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SR12813

Chemical Structure : SR12813

CAS No.: 126411-39-0

SR12813 (SR-12813;SR 12813;GW 485801;GW-485801;GW485801)

Catalog No.: PC-42261Not For Human Use, Lab Use Only.

SR12813 (GW485801) is potent and efficacious pregnane X receptor (PXR) activator with EC50 of 200 and 700 nM for human and rabbit PXR, respectively.

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Purity & Documentation Purity: >98% (HPLC) Select Batch:

Biological Activity

SR12813 (GW485801) is potent and efficacious pregnane X receptor (PXR) activator with EC50 of 200 and 700 nM for human and rabbit PXR, respectively.
SR12813 (GW485801) only shows weak activition for rat and mouse PXR.
SR12813 (GW485801) inhibits cholesterol synthesis (IC50=1.2 uM) with no effect on fatty acid synthesis, reduces cellular HMG-CoA reductase activity with IC50 of 0.85 uM.
SR12813 (GW485801) induce CYP3A expression in primary hepatocytes.

Physicochemical Properties

M.Wt 504.5336
Formula C24H42O7P2
Appearance Solid
CAS No.
Storage
Solide Powder
-20 °C 12 Months; 4°C 6 Months
In Solvent
-80 °C 6 Months; -20°C 6 Months
Shipping
Solubility

10 mM in DMSO

Chemical Name/SMILES

Phosphonic acid, P,P'-[[3,5-bis(1,1-dimethylethyl)-4-hydroxyphenyl]ethenylidene]bis-, P,P,P',P'-tetraethyl ester

References

1. Jones SA, et al. Mol Endocrinol. 2000 Jan;14(1):27-39.

2. Berkhout TA, et al. J Biol Chem. 1996 Jun 14;271(24):14376-82.

3. Watkins RE, et al. Science. 2001 Jun 22;292(5525):2329-33.

4. Berkhout TA, et al. Atherosclerosis. 1997 Sep;133(2):203-12.

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