XEN445

Modify Date: 2024-01-15 20:24:41

XEN445 Structure
XEN445 structure
Common Name XEN445
CAS Number 1515856-92-4 Molecular Weight 366.334
Density 1.4±0.1 g/cm3 Boiling Point 490.9±45.0 °C at 760 mmHg
Molecular Formula C18H17F3N2O3 Melting Point N/A
MSDS N/A Flash Point 250.7±28.7 °C

 Use of XEN445


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.

 Names

Name 2-[(3S)-3-(2-Pyridinylmethoxy)-1-pyrrolidinyl]-5-(trifluoromethyl)benzoic acid
Synonym More Synonyms

 XEN445 Biological Activity

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
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.

 Chemical & Physical Properties

Density 1.4±0.1 g/cm3
Boiling Point 490.9±45.0 °C at 760 mmHg
Molecular Formula C18H17F3N2O3
Molecular Weight 366.334
Flash Point 250.7±28.7 °C
Exact Mass 366.119141
LogP 3.30
Vapour Pressure 0.0±1.3 mmHg at 25°C
Index of Refraction 1.583
Storage condition -20℃

 Safety Information

RIDADR NONH for all modes of transport

 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
Top Suppliers:I want be here
  • DC Chemicals Limited
  • China
  • Product Name: XEN445
  • Price: $400.0/100mg $750.0/250mg $1500.0/1g
  • Purity: 98.0%
  • Stocking Period: 3 Day
  • Contact: Tony Cao

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XEN445 suppliers


Price: $136/10mM*1mLinDMSO

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