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ID: ALA1131547

Journal: Bioorg Med Chem Lett

Title: Discovery of IRL 3461: a novel and potent endothelin antagonist with balanced ETA/ETB affinity.

Authors: Sakaki J, Murata T, Yuumoto Y, Nakamura I, Trueh T, Pitterna T, Iwasaki G, Oda K, Yamamura T, Hayakawa K.

Abstract: IRL 3461, N-butanesulfonyl-[N-(3,5-dimethylbenzoyl)-N-methyl-3-[4-(5-+ ++isoxazolyl) -phenyl]-alanyl]-(L)-valineamide, a potent and bifunctional (ETA + ETB) [Ki(ETA) = 1.8 nM, Ki(ETB) = 1.2 nM] antagonist was discovered by structural modification of IRL 2500, an ETB selective antagonist. IRL 3461 was found to be stable on incubation with human, rat, mouse, and guinea pig plasmas.

CiteXplore: 9873521

DOI: 10.1016/s0960-894x(98)00387-4