T0901317

Additional information:
T0901317 is an orally active and highly selective LXR agonist with an EC50 of 20 nM for LXRα.{{Daprodustat} web|{Daprodustat} HIF/HIF Prolyl-Hydroxylase|{Daprodustat} Technical Information|{Daprodustat} In stock|{Daprodustat} manufacturer|{Daprodustat} Cancer} T0901317 activates FXR with an EC50 of 5 μM.PMID:32875925 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:|J R Schultz, et al. Role of LXRs in Control of Lipogenesis. Genes Dev. 2000 Nov 15;14(22):2831-8.Keith A Houck, et al. T0901317 Is a Dual LXR/FXR Agonist. Mol Genet Metab. Sep-Oct 2004;83(1-2):184-7.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.|