Size | Price | Stock |
---|---|---|
1mg | $33 | In-stock |
5mg | $70 | In-stock |
10mg | $130 | In-stock |
50mg | $450 | In-stock |
100mg | $700 | In-stock |
200 mg | Get quote | |
500 mg | Get quote | |
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Cat. No. : | HY-12246 |
M.Wt: | 366.33 |
Formula: | C18H17F3N2O3 |
Purity: | >98 % |
Solubility: | DMSO : ≥ 40 mg/mL (109.19 mM) |
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.
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