A 74273

A 74273 is a nonpeptidic and renin inhibitor. It may be used to treat cardiovascular diseases due to renin inhibition.

A-74273 is an orally active peptide renin inhibitor (IC50=3.1 nM). A-74273 competitively binds to the active site of renin, preventing angiotensinogen from being converted to ANG-I, thereby reducing the level of angiotensin II. A-74273 can be used in the study of diseases such as hypertension[1][2].

[1] Dayton, et al. Effects of angiotensinase inhibitors on plasma protein binding and IC50 determinations of renin inhibitors. Clinical chemistry 38.11 (1992): 2239-2243. PMID:1330373
[2] Kleinert, et al. "Discovery of a well-absorbed, efficacious renin inhibitor, A-74273." Hypertension 20.6 (1992): 768-775. DOI:10.1161/01.hyp.20.6.768