PF-04457845 (Redafamdastat) is a highly potent, selective and covalent fatty acid amide hydrolase (FAAH) inhibitor with IC50 of 7.2 nM (human FAAH).
PF-04457845 displays no activity against other FP-reactive serine hydrolases at 100 uM, as well as a broad panel of 68 targets including receptors, enzymes, ion channels, and transporters.
PF-04457845 is orally bioavailable, and PF-04457845 (10 mg/kg, p.o.) displays antihyperalgesic activity with long duration of action in the CFA model of inflammatory pain in rats.
PF-04457845 does not elicit effect in motility, catalepsy, and body temperature.
