Description
PF-622 (898235-65-9) is a potent and selective irreversible FAAH inhibitor. Covalently modifies active site-serine (IC50=33 nM). Completely selective for FAAH relative to other mammalian serine hydrolases. Cell permeable
in vitro
pf-622 inhibited the activity of faah in a time-dependent manner with the ic50 values of 0.99 and 0.033 μm in human recombinant faah for 5 and 60 minutes, respectively [1]. in various human and murine tissue proteome samples, pf-622 showed highly selectivity for faah in relative to other serine hydrolases, showing no discernable off-site activity up to 500 μm [1]. pf-622 at 1 μm decreased il-2 production in both healthy subjects and in hcv patients [2].
References
1) Ahn et al. (2007), Novel mechanistic class of fatty acid amide hydrolase inhibitors with remarkable selectivity; Biochemistry, 46 13019