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Bioorg Med Chem Lett. 1998 Aug 18;8(16):2241-6.

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

Author information

1
Takarazuka Research Institute, Novartis Pharma K.K., Japan.

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.

PMID:
9873521
DOI:
10.1016/s0960-894x(98)00387-4
[Indexed for MEDLINE]

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