T0901317

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AdipoGen Life Sciences
Product Code: AG-CR1-2906
Product Group: Other Biochemicals
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AG-CR1-2906-M01010 mg£35.00
Quantity:
AG-CR1-2906-M05050 mg£105.00
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Prices exclude any Taxes / VAT

Overview

Regulatory Status: RUO
Shipping:
Ambient
Storage:
-20°C

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Chemical Structure
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Chemical Structure

Documents

Further Information

Alternate Names/Synonyms:
TO-901317; T 1317
Appearance:
White to off-white solid.
CAS:
293754-55-9
EClass:
32160000
Form (Short):
liquid
Handling Advice:
Keep cool and dry.
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
Long Description:
Chemical. CAS: 293754-55-9. Formula: C17H12F9NO3S. MW: 481.3. T0901317 is a potent, cell permeable and selective agonist of LXRalpha and LXRbeta (EC50 of 50nM, Kd values are 7 and 22 nM for LXR-alpha and LXR-beta, respectively), results in LXR-dependent up-regulation of ABC1 gene expression. The Liver X Receptors (LXRalpha and LXRbeta) are nuclear hormone receptors whose native ligands are oxysterols. T0901317 acting through LXR and in concert with its RXR heterodimerization partner induces the expression of the ABCA1 reverse cholesterol transporter. This acts to increase the efflux of cholesterol and regulation of HDL metabolism. T0901317 activates farnesoid X receptor (FXR) (EC50 ~5µM), less potent then LXR, but activates FXR more potently than a natural bile acid FXR ligand, chenodeoxycholic acid. It also is a high-affinity ligand for the xenobiotic receptor pregnane X receptor (PXR). T0901317 binds and activates PXR with the same nanomolar potency with which it stimulates LXR activity. T0901317 directly binds retinoic acid receptor-related orphan receptors RORalpha and RORgamma with high affinity (K(i) = 132 and 51nM, respectively) resulting in the modulation of the receptor's ability to interact with transcriptional cofactor proteins. T0901317 acts as an antiandrogen for AR in prostate cancer cells. T0901317 shows anti-atherosclerosis, antidiabetic, insulin sensitizing, anticancer, anti-proliferative, metabolism modulating and neuroprotective properties. Exhibits inverse agonist activity at human constitutive androstane receptor (CAR), a member of the nuclear receptor superfamily and key regulator of xenobiotic and endobiotic metabolism.
MDL:
MFCD03412028
Molecular Formula:
C17H12F9NO3S
Molecular Weight:
481.3
Package Type:
Vial
Product Description:
T0901317 is a potent, cell permeable and selective agonist of LXRalpha and LXRbeta (EC50 of 50nM, Kd values are 7 and 22 nM for LXR-alpha and LXR-beta, respectively), results in LXR-dependent up-regulation of ABC1 gene expression. The Liver X Receptors (LXRalpha and LXRbeta) are nuclear hormone receptors whose native ligands are oxysterols. T0901317 acting through LXR and in concert with its RXR heterodimerization partner induces the expression of the ABCA1 reverse cholesterol transporter. This acts to increase the efflux of cholesterol and regulation of HDL metabolism. T0901317 activates farnesoid X receptor (FXR) (EC50 ~5µM), less potent then LXR, but activates FXR more potently than a natural bile acid FXR ligand, chenodeoxycholic acid. It also is a high-affinity ligand for the xenobiotic receptor pregnane X receptor (PXR). T0901317 binds and activates PXR with the same nanomolar potency with which it stimulates LXR activity. T0901317 directly binds retinoic acid receptor-related orphan receptors RORalpha and RORgamma with high affinity (K(i) = 132 and 51nM, respectively) resulting in the modulation of the receptor's ability to interact with transcriptional cofactor proteins. T0901317 acts as an antiandrogen for AR in prostate cancer cells. T0901317 shows anti-atherosclerosis, antidiabetic, insulin sensitizing, anticancer, anti-proliferative, metabolism modulating and neuroprotective properties. Exhibits inverse agonist activity at human constitutive androstane receptor (CAR), a member of the nuclear receptor superfamily and key regulator of xenobiotic and endobiotic metabolism.
Purity:
>97%
SMILES:
OC(C(F)(F)F)(C(F)(F)F)C(C=C1)=CC=C1N(CC(F)(F)F)S(C2=CC=CC=C2)(=O)
Solubility Chemicals:
Soluble in DMSO, DMF or ethanol (all 50mg/ml).
Transportation:
Non-hazardous
UNSPSC Category:
Biochemical Reagents
UNSPSC Number:
12352200
Use & Stability:
Stable for at least 2 years after receipt when stored at -20°C.Working aliquots are stable for up to 3 months when stored at -20°C.

References

Regulation of absorption and ABC1-mediated efflux of cholesterol by RXR heterodimers: J.J. Repa, et al.; Science 289, 1524 (2000) | Antidiabetic Action of a Liver X Receptor Agonist Mediated by Inhibition of Hepatic Gluconeogenesis: G. Cao, et al.; J. Biol. Chem. 278, 1131 (2002) | T0901317, a potent LXR agonist, is an inverse agonist of CAR: Y. Kanno, et al.; J. Toxicol. Sci. 38, 309 (2013) | T-0901317, a synthetic liver X receptor ligand, inhibits development of atherosclerosis in LDL receptor-deficient mice: N. Terasaka, et al.; FEBS Lett. 536, 6 (2003) | T0901317 is a dual LXR/FXR agonist: K.A. Houck, et al.; Mol. Genet. Metab. 83, 184 (2004) | The liver X receptor ligand T0901317 decreases amyloid beta production in vitro and in a mouse model of Alzheimer's disease: R.P. Koldamova, et al.; J. Biol. Chem. 280, 4079 (2005) | The liver X receptor agonist T0901317 acts as androgen receptor antagonist in human prostate cancer cells: C.P. Chuu, et al.; BBRC 357, 341 (2007) | T0901317 is a potent PXR ligand: implications for the biology ascribed to LXR: N. Mitro, et al.; FEBS Lett. 581, 1721 (2007) | 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: N. Kumar, et al.; Mol. Pharmacol. 77, 228 (2010) | Antiproliferative effect of LXR agonists T0901317 and 22(R)-hydroxycholesterol on multiple human cancer cell lines: C.P. Chuu & H.P. Lin; Anticancer Res. 30, 3643 (2010) | The liver X receptor agonist T0901317 protects mice from high fat diet-induced obesity and insulin resistance: M. Gao & D. Liu; AAPS J. 15, 258 (2013) | Insulin-sensitizing effect of LXR agonist T0901317 in high-fat fed rats is associated with restored muscle GLUT4 expression and insulin-stimulated AS160 phosphorylation: M. Baranowski, et al.; Cell Physiol. Biochem. 33, 1047 (2014) | Liver X receptor agonist T0901317 reduces neuropathological changes and improves memory in mouse models of experimental dementia: R.K. Sodhi & N. Singh; Eur. J. Pharmacol. 732, 50 (2014) | Liver X receptor agonist T0901317 inhibits the migration and invasion of non-small-cell lung cancer cells in vivo and in vitro: R. Lou, et al.; Anticancer Drugs 30, 495 (2019)