Edonentan, formerly known as BMS-207940, is a highly potent and orally bioavailable ET(A) selective antagonist. Edonentan is an extremely potent (ET(A) K(i) = 10 pM) and selective (80,000-fold for ET(A) vs ET(B)) antagonist. It is also 150-fold more potent and >6-fold more selective than BMS-193884. The bioavailability of Edonentan was 100% in rats and the systemic clearance and volume of distribution are higher than that of BMS-193884. In rats, intravenous Edonentan blocks big ET pressor responses with 30-fold greater potency than 1. After orally bioavailable dosing at 3 micromol/kg, Edonentan exhibits enhanced duration relative to BMS-193884. References: Chopra A. (11)C-BMS-5p and (18)F-FBzBMS: radiolabeled analogs of BMS-207940, a potent and selective antagonist of endothelin receptor subtype A. 2013 Mar 12 [updated 2013 Jun 27]. Molecular Imaging and Contrast Agent Database (MICAD) [Internet]. Bethesda (MD): National Center for Biotechnology Information (US); 2004-2013. Available from .gov/books/NBK148379/ PubMed PMID: 23833790.

纯度：≥98%

CAS：210891-04-6