T0901317

T0901317 is an orally active and highly selective LXR agonist with an EC50 of 20 nM for LXRα[1]. T0901317 activates FXR with an EC50 of 5 μM[2]. T0901317 is RORα and RORγ dual inverse agonist with Ki values of 132 nM and 51 nM, respectively[3]. T0901317 induces apoptosis and inhibits the development of atherosclerosis in low-density lipoprotein (LDL) receptor-deficient mice[4][5].

Product Specifications

CAS Number

[293754-55-9]

UNSPSC

12352005

Hazard Statement

H302, H315, H319, H335

Target

Apoptosis; FXR; LXR; ROR

Type

Reference compound

Related Pathways

Apoptosis; Metabolic Enzyme/Protease; Vitamin D Related/Nuclear Receptor

Applications

Cancer-programmed cell death

Field of Research

Cancer; Metabolic Disease; Cardiovascular Disease

Assay Protocol

https://www.medchemexpress.com/T0901317.html

Purity

99.93

Solubility

DMSO : 100 mg/mL (ultrasonic) |Ethanol : 100 mg/mL (ultrasonic)

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

Molecular Formula

C17H12F9NO3S

Molecular Weight

481.33

Precautions

H302, H315, H319, H335

References & Citations

[1]J R Schultz, et al. Role of LXRs in Control of Lipogenesis. Genes Dev. 2000 Nov 15;14 (22) :2831-8.|[2]Rough JJ, et al. Anti-proliferative effect of LXR agonist T0901317 in ovarian carcinoma cells. J Ovarian Res. 2010 May 26;3:13.|[3]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.|[4]Keith A Houck, et al. T0901317 Is a Dual LXR/FXR Agonist. Mol Genet Metab. Sep-Oct 2004;83 (1-2) :184-7.|[5]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.|[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.