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LXR 623
- WAY 252623
- Soluble in DMSO
- MF: C21H12ClF5N2
- MW: 422.78
Description
Partial agonist of Liver X Receptor (LXR; IC50 value 179 nM and 24 nM for LXRα- and LXRβ-binding, respectively. EC50 values 6.66 μM and 3.67 μM for Huh-7 human hepatoma cell based Gal4 LXRα and LXRβ transactivation essays respectively). Despite its partial agonism in transactivation essays, LXR 623 exhibits full agonism in THP-1 cells with respect to increasing ABCA1 gene expression and on cholesterol efflux in THP-1 foam cells. In vivo, LXR 623 lowers LDL cholesterol in primates, is lipid neutral in hamster, and reduces atherosclerosis in mouse.
More Information
| Parent CAS No. | 875787-07-8 |
|---|---|
| Chemical Name | 2-(2-chloro-4-fluorobenzyl)-3-(4-fluorophenyl)-7-(trifluoromethyl)-2H-indazole |
| SMILES | C12=C(C3C=CC(F)=CC=3)N(CC3C=CC(F)=CC=3Cl)N=C1C(C(F)(F)F)=CC=C2 |
| MFCD | MFCD16495812 |
| InChi | InChI=1S/C21H12ClF5N2/c22-18-10-15(24)9-6-13(18)11-29-20(12-4-7-14(23)8-5-12)16-2-1-3-17(19(16)28-29)21(25,26)27/h1-10H,11H2 |
| InChiKey | KYWWJENKIMRJBI-UHFFFAOYSA-N |
| CID | 16734800 |
| Short Description | LXR partial agonist |
References
- C. Giannarelli et al. Synergistic effect of liver X receptor activation and simvastatin on plaque regression and stabilization: an magnetic resonance imaging study in a model of advanced atherosclerosis. Eur. Heart J. 2012, 33, 264-273.
- J. Wrobel et al. Indazole-based liver X receptor (LXR) modulators with maintained atherosclerotic lesion reduction activity but diminished stimulation of hepatic triglyceride synthesis. J. Med. Chem. 2008, 51, 7161-7168.
- E.M. Quinet et al. LXR ligand lowers LDL cholesterol in primates, is lipid neutral in hamster, and reduces atherosclerosis in mouse. J. Lipid Res. 2009, 50, 2358-2370.
- E.A. DiBlasio-Smith et al. Discovery and implementation of transcriptional biomarkers of synthetic LXR agonists in peripheral blood cells. J. Transl. Med. 2008, 6, 59.
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