T0901317

T0901317 is an orally active and highly selective LXR agonist with an EC50 of 20 nM for LXRα. T0901317 activates FXR with an EC50 of 5 μM. T0901317 is RORα and RORγ dual inverse agonist with Ki values of 132 nM and 51 nM, respectively. T0901317 induces apoptosis and inhibits the development of atherosclerosis in low-density lipoprotein (LDL) receptor-deficient mice.

Product information

CAS Number: 293754-55-9

Molecular Weight: 481.33

Formula: C17H12F9NO3S

Chemical Name: N-[4-(1, 1, 1, 3, 3, 3-hexafluoro-2-hydroxypropan-2-yl)phenyl]-N-(2, 2, 2-trifluoroethyl)benzenesulfonamide

Smiles: OC(C1C=CC(=CC=1)N(CC(F)(F)F)S(=O)(=O)C1C=CC=CC=1)(C(F)(F)F)C(F)(F)F

InChiKey: SGIWFELWJPNFDH-UHFFFAOYSA-N

InChi: InChI=1S/C17H12F9NO3S/c18-14(19,20)10-27(31(29,30)13-4-2-1-3-5-13)12-8-6-11(7-9-12)15(28,16(21,22)23)17(24,25)26/h1-9,28H,10H2

Technical Data

Appearance: Solid Power

Purity: ≥98% (or refer to the Certificate of Analysis)

Solubility: DMSO : 100 mg/mL (207.76 mM; Need ultrasonic)

Shipping Condition: Shipped under ambient temperature as non-hazardous chemical or refer to Certificate of Analysis

Storage Condition: Dry, dark and -20 ^oC for 1 year or refer to the Certificate of Analysis.

Shelf Life: ≥360 days if stored properly.

Stock Solution Storage: 0 - 4 ^oC for 1 month or refer to the Certificate of Analysis.

Drug Formulation: To be determined

HS Tariff Code: 382200

How to use

In Vitro:

T0901317 (5-50 μM; 72 hours) significantly inhibits cellular proliferation in CaOV3, SKOV3, A2780 (human ovarian carcinoma cell lines) in a dose-dependent and time-dependent manner. T0901317 (10 μM; 24-72 hours) decreases the percentage of cells in S phase and increases the percentage of cells in the G0/G1 phase, indicating a cell cycle arrest at the G1-S checkpoint. The percentage of cells in G0/G1 phase increases in a time-dependent manner. T0901317 (10-40 μM; 24 hours ) results in a significant increase of cells in early apoptosis. T0901317 (5-40 μM; 48 hours) results in an increase of p21 and p27 protein expression in a dose-dependent manner after 48 hours.

In Vivo:

T0901317 (10 mg/kg/day; orally; for 12 weeks) inhibits the progression of atherosclerosis. T0901317 (i.p.; 50 mg/kg; twice weekly for 7 days) can protect male C57BL/6 mice from high fat diet-induced obesity and insulin resistance.

References:

1. J R Schultz, et al. Role of LXRs in Control of Lipogenesis. Genes Dev. 2000 Nov 15;14(22):2831-8.
2. Keith A Houck, et al. T0901317 Is a Dual LXR/FXR Agonist. Mol Genet Metab. Sep-Oct 2004;83(1-2):184-7.
3. Naresh Kumar, et al. The Benzenesulfoamide T0901317 [N-(2,2,2-trifluoroethyl)-N-[4-[2,2,2-trifluoro-1-hydroxy-1-(trifluoromethyl)ethyl]phenyl]-benzenesulfonamide] Is a Novel Retinoic Acid Receptor-Related Orphan Receptor-Alpha/Gamma Inverse Agonist. Mol Pharmacol. 2010 Feb;77(2):228-36.

Products are for research use only. Not for human use.