Lp-PLA2-IN-3

Research use only, not for human use.

Lp-PLA2-IN-3 is a potent, orally bioactive lipoprotein-associated phospholipase A2 (Lp-PLA2) inhibitor, effectively inhibiting recombinant human [Lp-PLA2] with an IC50 value of 14 nM.

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).

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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.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.Animal Model:Male Sprague?Dawley (SD) rats (180-220 g)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.

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Metabolic Enzyme/Protease

Phospholipase

Phospholipase

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2196245-16-4

467.85

C20H13ClF3N3O3S

>98% (HPLC)

In Vitro:?DMSO : ≥ 250 mg/mL (534.36 mM )

Nc1ccc(cc1)S(=O)(=O)Nc1ccc(Oc2ccc(Cl)c(c2)C(F)(F)F)c(c1)C#N

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(-20℃)

With Ice Pack

≥ 2 years