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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)
Biological Activity for T 0901317
T 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).
Compound Libraries for T 0901317
T 0901317 is also offered as part of the Tocriscreen 2.0 Max. Find out more about compound libraries available from Tocris.
Technical Data for T 0901317
| 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 for T 0901317
| Solvent | Max Conc. mg/mL | Max Conc. mM | |
|---|---|---|---|
| Solubility | |||
| DMSO | 48.13 | 100 | |
| ethanol | 48.13 | 100 |
Preparing Stock Solutions for T 0901317
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 for T 0901317
References for T 0901317
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
If you know of a relevant reference for T 0901317, please let us know.
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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:
Singh et al (2016) The fatty acid synthase inhibitor platensimycin improves Ins 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
Bonney (2017) Differential Effects of Retinoic Acid Concentrations in Regulating Blood-Brain Barrier Properties. Eneuro 4 PMID: 28560318
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
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
Kasmi (2018) Macrophage-derived IL-1β/NF-κB signaling mediates parenteral nutrition-associated cholestasis. Nat Commun 9 1393 PMID: 29643332
Do you know of a great paper that uses T 0901317 from Tocris? Please let us know.
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