FIPI HCl

Description: FIPI HCl, the hydrochloride salt of FIPI which is formerly known as 5-Fluoro-2-indolyl deschlorohalopemide, is a derivative of halopemide which potently and selectively inhibits both PLD1 (phospholipase D) and PLD2 with IC50 values of 25 nM and 20 nM, respectively. FIPI is able to attenuate mercury-induced lipid signaling resulting in protection against cytotoxicity in aortic endothelial cells. FIPI rapidly blocks in vivo PA production with low nanomolar potency. FIPI has favorable pharmacokinetics with a half-life of greater than 5 hours, a Cmax of greater than 10-fold the 50 versus PLD2, and moderate bioavailability of 18%. FIPI inhibits both PLD1 and PLD2 in a dose-dependent manner with 50% loss of activity observed at approximately 25 nM.

References: Bioorg Med Chem Lett. 2007 Apr 15; 17(8):2310-1.Mol Pharmacol. 2009 Mar; 75(3):437-46.

Related CAS#:939055-18-2 (free base)