T 0901317

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Cat.No. 2373 - T 0901317 | C17H12F9NO3S | CAS No. 293754-55-9
Description: Potent liver X receptor (LXR) agonist; also CAR inverse agonist
Chemical Name: N-(2,2,2-Trifluoroethyl)-N-[4-[2,2,2-trifluoro-1-hydroxy-1-(trifluoromethyl)ethyl]phenyl]benzenesulfonamide
Purity: ≥98% (HPLC)
Datasheet
Citations (5)
Literature

Biological Activity

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).

Compound Libraries

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Technical Data

M. Wt 481.33
Formula C17H12F9NO3S
Storage Store at +4°C
Purity ≥98% (HPLC)
CAS Number 293754-55-9
PubChem ID 447912
InChI Key SGIWFELWJPNFDH-UHFFFAOYSA-N
Smiles OC(C1=CC=C(C=C1)N(CC(F)(F)F)S(=O)(=O)C1=CC=CC=C1)(C(F)(F)F)C(F)(F)F

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.

Solubility Data

Solvent Max Conc. mg/mL Max Conc. mM
Solubility
DMSO 48.13 100
ethanol 48.13 100

Preparing Stock Solutions

The following data is based on the product molecular weight 481.33. Batch specific molecular weights may vary from batch to batch due to solvent of hydration, which will affect the solvent volumes required to prepare stock solutions.

Select a batch to recalculate based on the batch molecular weight:
Concentration / Solvent Volume / Mass 1 mg 5 mg 10 mg
1 mM 2.08 mL 10.39 mL 20.78 mL
5 mM 0.42 mL 2.08 mL 4.16 mL
10 mM 0.21 mL 1.04 mL 2.08 mL
50 mM 0.04 mL 0.21 mL 0.42 mL

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Product Datasheets

Safety Datasheet

References

References are publications that support the products' biological activity.

Repa et al (2000) Regulation of absorption and ABC1-mediated efflux of cholesterol by RXR heterodimers. Science 289 1524 PMID: 10968783

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 PMID:

Mitro et al (2007) The nuclear receptor LXR is a glucose sensor. Nature Lett. 445 219 PMID:

Kanno et al (2013) T0901317, a potent LXR agonist, is an inverse agonist of CAR. J.Toxicol.Sci. 38 309 PMID: 23665929


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Keywords: Potent liver X receptor LXR agonists FXR Receptors Liver Farnesoid LXR-like T0901317 LXR-like Receptors

5 Citations for T 0901317

Citations are publications that use Tocris products. Selected citations for T 0901317 include:

Paterniti (2017) Liver X receptors activation, through TO901317 binding, reduces neuroinflammation in Parkinson's disease. PLoS One 12 e0174470 PMID: 28369131

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

Kim et al (2016) The transcription cofactor CRTC1 protects from aberrant hepatic lipid accumulation Scientific Reports 6 37280 PMID: 27869139

Wahlang et al (2014) Human receptor activation by aroclor 1260, a polychlorinated biphenyl mixture. Toxicol Sci 140 283 PMID: 24812009

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


Do you know of a great paper that uses T 0901317 from Tocris? If so please let us know.

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