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Purity: ≥98%
T0901317 (formerly known as T-1317 or TO-091317 or TO 901317) is a potent and selective liver X receptor (LXR) agonist for multiple targets, which has EC50 values of 20 nM and 5 μM for LXRα and FXR, respectively. It has the potential for the treatment of atherosclerosis. In addition, it is RORα and RORγ dual inverse agonist with estimated IC50 of 2.0 μM and 1.7 μM, respectively. T0901317 inhibited transactivation activity of RORα and RORγ by direct binding with high affinity which led to the regulation of the receptor’s ability to interact with transcriptional cofactor proteins, but did not show inhibitory activity against RORβ.
| ln Vitro |
In a dose- and time-dependent way, T0901317 (5-50 μM; 72 hours) effectively reduces the cell growth of human ovarian cancer cell lines, CaOV3, SKOV3, and A2780 [5]. Cell cycle arrest at the G1-S checkpoint is indicated by T0901317 (10 μM; 24-72 hours) which decreases the percentage of cells in S phase and increases the percentage of cells in G0/G1 phase. Time-dependently, the proportion of cells in the G0/G1 phase rises [5]. Twenty-four hours at 10–40 μM, T0901317 significantly increases early apoptosis [5]. After 48 hours, T0901317 (5–40 μM; 48 hours) increases the expression of the proteins p21 and p27 in a dose-dependent manner [5].
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| ln Vivo |
T0901317 (10 mg/kg/day; oral; 12 weeks) slows the rate at which atherosclerosis advances [5]. T0901317 (ip; 50 mg/kg; twice weekly for 7 days) prevents insulin resistance and obesity in male C57BL/6 mice fed a high-fat diet [6].
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| Cell Assay |
Cell Proliferation Assay[5]
Cell Types: A2780, CaOV3 and SKOV3 ovarian cancer cell lines Tested Concentrations: 5, 10, 20, 40 or 50 μM Incubation Duration: 72 hrs (hours) Experimental Results: Inhibited cellular proliferation in all cell lines in a dose-dependent and time-dependent manner. Cell Cycle Analysis[5] Cell Types: A2780, CaOV3 and SKOV3 cells Tested Concentrations: 10 μM Incubation Duration: 24, 48 or 72 hrs (hours) Experimental Results: diminished the percentage of cells in S phase and increased the percentage of cells in the G0/G1 phase. Apoptosis Analysis[5] Cell Types: CaOV3 cells Tested Concentrations: 10 to 40 μM Incubation Duration: 24 hrs (hours) Experimental Results: Resulted in a significant increase of cells in early apoptosis. Western Blot Analysis[5] Cell Types: CaOV3 cells Tested Concentrations: 5 to 40 μM Incubation Duration: 48 hrs (hours) Experimental Results: Resulted in an increase of p21 and p27 protein expression in a dose-dependent manner. |
| Animal Protocol |
Animal/Disease Models: 8- to 10weeks old LDL receptor null mice[5]
Doses: 10 mg/kg Route of Administration: po (oral gavage) daily; for 12 weeks Experimental Results: Inhibited the progression of atherosclerosis. |
| 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. [4]. Rough JJ, et al. Anti-proliferative effect of LXR agonist T0901317 in ovarian carcinoma cells. J Ovarian Res. 2010 May 26;3:13. [5]. Todd G Kirchgessner, et al. Beneficial and Adverse Effects of an LXR Agonist on Human Lipid and Lipoprotein Metabolism and Circulating Neutrophils. Cell Metab. 2016 Aug 9;24(2):223-33. [6]. Mingming Gao, et al. The Liver X Receptor Agonist T0901317 Protects Mice From High Fat Diet-Induced Obesity and Insulin Resistance. AAPS J. 2013 Jan;15(1):258-66. |
| Molecular Formula |
C17H12F9NO3S
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| Molecular Weight |
481.33
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| CAS # |
293754-55-9
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| Related CAS # |
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| SMILES |
OC(C(F)(F)F)(C(F)(F)F)C1=CC=C(N(CC(F)(F)F)S(C2=CC=CC=C2)(=O)=O)C=C1
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| Synonyms |
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| Storage |
Powder -20°C 3 years 4°C 2 years In solvent -80°C 6 months -20°C 1 month |
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| Shipping Condition |
Room temperature (This product is stable at ambient temperature for a few days during ordinary shipping and time spent in Customs)
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| Solubility (In Vitro) |
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| Preparing Stock Solutions | 1 mg | 5 mg | 10 mg | |
| 1 mM | 2.0776 mL | 10.3879 mL | 20.7758 mL | |
| 5 mM | 0.4155 mL | 2.0776 mL | 4.1552 mL | |
| 10 mM | 0.2078 mL | 1.0388 mL | 2.0776 mL |
*Note: Please select an appropriate solvent for the preparation of stock solution based on your experiment needs. For most products, DMSO can be used for preparing stock solutions (e.g. 5 mM, 10 mM, or 20 mM concentration); some products with high aqueous solubility may be dissolved in water directly. Solubility information is available at the above Solubility Data section. Once the stock solution is prepared, aliquot it to routine usage volumes and store at -20°C or -80°C. Avoid repeated freeze and thaw cycles.
Calculation results
Working concentration： mg/mL；
Method for preparing DMSO stock solution： mg drug pre-dissolved in μL DMSO (stock solution concentration mg/mL). Please contact us first if the concentration exceeds the DMSO solubility of the batch of drug.
Method for preparing in vivo formulation:：Take μL DMSO stock solution, next add μL PEG300, mix and clarify, next addμL Tween 80, mix and clarify, next add μL ddH2O，mix and clarify.
(1) Please be sure that the solution is clear before the addition of next solvent. Dissolution methods like vortex, ultrasound or warming and heat may be used to aid dissolving.
(2) Be sure to add the solvent(s) in order.
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