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SR12813

🥰Excellent
Catalog No. T6994Cas No. 126411-39-0
Alias SR-12813, SR 12813, GW 485801

SR12813 (GW 485801) is a pregnane X receptor (PXR) agonist.

SR12813

SR12813

🥰Excellent
Purity: 99.43%
Catalog No. T6994Alias SR-12813, SR 12813, GW 485801Cas No. 126411-39-0
SR12813 (GW 485801) is a pregnane X receptor (PXR) agonist.
Pack SizePriceAvailabilityQuantity
5 mg47 € In Stock
10 mg64 € In Stock
25 mg136 € In Stock
50 mg230 € In Stock
100 mg333 € In Stock
200 mg538 € In Stock
1 mL x 10 mM (in DMSO)52 € In Stock
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Purity:99.43%
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Product Introduction

Bioactivity
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)
AliasSR-12813, SR 12813, GW 485801
Chemical Properties
Molecular Weight504.53
FormulaC24H42O7P2
Cas No.126411-39-0
SmilesP(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 & Solubility Information
StoragePowder: -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
1mg5mg10mg50mg
1 mM1.9820 mL9.9102 mL19.8204 mL99.1021 mL
5 mM0.3964 mL1.9820 mL3.9641 mL19.8204 mL
10 mM0.1982 mL0.9910 mL1.9820 mL9.9102 mL
20 mM0.0991 mL0.4955 mL0.9910 mL4.9551 mL
50 mM0.0396 mL0.1982 mL0.3964 mL1.9820 mL
100 mM0.0198 mL0.0991 mL0.1982 mL0.9910 mL

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