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 (8)
Reviews
Literature (2)

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.

Tocris products are intended for laboratory research use only, unless stated otherwise.

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 the degree of hydration, which will affect the solvent volumes required to prepare stock solutions.

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

Certificate of Analysis / Product Datasheet
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References

References are publications that support the biological activity of the product.

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

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

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: T 0901317, T 0901317 supplier, Potent, liver, X, receptor, LXR, agonists, FXR, Receptors, Liver, Farnesoid, LXR-like, T0901317, Constitutive, Androstane, Receptor, 2373, Tocris Bioscience

8 Citations for T 0901317

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

Kasmi (2018) Macrophage-derived IL-1β/NF-κB signaling mediates parenteral nutrition-associated cholestasis. Nat Commun 9 1393 PMID: 29643332

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

Herold (2017) Liver X receptor activation promotes differentiation of regulatory T cells. PLoS One 12 e0184985 PMID: 28926619

Bonney (2017) Differential Effects of Retinoic Acid Concentrations in Regulating Blood-Brain Barrier Properties. Eneuro 4 PMID: 28560318


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