Lp-PLA2-IN-3

Lp-PLA2-IN-3 is a potent and orally bioavailable lipoprotein-associated phospholipase A2 (Lp-PLA2) inhibitor, with an IC50 of 14 nM for recombinant human Lp-PLA2 (rhLpPLA2)[1].

Research Areas >> Cardiovascular Disease

Signaling Pathways >> Metabolic Enzyme/Protease >> Phospholipase

Lp-PLA2-IN-3 (3 mg/kg; p.o.) treatment shows the Cmax, AUC0-24h, t1/2 and F were 0.27 μg/mL, 3.4 μg h/mL, 7.7 hours and 35.5%, respectively[1]. Lp-PLA2-IN-3 (1 mg/kg; i.v.) treatment shows the CL, Vss, and t1/2 were 3.1mL/min/kg, 0.3 L/kg, 4 hours, respectively[1]. Animal Model: Male Sprague−Dawley (SD) rats (180-220 g)[1] Dosage: 3 mg/kg Administration: p.o. (Pharmacokinetic Analysis) Result: The Cmax, AUC0-24h, t1/2 and F were 0.27 μg/mL, 6.2 μg h/mL, 7.7 hours and 35.5%, respectively.

[1]. Liu Q, et al. Structure-Guided Discovery of Novel, Potent, and Orally Bioavailable Inhibitors of Lipoprotein-Associated Phospholipase A2. J Med Chem. 2017 Dec 28;60(24):10231-10244.