Cat. No. 2373
Chemical Name: N-(2,2,2-Trifluoroethyl)-N-[4-[2,2,
Biological ActivityPotent, high affinity liver X receptor (LXR) agonist (EC50 ~ 50 nM, Kd values are 7 and 22 nM for LXR-α and LXR-β respectively). Upregulates expression of the ABCA1 gene associated with cholesterol efflux regulation and HDL metabolism. Decreases amyloid-β production in primary neurons in vitro. Displays an EC50 of ~ 5 μM for activation of bile acid farnesoid X receptors (FXRs); 10-fold more potent than natural FXR ligand chenodeoxycholic acid. Also exhibits inverse agonist activity at constitutive androstane receptors (CAR).
The technical data provided above is for guidance only. For batch specific data refer to the Certificate of Analysis.
All Tocris products are intended for laboratory research use only.
Certificate of Analysis / Product Datasheet / Safety Datasheet
Kanno et al (2013) T0901317, a potent LXR agonist, is an inverse agonist of CAR. J.Toxicol.Sci. 38 309. PMID: 23665929.
Mitro et al (2007) The nuclear receptor LXR is a glucose sensor. Nature Lett. 445 219.
Koldamova et al (2005) The liver X receptor ligand T0901317 decreases amyloid β production in vitro and in a mouse model of Alzheimer's disease. J.Biol.Chem. 280 4079. PMID: 15557325.
Houck et al (2004) T0901317 is a dual LXR/FXR agonist. Mol.Gen.Metab. 83 184.
Repa et al (2000) Regulation of absorption and ABC1-mediated efflux of cholesterol by RXR heterodimers. Science 289 1524. PMID: 10968783.
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Citations are publications that use Tocris products. Selected citations for T 0901317 include:
Kim et al (2016) The transcription cofactor CRTC1 protects from aberrant hepatic lipid accumulation Scientific Reports 6 37280. PMID: 27869139.
Singh et al (2016) The fatty acid synthase inhibitor platensimycin improves insulin resistance without inducing liver steatosisin mice and monkeys PLoS One 11 e0164133. PMID: 27695056.
Candelaria et al (2014) Antiproliferative effects and mechanisms of liver X receptor ligands in pancreatic ductal adenocarcinoma cells. J Biomol Screen 9 e106289. PMID: 25184494.
Wahlang et al (2014) Human receptor activation by aroclor 1260, a polychlorinated biphenyl mixture. Toxicol Sci 140 283. PMID: 24812009.
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Keywords: T 0901317, supplier, Potent, liver, X, receptor, LXR, agonists, FXR, Receptors, Liver, Farnesoid, LXR-like, T0901317, Tocris Bioscience, LXR-like Receptor Agonist products