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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
🥰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 Size | Price | Availability | Quantity |
|---|---|---|---|
| 5 mg | $50 | In Stock | |
| 10 mg | $68 | In Stock | |
| 25 mg | $144 | In Stock | |
| 50 mg | $243 | In Stock | |
| 100 mg | $351 | In Stock | |
| 200 mg | $567 | In Stock | |
| 1 mL x 10 mM (in DMSO) | $55 | In Stock |
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Purity:99.43%
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With extensive experience in compound synthesis, we can provide rapid custom synthesis services for this product according to your research needs.Product Introduction
Bioactivity
Chemical Properties
| 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 & Solubility Information
| 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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In Vivo Formulation Calculator (Clear solution)
Please enter your animal experiment information in the following box and click Calculate to obtain the mother liquor preparation method and in vivo formula preparation method:
For example, your dosage is 10 mg/kg Each animal weighs 20 g, and the dosage volume is 100 μL . A total of 10 animals were administered, and the formula you used is 5% 
DMSO+30% PEG300+5% Tween 80+60% ddH2O. So your working solution concentration is 2 mg/mL。Mother liquor preparation method: 2 mg of drug dissolved in 50 μL DMSO (mother liquor concentration of 40 mg/mL), if you need to configure a concentration that exceeds the solubility of the product, please contact us first.
(mother liquor concentration of 40 mg/mL), if you need to configure a concentration that exceeds the solubility of the product, please contact us first.Preparation method for in vivo formula: Take 50 μL DMSO main solution, add 300 μLPEG300 mix well and clarify, then add 50 more μL Tween 80, mix well and clarify, then add 600 more μLddH2O mix well and clarify
main solution, add 300 μLPEG300 mix well and clarify, then add 50 more μL Tween 80, mix well and clarify, then add 600 more μLddH2O mix well and clarifyFor Reference Only. Please develop an appropriate dissolution method based on your laboratory animals and route of administration.
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