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| Cas No.: | 1515856-92-4 |
| Synonyms: | XEN 445; XEN-445 |
| SMILES: | C(O)(=O)C1=CC(C(F)(F)F)=CC=C1N1CC[C@@H](OCC2=NC=CC=C2)C1 |
| Formula: | C18H17F3N2O3 |
| M.Wt: | 366.33 |
| Purity: | >98% |
| Sotrage: | 2 years -20°C Powder, 2 weeks 4°C in DMSO, 6 months -80°C in DMSO |
| Description: | 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.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. |
| Target: | IC50 value: 0.237 uM [1] Target: Endothelial lipase inhibitor |
| References: | [1]. Sun S, et al. Discovery of XEN445: a potent and selective endothelial lipase inhibitor raises plasma HDL-cholesterol concentration in mice. Bioorg Med Chem. 2013 Dec 15;21(24):7724-34. |
MSDS
COA
| LOT NO. | DOWNLOAD |
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| 2018-0101 |
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| 2018-0101 |
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