Endothelin Receptor Antagonist

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 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.

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.

Sparsentan (RE-021) is a highly potent dual angiotensin II and endothelin A receptor antagonist with K_is of 0.8 and 9.3 nM, respectively.

Atrasentan (ABT-627) is an endothelin receptor antagonist with IC₅₀ of 0.0551 nM for ET_A.

Atrasentan hydrochloride (ABT-627 hydrochloride) is a selective endothelin A receptor antagonist with an IC₅₀ of 0.0551 nM for ET_A.

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.

Patecibart is a humanized immunoglobulin G4-kappa, anti-EDNRA monoclonal antibody. Patecibart is an endothelin receptor antagonist.

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.

Enrasentan (SB 217242) is an endothelin (ET) receptor antagonist. Enrasentan has antihypertensive effects.

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.

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).

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.

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.

Sulfatroxazole-d₄ (Isosulfafurazole-d₄) is the deuterium labeled Sulfatroxazole (HY-105829). Sulfatroxazole (Isosulfafurazole) (compound 12) is a selective antagonist of ETA receptor (IC₅₀ of 0.26 μM).

BMS-248360 is a potent and orally active dual antagonist of both angiotensin II receptor (AT1) and endothelin A (ET_A) receptor, with K_is of 10 nM and 1.9 nM for hAT1 and hETA receptor, respectively. BMS-248360 displays hypertensive effects.

ETA antagonist 1 is a ETA selective antagonist with an IC₅₀ of 0.08 μM.

JKC 302 is an ET-A receptor antagonist. JKC 302 partly blocks ET-1-induced contraction in asthmatic rat trachea ring.

PD 142893 is a endothelin-B receptor antagonist.

K-8794 is an orally active selective endothelin receptor ET_B antagonist that can be used in research on cardiovascular diseases.