XEN445 [1515856-92-4]

MedChem Express

XEN445 [1515856-92-4]

10

1515856-92-4

Research Use Only

99.85

C18H17F3N2O3

366.33

XEN445 is a potent and selective EL inhibitor(IC50=0.237 uM), that showed good ADME and PK properties, and demonstrated in vivo efficacy in raising plasma HDLc concentrations in mice. IC50 value: 0.237 uM [1] Target: Endothelial lipase inhibitor XEN445 can be readily prepared in good yield from commercial available chemicals, which was selected for further evaluation of this series of EL inhibitors. After a 30 min preincubation of EL-expressing HEK cells with XEN445, the IC50 value for XEN445 of 0.25 lM was obtained. This value was very similar to that determined in the cell-free assay. Wild-type mice were orally dosed with XEN445 at 30 mg/kg b.i.d. for 3 days and blood was taken on the morning of day 4, 16 h post final dose. At termination, the average plasma levels of XEN445 was 9.9 lM and the drug caused an 18% and 16% increase in total plasma cholesterol and HDLc, respectively.

O=C(O)C1=CC(C(F)(F)F)=CC=C1N2C[C@@H](OCC3=NC=CC=C3)CC2

-20°C,2°C to 8°C

12352200