KH064

KH064 is an orally active small molecule and a potent, selective inhibitor of secretory phospholipase A2 group IIA (sPLA2-IIA), with an IC50 of 29 nM for the human nonpancreatic isoform. It is a D-tyrosine derivative that binds in the active site of sPLA2-IIA and inhibits its enzymatic activity. In preclinical studies, KH064 has demonstrated anti-inflammatory effects and has been shown to attenuate adiposity and metabolic dysfunction in diet-induced obese rats by promoting lipolysis and reducing fat deposition. The compound also reduces inflammation markers such as PGE2 concentrations and macrophage infiltration in adipose tissue[1][3][4][5][7].

Other names

(S)-5-(4-Benzyloxy-phenyl)-4-(7-phenyl-heptanoylamino)-pentanoic acid5-(4-Benzyloxyphenyl)-4S-(7-phenylheptanoylamino)pentanoic acid(4S)-4-(7-phenylheptanoylamino)-5-[4-(phenylmethoxy)phenyl]pentanoic acid