Chemical Name: N-(2,2,2-Trifluoroethyl)-N-[4-[2,2,2-trifluoro-1-hydroxy-1-(trifluoromethyl)ethyl]phenyl]benzenesulfonamide
Biological ActivityT 0901317 is a potent, 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.
Tocris products are intended for laboratory research use only, unless stated otherwise.
T0901317, a potent LXR agonist, is an inverse agonist of CAR.
Kanno et al.
Regulation of absorption and ABC1-mediated efflux of cholesterol by RXR heterodimers.
Repa et al.
The liver X receptor ligand T0901317 decreases amyloid β production in vitro and in a mouse model of Alzheimer's disease.
Koldamova et al.
T0901317 is a dual LXR/FXR agonist.
Houck et al.
The nuclear receptor LXR is a glucose sensor.
Mitro et al.
Nature Lett., 2007;445:219
Citations for T 0901317
The citations listed below are publications that use Tocris products. Selected citations for T 0901317 include:
8 Citations: Showing 1 - 8
Macrophage-derived IL-1β/NF-κB signaling mediates parenteral nutrition-associated cholestasis.
Nat Commun 2018;9(1):1393
Differential Effects of Retinoic Acid Concentrations in Regulating Blood-Brain Barrier Properties.
Liver X receptor activation promotes differentiation of regulatory T cells.
PLoS One 2017;12(9):e0184985
Liver X receptors activation, through TO901317 binding, reduces neuroinflammation in Parkinson's disease.
PLoS One 2017;12(4):e0174470
The transcription cofactor CRTC1 protects from aberrant hepatic lipid accumulation
Authors: Kim Et al.
Scientific Reports 2016;6:37280
The fatty acid synthase inhibitor platensimycin improves Ins resistance without inducing liver steatosisin mice and monkeys
Authors: Singh Et al.
PLoS One 2016;11:e0164133
Antiproliferative effects and mechanisms of liver X receptor ligands in pancreatic ductal adenocarcinoma cells.
Authors: Candelaria Et al.
J Biomol Screen 2014;9:e106289
Human receptor activation by aroclor 1260, a polychlorinated biphenyl mixture.
Authors: Wahlang Et al.
Toxicol Sci 2014;140:283
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