|Description||atrasentan hydrochloride is the orally available hydrochloride salt of pyrrolidine-3-carboxylic acid with potential antineoplastic activity. As a selective antagonist of the endothelin-A (ETA) receptor, atrasentan binds selectively to the ETA receptor, which may result in inhibition of endothelin-induced angiogenesis and tumor cell proliferation.|
|Synonyms||US brand name: Xinlay; Code names: (+)-A 127722; ABT-627; A 127722; Xinlay; ABT 627; NSC720763; A-147627.|
|Current Developer||Abbott Laboratories|
Clazosentan, also called as AXV 034, Ro 61-1790 or VML 588, a novel endothelin A antagonist, improves cerebral blood flow and behavior after traumatic brain inj...
Sparsentan, also known as RE-021, BMS346567, is a dual antagonist of both angiotensin II and endothelin A receptor antagonist.
Macitentan is an orally available dual endothelin receptor (ETR) antagonist with potential antihypertensive and antineoplastic activity.
Fandosentan potassium is an endothelin A antagonist developed for the treatment of pulmonary hypertension.
Sarafotoxin S6a is an endothelin receptor agonist (EC50 = 7.5 and > 150 nM for contraction of pig coronary artery and guinea pig aorta, respectively).
Sitaxsentan, also called as IPI 1040 or TBC 11251, is a potent orally bioactive ET receptor antagonist that has a long duration of action (t1/2, 5–7 hours) and ...
SB-209670 has been found to be an endothelin receptor antagonist that was once studied against arrhythmias and hypertension.
Endothelin 1 swine, human
Endothelin 1 (swine, human), a vasoconstrictor increased in plasma and explants of patients with uterine leiomyomas, is a synthetic peptide with the sequence of...
A 127722 is a potent and selective ETA endothelin receptor antagonist (IC50 = 0.11 nM and 98 nM for human ETA and ETB receptors, respectively). It attenuates hy...
Zibotentan (ZD4054)is an orally administered, potent and specific ETA-receptor (endothelin A receptor) antagonist (IC50 = 21 nM).
CI 1020 has been found to be a novel endothelin-A receptor antagonist and could be used as an antihypertensive agent.
Endothelin 3 (human, rat)
Endothelin 3 is a ligand of the endothelin (ET) receptors and a potent vasoconstrictor. Endothelin 3 increases blood pressure in spontaneously hypertensive and ...
BMS 182874 Hydrochloride
This active molecular is a selective non-peptide Endothelin ETA receptor antagonist. It displays more than 1000-fold selectivity over ETB receptors (Ki of 48 nM...
Sitaxentan sodium inhibits ET-1-induced stimulation of phosphoinositide turnover with a Ki of 0.69 nM and a pA2 of 8.0.
N-Despropyl-macitentan, an active metabolite of Macitentan, is a dual ET receptor antagonist with longer half-life than Macitentan. It has been proved to be eff...
Bosentan is an endothelin (ET) receptor antagonist for ET-A and ET-B with Ki of 4.7 nM and 95 nM, respectively.
Avosentan, also known as SPP301, R-639, and RO 67-0565, is a potent and selective endothelin receptor(ETA receptor) antagonist.
Atrasentan hydrochloride is the hydrochloride salt form of Atrasentan. Atrasentan, also called as ABT-627, is a selective and orally available antagonist of ETA...
BQ-3020 is a potent and selective ETB endothelin receptor agonist (Ki = 0.18 and 970 nM at human ETB and ETA receptors, respectively).
Sarafotoxin S6b is a non-selective endothelin receptor agonist with vasoconstrictor activity.