肝X受体(liverXreceptors,L…

肝X受体(liverXreceptors,LXRs)激动剂:T0901317
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  • 参考报价:392 产地:美国 品牌:cayman chemical 型号:71810-10 更新时间:2012/7/19

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T0901317

Cayman Chemical Item Number 71810

(CAS 293754-55-9)

T0901317 (CAS 293754-55-9)

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  • Nuclear Receptors (80)
  • Atherosclerosis (323)

Description

The Liver X Receptors (LXRα and LXRβ) are nuclear hormone receptors whose native ligands are oxysterols, such as 22(R)-hydroxycholesterol. The LXRs regulate the oxysterol-induced expression of cholesterol 7α-hydroxylase, the rate limiting enzyme of classic bile acid synthesis. T0901317 is a potent and selective agonist for both LXRα and LXRβ, with an EC50 of about 50 nM.1 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 from enterocytes and thus inhibit the overall absorption of cholesterol.

1 Repa, J.J., Turley, S.D., Lobaccaro, J.A., et al. Regulation of absorption and ABC1-mediated efflux of cholesterol by RXR heterodimers. Science 289 1524-1529 (2000).

Formal Name N-?(2,?2,?2-?trifluoroethyl)-?N-?[4-?[2,?2,?2-?trifluoro-?1-?hydroxy-?1-?(trifluoromethyl)ethyl]phenyl]-?benzenesulfonamide
CAS Number 293754-55-9
Molecular Formula C17H12F9NO3S
Formula Weight 481.3
Formulation A crystalline solid
Purity >98%
λmax 227, 265, 272 nm
Stability 1 year
Storage -20°C
Shipping Wet ice in continental US; may vary elsewhere
SMILES O=S(=O)?(c1ccccc1)?N(CC(F)?(F)?F)?c1ccc(cc1)?C(O)?(C(F)?(F)?F)?C(F)?(F)?F

Background Reading

Repa, J.J., Turley, S.D., Lobaccaro, J.A., et al. Regulation of absorption and ABC1-mediated efflux of cholesterol by RXR heterodimers. Science 289 1524-1529 (2000).

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