XEN445 Chemical Properties

Boiling point:

490.9±45.0 °C(Predicted)

Density 

1.40±0.1 g/cm3(Predicted)

storage temp. 

under inert gas (nitrogen or Argon) at 2-8°C

solubility 

DMF: 30 mg/ml; DMF:PBS (pH 7.2) (1:1): 0.5 mg/ml; DMSO: 25 mg/ml; Ethanol: 14 mg/ml

form 

A crystalline solid

pka

3.35±0.36(Predicted)

XEN445 Usage And Synthesis

Description

Endothelial lipase, a member of the triglyceride lipase gene family expressed in endothelial cells, prefers phospholipid-enriched high-density lipoprotein (HDL) over triglyceride as a substrate. XEN445 is an endothelial lipase inhibitor (IC₅₀ = 237 nM) that demonstrates selectivity for endothelial lipase compared to lipoprotein and hepatic lipases (IC₅₀s = 20 and 9.5 μM, respectivley). An oral dose of 30 mg/kg XEN445 is reported to increase HDL cholesterol concentrations by 16% after three days and by 30% after nine days dosing in wild-type mice.

Uses

XEN445 is a potent and selective endothelial lipase inhibitor.

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