T 0901317

Biological Activity

T 0901317 is a potent, high affinity liver X receptor (LXR) agonist (EC₅₀ ~ 50 nM, K_d 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).

Technical Data

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.

Background References

1. The transcription cofactor CRTC1 protects from aberrant hepatic lipid accumulation
   
   Sci Rep, 2016;6(0):37280.
2. RAGE Suppresses ABCG1-Mediated Macrophage Cholesterol Efflux in Diabetes.
   Daffu G, Shen X, Senatus L, Thiagarajan D, Abedini A, Hurtado Del Pozo C, Rosario R, Song F, Friedman R, Ramasamy R, Schmidt A
   Diabetes, 2015;64(12):4046-60.
3. T0901317, a potent LXR agonist, is an inverse agonist of CAR.
   Kanno et al.
   J.Toxicol.Sci., 2013;38:309
4. Regulation of absorption and ABC1-mediated efflux of cholesterol by RXR heterodimers.
   Repa et al.
   Science, 2000;289:1524
5. The liver X receptor ligand T0901317 decreases amyloid β production in vitro and in a mouse model of Alzheimer's disease.
   Koldamova et al.
   J.Biol.Chem., 2005;280:4079
6. T0901317 is a dual LXR/FXR agonist.
   Houck et al.
   Mol.Gen.Metab., 2004;83:184
7. The nuclear receptor LXR is a glucose sensor.
   Mitro et al.
   Nature Lett., 2007;445:219

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