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Cat. No. Name Size Price Add Cart
KI2429T090131725 mg$234
T0901317100 mg$752

Chemical Characteristic

Product NameT0901317
CAS No.293754-55-9
Molecular Weight 481.3
FormulaC17H12F9NO3S
Chemical NameN-[4-(1,1,1,3,3,3-hexafluoro-2-hydroxypropan-2-yl)phenyl]-N-(2,2,2-trifluoroethyl)benzenesulfonamide
Smilesc1(ccccc1)S(=O)(=O)N(c1ccc(cc1)C(C(F)(F)F)(C(F)(F)F)O)CC(F)(F)F
Chemical Structure

Biological activities

T0901317 is a potent and selective dual agonist of oxysterol receptor (LXR) and the bile acid receptor (FXR). The EC50 value of T0901317 for LXR is 50 nM.[1] The EC50 value of T0901317 for FXR is 5 µM. T0901317 induces FXR target genes BSEP and SHP in Huh7 cells.[2] In vitro, T0901317 treatment also causes LXR-dependent up-regulation of ABC1 expression in macrophages.[1] T0901317 inhibits Aβ production in vitro, being more prominent in primary neurons than in non-neuronal cells. In APP23 mice, T0901317 treatment shows a significant increase in ABCA1 expression and a decrease in the ratio of soluble APP (sAPP)β- to sAPPα-cleavage products. Moreover, T0901317 treatment also causes a significant reduction in the levels of soluble Aβ40 and of Aβ42 in the brain of APP23 mice.[3] T0901317 administration causes a more severe hypertriacylglycerolemia and hepatic triacylglycerol accumulation in diabetic db/db mice than observed in nondiabetic mice. T0901317 administration also upregulates the LXR target genes ABCA1, SREBP1c, FAS, and stearoyl-CoA desaturase 1 in both diabetic db/db and nondiabetic C57BLKS mice.[4] In Lxra/b-deficient mice, T0901317 treatment (50 mg/kg) inhibits cholesterol absorption and prevents liver cholesterol accumulation.[1]

Protocols

In vivo, T0901317 is dissolved in 0.125% carboxymethyl cellulose.[5]

References

[1] Repa JJ, et al. Regulation of absorption and ABC1-mediated efflux of cholesterol by RXR heterodimers. Science. 2000, 289(5484): 1524-1529.
[2] Houck KA, et al. T0901317 is a dual LXR/FXR agonist. Mol Genet Metab. 2004, 83(1-2): 184-187.
[3] Koldamova RP, et al. The liver X receptor ligand T0901317 decreases amyloid beta production in vitro and in a mouse model of Alzheimer's disease. J Biol Chem. 2005, 280(6): 4079-4088.
[4] Chisholm JW, et al. The LXR ligand T0901317 induces severe lipogenesis in the db/db diabetic mouse. J Lipid Res. 2003, 44(11): 2039-2048.
[5] Liu Y, et al. Liver X receptor agonist T0901317 inhibition of glucocorticoid receptor expression in hepatocytes may contribute to the amelioration of diabetic syndrome in db/db mice. Endocrinology. 2006, 147(11): 5061-5068.

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