IRL-2500 is a potent and selective endothelin-B receptor antagonist. IRL-2500 inhibited the binding of [125I]-endothelin-1 (ET-1) to human ETB (IC50 1.3 +/- 0.2 nM) and ETA (IC50 94 +/- 3 nM) receptors expressed in transfected Chinese hamster ovary (CHO) cells. In in vitro studies, IRL 2500 inhibited the sarafotoxin S6c (STX6c)-mediated contraction of the dog saphenous vein (pKb 7.77) and the STX6c-induced relaxation of the preconstricted rabbit mesenteric artery (pKb 6.92). IRL 2500 also attenuated the IRL 1620-mediated increase in renal vascular resistance (RVR) in the anesthetized rat. References: Bergdahl A, Valdemarsson S, Adner M, Sun XY, Hedner T, Edvinsson L. Enhanced endothelin-1-induced contractions in mesenteric arteries from rats with congestive heart failure: role of ET(B) receptors. Eur J Heart Fail. 2001 Jun;3(3):293-9. PubMed PMID: 11377999.

纯度：≥98%

CAS：169545-27-1