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XEN445

Endothelial lipase(EL) inhibitor CAS# 1515856-92-4

XEN445

Catalog No. BCC5382----Order now to get a substantial discount!

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Quality Control of XEN445

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Chemical structure

XEN445

3D structure

Chemical Properties of XEN445

Cas No. 1515856-92-4 SDF Download SDF
PubChem ID 72736173 Appearance Powder
Formula C18H17F3N2O3 M.Wt 366.33
Type of Compound N/A Storage Desiccate at -20°C
Solubility DMSO : ≥ 40 mg/mL (109.19 mM)
*"≥" means soluble, but saturation unknown.
Chemical Name 2-[(3S)-3-(pyridin-2-ylmethoxy)pyrrolidin-1-yl]-5-(trifluoromethyl)benzoic acid
SMILES C1CN(CC1OCC2=CC=CC=N2)C3=C(C=C(C=C3)C(F)(F)F)C(=O)O
Standard InChIKey NBGRERFNOKZQLO-AWEZNQCLSA-N
Standard InChI InChI=1S/C18H17F3N2O3/c19-18(20,21)12-4-5-16(15(9-12)17(24)25)23-8-6-14(10-23)26-11-13-3-1-2-7-22-13/h1-5,7,9,14H,6,8,10-11H2,(H,24,25)/t14-/m0/s1
General tips For obtaining a higher solubility , please warm the tube at 37 ℃ and shake it in the ultrasonic bath for a while.Stock solution can be stored below -20℃ for several months.
We recommend that you prepare and use the solution on the same day. However, if the test schedule requires, the stock solutions can be prepared in advance, and the stock solution must be sealed and stored below -20℃. In general, the stock solution can be kept for several months.
Before use, we recommend that you leave the vial at room temperature for at least an hour before opening it.
About Packaging 1. The packaging of the product may be reversed during transportation, cause the high purity compounds to adhere to the neck or cap of the vial.Take the vail out of its packaging and shake gently until the compounds fall to the bottom of the vial.
2. For liquid products, please centrifuge at 500xg to gather the liquid to the bottom of the vial.
3. Try to avoid loss or contamination during the experiment.
Shipping Condition Packaging according to customer requirements(5mg, 10mg, 20mg and more). Ship via FedEx, DHL, UPS, EMS or other couriers with RT, or blue ice upon request.

Biological Activity of XEN445

DescriptionSelective endothelial lipase (EL) inhibitor (IC50 = 237 nM for human EL). Exhibits >20-fold selectivity for EL over lipoprotein lipase (LPL) and hepatic lipase (HL). Increases high density lipoprotein cholesterol (HDLc) plasma levels in mice. Orally bioavailable.

XEN445 Dilution Calculator

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XEN445 Molarity Calculator

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Preparing Stock Solutions of XEN445

1 mg 5 mg 10 mg 20 mg 25 mg
1 mM 2.7298 mL 13.6489 mL 27.2978 mL 54.5956 mL 68.2445 mL
5 mM 0.546 mL 2.7298 mL 5.4596 mL 10.9191 mL 13.6489 mL
10 mM 0.273 mL 1.3649 mL 2.7298 mL 5.4596 mL 6.8244 mL
50 mM 0.0546 mL 0.273 mL 0.546 mL 1.0919 mL 1.3649 mL
100 mM 0.0273 mL 0.1365 mL 0.273 mL 0.546 mL 0.6824 mL
* Note: If you are in the process of experiment, it's necessary to make the dilution ratios of the samples. The dilution data above is only for reference. Normally, it's can get a better solubility within lower of Concentrations.

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Background on XEN445

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.

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References on XEN445

Discovery of XEN445: a potent and selective endothelial lipase inhibitor raises plasma HDL-cholesterol concentration in mice.[Pubmed:24211162]

Bioorg Med Chem. 2013 Dec 15;21(24):7724-34.

Endothelial lipase (EL) activity has been implicated in HDL metabolism and in atherosclerotic plaque development; inhibitors are proposed to be efficacious in the treatment of dyslipidemia related cardiovascular disease. We describe here the discovery of a novel class of anthranilic acids EL inhibitors. XEN445 (compound 13) was identified as a potent and selective EL inhibitor, that showed good ADME and PK properties, and demonstrated in vivo efficacy in raising plasma HDLc concentrations in mice.

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.

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