1515856-92-4

1515856-92-4 structure

Name: XEN445
Chemical Name: 2-[(3S)-3-(2-Pyridinylmethoxy)-1-pyrrolidinyl]-5-(trifluoromethyl)benzoic acid
CAS Number: 1515856-92-4
Molecular Formula: C₁₈H₁₇F₃N₂O₃
Molecular Weight: 366.334
Catalog: Research Areas Cardiovascular Disease
Create Date: 2018-05-11 22:09:30
Modify Date: 2024-01-15 20:24:41
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 inhibitorXEN445 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.

Name	2-[(3S)-3-(2-Pyridinylmethoxy)-1-pyrrolidinyl]-5-(trifluoromethyl)benzoic acid
Synonyms	Benzoic acid, 2-[(3S)-3-(2-pyridinylmethoxy)-1-pyrrolidinyl]-5-(trifluoromethyl)- 2-[(3S)-3-(2-Pyridinylmethoxy)-1-pyrrolidinyl]-5-(trifluoromethyl)benzoic acid (S)-2-(3-(PYRIDIN-2-YLMETHOXY)PYRROLIDIN-1-YL)-5-(TRIFLUOROMETHYL)BENZOIC ACID. HCL XEN-445 XEN445

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.IC50 value: 0.237 uM [1]Target: Endothelial lipase inhibitorXEN445 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.
Related Catalog	Signaling Pathways >> Others >> Others Research Areas >> Cardiovascular Disease
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.

RIDADR	NONH for all modes of transport