169547-22-2Relevant articles and documents
Discovery of IRL 3461: A novel and potent endothelin antagonist with balanced ET(A)/ET(B) affinity
Sakaki, Junichi,Murata, Toshiki,Yuumoto, Yoko,Nakamura, Ikushi,Frueh, Thomas,Pitterna, Thomas,Iwasaki, Genji,Oda, Kyoko,Yamamura, Takaki,Hayakawa, Kenji
, p. 2241 - 2246 (2007/10/03)
IRL 3461, N-butanesulfonyl-[N-(3,5-dimethylbenzoyl)-N-methyl-3-[4-(5- isoxazolyl)-phenyl]-alanyl]-(L)-valineamide, a potent and bifunctional (ET(A) + ET(B)) [Ki(ET(A))=1.8 nM, Ki(ET(B))=1.2 nM] antagonist was discovered by structural modification of IRL 2500, an ET(B) selective antagonist. IRL 3461 was found to be stable on incubation with human, rat, mouse, and guinea pig plasmas.