XEN445Endothelial lipase(EL) inhibitor CAS# 1515856-92-4 |
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Quality Control & MSDS
Number of papers citing our products
Chemical structure
3D structure
| 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. |
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| 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. |
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| 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. | ||
| Description | Selective 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
XEN445 Molarity Calculator
| 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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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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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.
