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AdipoGen Life Sciences
T0901317
40
CHF
CHF 40.00
In stock
AG-CR1-2906-M01010 mgCHF 40.00
AG-CR1-2906-M05050 mgCHF 130.00
| Product Details | |
|---|---|
| Synonyms | TO-901317; T 1317 |
| Product Type | Chemical |
| Properties | |
| Formula |
C17H12F9NO3S |
| MW | 481.3 |
| CAS | 293754-55-9 |
| RTECS | DB3192000 |
| Purity Chemicals | ≥97% |
| Appearance | White to off-white solid. |
| Solubility | Soluble in DMSO, DMF or ethanol (all 50mg/ml). |
| InChi Key | SGIWFELWJPNFDH-UHFFFAOYSA-N |
| 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) |
| Shipping and Handling | |
| Shipping | AMBIENT |
| Short Term Storage | +4°C |
| Long Term Storage | -20°C |
| Handling Advice | Keep cool and dry. |
| 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. |
| Documents | |
| MSDS |
 Download PDF |
| Product Specification Sheet | |
| Datasheet |
Download PDF |
Description
- T0901317 is a potent, cell permeable and selective agonist of LXRα and LXRβ (EC50 of 50nM, Kd values are 7 and 22 nM for LXR-α and LXR-β, respectively), results in LXR-dependent up-regulation of ABC1 gene expression. The Liver X Receptors (LXRα and LXRβ) 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 RORα and RORγ 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.
Product 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)
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