Lp-PLA2-IN-3

• CAT Number: I017344
• CAS Number: 2196245-16-4
• Molecular Formula: C20H13ClF3N3O3S
• Molecular Weight: 467.85
• Purity: ≥95%
• Synonyms: 4-amino-N-[4-[4-chloro-3-(trifluoromethyl)phenoxy]-3-cyanophenyl]benzenesulfonamide
• InChI: InChI=1S/C20H13ClF3N3O3S/c21-18-7-4-15(10-17(18)20(22,23)24)30-19-8-3-14(9-12(19)11-25)27-31(28,29)16-5-1-13(26)2-6-16/h1-10,27H,26H2
• InChIKey: GADGQEKPNKSGMT-UHFFFAOYSA-N
• SMILES: C1=CC(=CC=C1N)S(=O)(=O)NC2=CC(=C(C=C2)OC3=CC(=C(C=C3)Cl)C(F)(F)F)C#N

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].
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].

Reference

[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.
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