Description
InformationML355 ML355 is a potent and selective inhibitor of human 12-Lipoxygenase with an IC50 of 290 nM and shows excellent selectivity over related lipoxygenases and cyclooxygenases.Targets12-LOXIn vitroML355 displays nM potency against 12-LOX and excellent selectivity over related lipoxygenases and cyclooxygenases.In vivoIn vivo PK studies where ML355 is administered as a solution via IV (3mpk) and PO (30mpk) demonstrated that ML355 is orally bioavailable (%F = 20) with good half-life (T1/2 = 2.9 hours). At 30 mpk dosing, ML355 achieves a Cmax of over 135 times the in vitro IC50 and remains over IC50 value for over 12 hours. The compound has low clearance (3.4 mL/min/kg) and good overall exposure (AUCinf) of 38 µM. Although, the volume of distribution (VD) observed is low (0.55 L/kg), the rest of the PK profiling results suggest a reasonable distribution between tissue and blood