Small-molecule inhibitor: NK3201

Name

History: NK3201 was described as an inhibitor of chymase by Takai et al. (2001).
Peptidases inhibited: NK3201 inhibited human, dog and hamster forms of chymase with IC₅₀ values of 2.5, 1.2 and 28 nM, respectively (Takai et al., 2001).
Mechanism: Inhibition is presumably reversible.
Pharmaceutical relevance: NK3201 was initially shown to reduce the proliferation of damaged blood vessels in animal experiments, possibly acting primarily by decreasing the formation of angiotensin II by chymase, since an antagonist of the angiotensin II receptor had similar activity (Takai et al., 2001). NK3201 is orally bioavailable. Subsequently, it has been shown to have therapeutic value in a variety of models of cardivascular pathology (see Literature).

CID at PubChem: 213050
Structure
Chemical/biochemical name: N-(3,4-dioxo-1-phenyl-7-pyridin-2-yloxy-heptan-2-yl)-2-(5-formamido-6-oxo-2-phenyl-pyrimidin-1-yl)acetamide
Formula weight: 567