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SR12813

Name: SR12813
Brand: TargetMol
SKU: T6994
Price: 50 USD
Availability: InStock
Rating: 5 (10 reviews)

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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

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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	USA Warehouse	Global Warehouse
5 mg	$50	In Stock	In Stock
10 mg	$68	In Stock	In Stock
25 mg	$144	In Stock	In Stock
50 mg	$243	In Stock	In Stock
100 mg	$351	In Stock	In Stock
200 mg	$567	-	In Stock
1 mL x 10 mM (in DMSO)	$55	In Stock	In Stock

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In Stock Estimated shipping dateUSA Warehouse[1-2 days] Global Warehouse[5-7 days]

This molecule is a custom-made product. TargetMol has an excellent synthesis team with the experience and capability to provide you with cost-effective products.If you have any questions, please feel free to contact us. We are committed to serving you wholeheartedly.

All TargetMol products are for research purposes only and cannot be used for human consumption. We do not provide products or services to individuals. Please comply with the intended use and do not use TargetMol products for any other purpose.

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Batch Information

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Purity:99.43%

Appearance:Solid

Color:White

Resource Download

COA HNMR HPLC LCMS

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)
Synonyms	SR-12813, SR 12813, GW 485801

Chemical Properties

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

In solvent: -80°C for 1 year | Shipping with blue ice/Shipping at ambient temperature.

Solubility Information

DMSO: 50.5 mg/mL (100.09 mM), Sonication is recommended.

Ethanol: 50.5 mg/mL (100.09 mM), Sonication is recommended.

In Vivo Formulation

10% DMSO+40% PEG300+5% Tween 80+45% Saline: 2 mg/mL (3.96 mM), Sonication is recommended.

Please add the solvents sequentially, clarifying the solution as much as possible before adding the next one. Dissolve by heating and/or sonication if necessary. Working solution is recommended to be prepared and used immediately. The formulation provided above is for reference purposes only. In vivo formulations may vary and should be modified based on specific experimental conditions.

Solution Preparation Table

DMSO/Ethanol

	1mg	5mg	10mg	50mg
1 mM	1.9820 mL	9.9102 mL	19.8204 mL	99.1021 mL
5 mM	0.3964 mL	1.9820 mL	3.9641 mL	19.8204 mL
10 mM	0.1982 mL	0.9910 mL	1.9820 mL	9.9102 mL
20 mM	0.0991 mL	0.4955 mL	0.9910 mL	4.9551 mL
50 mM	0.0396 mL	0.1982 mL	0.3964 mL	1.9820 mL
100 mM	0.0198 mL	0.0991 mL	0.1982 mL	0.9910 mL

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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 stock solution preparation method and in vivo formula preparation method:

For example, if the intended dosage is 10 mg/kg for animals weighing 20 g , with a dosing volume of 100 μL per animal, TargetMol | Animal experiments

and a total of 10 animals are to be administered, using a formulation of TargetMol | reagent

10% DMSO+ 40% PEG300+ 5% Tween 80+ 45% Saline/PBS/ddH₂O , the resulting working solution concentration would be 2 mg/mL.

Stock Solution Preparation:

Dissolve 2 mg of the compound in 100 μL DMSO TargetMol | reagent to obtain a stock solution at a concentration of 20 mg/mL . If the required concentration exceeds the compound's known solubility, please contact us for technical support before proceeding.

Preparation of the In Vivo Formulation:

1) Add 100 μL of the DMSO TargetMol | reagent stock solution to 400 μL PEG300 and mix thoroughly until the solution becomes clear.

2) Add 50 μL Tween 80 and mix well until fully clarified.

3) Add 450 μL Saline,PBS or ddH₂O TargetMol | reagent and mix thoroughly until a homogeneous solution is obtained.

This example is provided solely to demonstrate the use of the In Vivo Formulation Calculator and does not constitute a recommended formulation for any specific compound. Please select an appropriate dissolution and formulation strategy based on your experimental model and route of administration.

All co-solvents required for this protocol, includingDMSO, PEG300/PEG400, Tween 80, SBE-β-CD, and Corn oil, are available for purchase on the TargetMol website.

Dose Conversion

You can also refer to dose conversion for different animals. More Dose Conversion

Tech Support

Please see Inhibitor Handling Instructions for more frequently ask questions. Topics include: how to prepare stock solutions, how to store products, and cautions on cell-based assays & animal experiments, etc