T0901317T0901317
MedChemExpress (MCE)
HY-10626
293754-55-9
99.93%
Powder -20°C 3 years 4°C 2 years In solvent -80°C 6 months -20°C 1 month
Room temperature in continental US
may vary elsewhere.
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.
rateand the 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[5]. 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[5]. T0901317 (10-40 μM
24 hours) results in a significant increase of cells in early apoptosis[5]. T0901317 (5-40 μM
48 hours) results in an increase of p21 and p27 protein expression in a dose-dependent manner after 48 hours[5].
T0901317 (10 mg/kg/day
orally
for 12 weeks) inhibits the progression of atherosclerosis[5]. 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[6].
EC50: 20 nM (LXRα) and 5 μM (FXR)[1][2] Ki: 132 nM (RORα) and 51 nM (RORγ)[3] Cellular Effect Cell Line Type Value Description References
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[1]. J R Schultz, et al. Role of LXRs in Control of Lipogenesis. Genes Dev. 2000 Nov 15
14(22):2831-8. [Content Brief]
[2]. Keith A Houck, et al. T0901317 Is a Dual LXR/FXR Agonist. Mol Genet Metab. Sep-Oct 2004
83(1-2):184-7. [Content Brief]
[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. [Content Brief]
[4]. Rough JJ, et al. Anti-proliferative effect of LXR agonist T0901317 in ovarian carcinoma cells. J Ovarian Res. 2010 May 26
3:13. [Content Brief]
[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. [Content Brief]
[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. [Content Brief]