apstatin

Apstatin is a potent and selective small molecule inhibitor of aminopeptidase P (APP), with Ki values of approximately 0.64 µM for human APP and 2.6 µM for rat APP[9][1]. It blocks the degradation of bradykinin by inhibiting membrane-bound aminopeptidase P, thereby exerting a bradykinin-sparing effect[5][7]. In preclinical models, apstatin has demonstrated cardioprotective effects by reducing myocardial infarct size in acute ischemia/reperfusion injury through a kinin-dependent pathway[4][7]. It can also potentiate the vasodilatory effect of bradykinin and reduce blood pressure in animal models of hypertension[7][8]. Apstatin is primarily used as an experimental tool compound in research settings; it is not approved for clinical use.

Other names

N-[(2S,3R)-3-amino-2-hydroxy-4-phenylbutanoyl]-L-prolyl-L-prolyl-L-alaninamide(2S)-1-[(2S)-1-[(2S,3R)-3-amino-2-hydroxy-4-phenylbutanoyl]pyrrolidine-2-carbonyl]-N-[(2S)-1-amino-1-oxopropan-2-yl]pyrrolidine-2-carboxamide