and Angiotensin Receptor Blocker (ARB).

254740-64-2
DC11513 Aprocitentan (ACT-132577) Featured

Aprocitentan (ACT-132577) is the major and pharmacologically active metabolite of macitentan, which is dual ETA/ETB antagonist designed for tissue targeting.

1103522-45-7
DC10018 Atrasentan hydrochloride Featured

Atrasentan Hcl(A-147627) is an endothelin antagonist receptor (IC50=0.0551 nM, ETA) being developed for the treatment of prostate cancer.

195733-43-8
DC9436 Avosentan

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

290815-26-8
DC9437 Bosentan

Bosentan is a competitive and dual antagonist of endothelin-1 at the endothelin-A (ET-A) and endothelin-B (ET-B) receptors.

147536-97-8
DCAPI1483 Bosentan Hydrate

Bosentan is an endothelin (ET) receptors antagonist for ET-A and ET-B with Ki of 4.7 nM and 95 nM, respectively.

157212-55-0
DC8392 BQ-123 Featured

BQ-123 is a selective endothelin A receptor (ETA) antagonist with IC50 of 7.3 nM. Phase 2.

136553-81-6
DC12498 S-Darusentan Featured

Darusentan is a potent inhibitor of endothelin signaling and function in both large and small arteries.

171714-84-4
DC1012 Macitentan (Actelion-1,ACT-064992)

macitentan (Actelion-1, ACT-064992) is an orally active, non-peptide dual endothelin (ET)A/B receptor antagonist with IC50 of 0.5 nM/391 nM.

441798-33-0
DC9666 Ro 46-2005 Featured

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.

150725-87-4
DC4108 Sitaxentan sodium

Sitaxentan sodium (TBC-11251) is a selective endothelin receptor-A antagonist with IC50 and Ki of 1.4 nM and 0.43 nM, respectively.

210421-74-2
DC9435 Zibotentan(ZD4054) Featured

Zibotentan (ZD4054) is an orally administered, potent and specific ETA-receptor (endothelin A receptor) antagonist (IC50 = 21 nM).

186497-07-4
DC28162 IRL 2500

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.

169545-27-1
DC28408 A-192621

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.

195529-54-5
DC28795 ABT-546

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.

212481-66-8
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