T0901317

• CAT Number: I003023
• CAS Number: 293754-55-9
• Molecular Formula: C17H12F9NO3S
• Molecular Weight: 481.33
• Purity: ≥95%
• Target: LXR
• Solubility: DMSO: ≥ 30 mg/mL
• Storage: Store at -20°C
• IUPAC Name: N-[4-(1,1,1,3,3,3-hexafluoro-2-hydroxypropan-2-yl)phenyl]-N-(2,2,2-trifluoroethyl)benzenesulfonamide
• 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
• InChIKey: SGIWFELWJPNFDH-UHFFFAOYSA-N
• SMILES: C1=CC=C(C=C1)S(=O)(=O)N(CC(F)(F)F)C2=CC=C(C=C2)C(C(F)(F)F)(C(F)(F)F)O

T0901317（Cat No.:I003023） is a potent and selective LXR and FXR agonist with EC50 of approximately 50nM and 5μM, respectively. T0901317 is a dual inverse agonist of RORα and RORγ, with Ki values of 132nM and 51nM, respectively. T0901317 can significantly inhibit cell proliferation and induce apoptosis.

Reference

1:The LXR ligand T0901317 acutely inhibits insulin secretion by affecting mitochondrial metabolism. Maczewsky J, Sikimic J, Bauer C, Krippeit-Drews P, Wolke C, Lendeckel U, Barthlen W, Drews G.Endocrinology. 2017 Apr 25. doi: 10.1210/en.2016-1941. [Epub ahead of print] PMID: 28449117 2:Liver X receptor agonist T0901317 reverses resistance of A549 human lung cancer cells to EGFR-TKI treatment. Cao H, Yu S, Chen D, Jing C, Wang Z, Ma R, Liu S, Ni J, Feng J, Wu J.FEBS Open Bio. 2016 Dec 20;7(1):35-43. doi: 10.1002/2211-5463.12147. eCollection 2017 Jan. PMID: 28097086 Free PMC Article3:Functional induction of P-glycoprotein efflux pump by phenyl benzenesulfonamides: Synthesis and biological evaluation of T0901317 analogs. Padala AK, Wani A, Vishwakarma RA, Kumar A, Bharate SB.Eur J Med Chem. 2016 Oct 21;122:744-55. doi: 10.1016/j.ejmech.2016.07.005. Epub 2016 Jul 6. PMID: 27497733 4:LXR agonist T0901317 upregulates thrombomodulin expression in glomerular endothelial cells by inhibition of nuclear factor‑κB. Ding H, Li Y, Feng Y, Chen J, Zhong X, Wang N, Wang W, Zhang P, Wang L.Mol Med Rep. 2016 Jun;13(6):4888-96. doi: 10.3892/mmr.2016.5138. Epub 2016 Apr 15. PMID: 27082844 5:Altered activity profile of a tertiary silanol analog of multi-targeting nuclear receptor modulator T0901317. Toyama H, Sato S, Shirakawa H, Komai M, Hashimoto Y, Fujii S.Bioorg Med Chem Lett. 2016 Apr 1;26(7):1817-20. doi: 10.1016/j.bmcl.2016.02.031. Epub 2016 Feb 12. PMID: 26905831 6:Cold Exposure Improves the Anti-diabetic Effect of T0901317 in Streptozotocin-Induced Diabetic Mice. Gao M, Zhang C, Ma Y, Liu D.AAPS J. 2015 May;17(3):700-10. doi: 10.1208/s12248-015-9746-4. Epub 2015 Mar 5. PMID: 25739819 Free PMC Article7:LXR agonist T0901317-Induced hyperlipidemia does not lead to lipid accumulation in the rat heart. Harasiuk D, Baranowski M, Zabielski P, Chabowski A, Górski J.Cell Physiol Biochem. 2015;35(3):1095-106. doi: 10.1159/000373935. Epub 2015 Feb 2. PMID: 25659329 Free Article8:Insulin-sensitizing effect of LXR agonist T0901317 in high-fat fed rats is associated with restored muscle GLUT4 expression and insulin-stimulated AS160 phosphorylation. Baranowski M, Zabielski P, Błachnio-Zabielska AU, Harasim E, Chabowski A, Górski J.Cell Physiol Biochem. 2014;33(4):1047-57. doi: 10.1159/000358675. Epub 2014 Apr 4. PMID: 24732673 Free Article9:Liver X receptor agonist T0901317 reduces neuropathological changes and improves memory in mouse models of experimental dementia. Sodhi RK, Singh N.Eur J Pharmacol. 2014 Jun 5;732:50-9. doi: 10.1016/j.ejphar.2014.03.025. Epub 2014 Mar 29. PMID: 24690259 10:A liver-X-receptor ligand, T0901317, attenuates IgE production and airway remodeling in chronic asthma model of mice. Shi Y, Xu X, Tan Y, Mao S, Fang S, Gu W.PLoS One. 2014 Mar 28;9(3):e92668. doi: 10.1371/journal.pone.0092668. eCollection 2014. PMID: 24681543 Free PMC Article