For research use only. Not for therapeutic Use.
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].
| Catalog Number | I017344 |
| CAS Number | 2196245-16-4 |
| Synonyms | 4-amino-N-[4-[4-chloro-3-(trifluoromethyl)phenoxy]-3-cyanophenyl]benzenesulfonamide |
| Molecular Formula | C20H13ClF3N3O3S |
| Purity | ≥95% |
| 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 |
| 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. |
