For research use only. Not for therapeutic Use.
XEN445(CAT: I001880) stands as a potent and selective inhibitor of endothelial lipase (EL). It has demonstrated favorable absorption, distribution, metabolism, and excretion (ADME) properties, along with pharmacokinetic (PK) attributes. In vivo, efficacy was observed in mice, where XEN445 effectively elevated plasma high-density lipoprotein cholesterol (HDLc) concentrations. This compound targets endothelial lipase, suggesting its potential in influencing lipid metabolism and cardiovascular health. XEN445’s synthesis involves readily available commercial chemicals, contributing to its accessibility for further evaluation.
| Catalog Number | I001880 |
| CAS Number | 1515856-92-4 |
| Synonyms | 2-[(3S)-3-(2-pyridinylmethoxy)-1-pyrrolidinyl]-5-(trifluoromethyl)-benzoic acid |
| Molecular Formula | C₁₈H₁₇F₃N₂O₃ |
| Purity | ≥95% |
| Target | Endothelial lipase inhibitor |
| Solubility | DMSO: ≥ 40 mg/mL |
| Storage | -20°C |
| IC50 | 0.237 uM [1] |
| 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 |
| InChIKey | NBGRERFNOKZQLO-AWEZNQCLSA-N |
| SMILES | O=C(O)C1=CC(C(F)(F)F)=CC=C1N2C[[email protected]@H](OCC3=NC=CC=C3)CC2 |
| Reference | 1:Bioorg Med Chem. 2013 Dec 15;21(24):7724-34. doi: 10.1016/j.bmc.2013.10.023. Epub 2013 Oct 28. Discovery of XEN445: a potent and selective endothelial lipase inhibitor raises plasma HDL-cholesterol concentration in mice.Sun S,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, PMID: 24211162 DOI: 10.1016/j.bmc.2013.10.023 </br><span>Abstract:</span> 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. Copyright © 2013 Elsevier Ltd. All rights reserved. |
