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SR12813 (GW 485801) is a pregnane X receptor (PXR) agonist.
Pack Size | Price | Availability | Quantity |
---|---|---|---|
5 mg | 47 € | In Stock | |
10 mg | 64 € | In Stock | |
25 mg | 136 € | In Stock | |
50 mg | 230 € | In Stock | |
100 mg | 333 € | In Stock | |
200 mg | 538 € | In Stock | |
1 mL x 10 mM (in DMSO) | 52 € | In Stock |
Description | SR12813 (GW 485801) is a pregnane X receptor (PXR) agonist. |
Targets&IC50 | HMG-CoA reductase:850 nM |
In vitro | SR12813 is a very potent and efficacious activator of both the human and rabbit PXR, with EC50 values of approximately 200 nM and 700 nM, respectively. By contrast, SR12813 is only a very weak activator of the rat and mouse PXR[1]. SR-12813 inhibits incorporation of tritiated water into cholesterol with an IC50 of 1.2 μM but has no effect on fatty acid synthesis. SR-12813 reduces cellular 3-hydroxy-3-methylglutaryl-coenzyme A (HMG-CoA) reductase activity with an IC50 of 0.85 μM. The inhibition of HMG-CoA reductase activity is rapid with a T1/2 of 10 min[2]. |
In vivo | The bisphosphonate ester SR12813 lowers cholesterol levels in a range of species including rats, dogs and primates[1]. |
Kinase Assay | Briefly, compounds are added to the cells in Me2SO (final concentration, 0.1%). After the experiment cells are lysed by the addition of 0.1 mL of 0.25% Brij 96, 0.1 M sucrose, 0.1 M KF, 50 mM KCl, 40 mM potassium dihydrophosphate, 30 mM EDTA, 5 mM dithiothreitol, pH 7.4 at room temperature. In some experiments KF is omitted to measure 'total' HMG-CoA reductase activity. HMG-CoA reductase activity in the cell lysate is further determined. |
Cell Research | Hep G2 cells are incubated for 21 h with either 1 μM lovastatin or 3 μM SR-12813 in 5% LPDS medium. mRNA is isolated and analyzed by Northern blotting.(Only for Reference) |
Alias | SR-12813, SR 12813, GW 485801 |
Molecular Weight | 504.53 |
Formula | C24H42O7P2 |
Cas No. | 126411-39-0 |
Smiles | P(C(P(OCC)(OCC)=O)=CC1=CC(C(C)(C)C)=C(O)C(C(C)(C)C)=C1)(OCC)(OCC)=O |
Relative Density. | 1.117g/cm3 |
Storage | Powder: -20°C for 3 years | In solvent: -80°C for 1 year | Shipping with blue ice. | |||||||||||||||||||||||||||||||||||
Solubility Information | DMSO: 50.5 mg/mL (100.09 mM), Sonication is recommended. Ethanol: 50.5 mg/mL (100.09 mM), Sonication is recommended. | |||||||||||||||||||||||||||||||||||
Solution Preparation Table | ||||||||||||||||||||||||||||||||||||
DMSO/Ethanol
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