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XEN445

Catalog No.
B4663
Endothelial lipase(EL) inhibitor
Grouped product items
SizePriceStock Qty
5mg
$70.00
In stock
10mg
$130.00
In stock
50mg
$470.00
In stock
100mg
$700.00
Ship with 10-15 days

Tel: +1-832-696-8203

Email: [email protected]

Worldwide Distributors

Background

XEN445 is a novel, highly selective and potent inhibitor of endothelial lipase(EL) with an IC 50 value of 0.237μM [1].

In vitro, XEN445 has been reported to selectively inhibit EL with IC50 values of 0.237μM, 20μM and 9.5μM for hEL, hLPL and hHL, respectively. In addition, XEN445 has been revealed to suppress EL in EL-transfected HEK cells with an IC50 value of 0.25μM which is very similar to that tested in cell-free assay. Besides, XEN445 has shown significantly high oral bioavailability and low clearance rates in C57BL6 mice. In vivo, XEN445 has been evidenced to increase plasma HDLc in wild-type mice. Moreover, XEN445 has exhibited the HDL-raising effect because of on-target inhibition by using the EL knockout mice [1].

References:
[1] Sun S1, Dean R, Jia Q, Zenova A, Zhong J, Grayson C, Xie C, Lindgren A, Samra P, Sojo L, van Heek M, Lin L, Percival D, Fu JM, Winther MD, Zhang Z. 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 Properties

Physical AppearanceA crystalline solid
StorageStore at -20°C
M.Wt366.33
Cas No.1515856-92-4
FormulaC18H17F3N2O3
SolubilitySoluble in DMSO
Chemical Name(S)-2-(3-(pyridin-2-ylmethoxy)pyrrolidin-1-yl)-5-(trifluoromethyl)benzoic acid
SDFDownload SDF
Canonical SMILESFC(F)(F)C1=CC(C(O)=O)=C(N2CC[[email protected]@](OCC3=CC=CC=N3)([H])C2)C=C1
Shipping ConditionEvaluation sample solution: ship with blue ice. All other available sizes: ship with RT, or blue ice upon request.
General tipsFor obtaining a higher solubility, please warm the tube at 37°C and shake it in the ultrasonic bath for a while. Stock solution can be stored below -20°C for several months.

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