Home Metabolism HMG-CoA Reductase inhibitor SR-12813 For research use only.

SR-12813

SR-12813 is a pregnane X receptor (PXR) agonist and HMG-CoA reductase inhibitor with an IC50 of 850 nM.

SR-12813 Chemical Structure

SR-12813 Chemical Structure

CAS No. 126411-39-0

Purity & Quality Control

SR-12813 Related Products

Signaling Pathway

HMG-CoA Reductase Signaling Pathways

HMG-CoA Reductase Signaling Pathway

Biological Activity

Description SR-12813 is a pregnane X receptor (PXR) agonist and HMG-CoA reductase inhibitor with an IC50 of 850 nM.
Targets
pregnane X receptor [1] HMG-CoA reductase [2]
850 nM
In vitro
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].
Cell Research Cell lines Hep G2 cells
Concentrations 3 μM
Incubation Time 21 h
Method 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.
In Vivo
In vivo The bisphosphonate ester SR12813 lowers cholesterol levels in a range of species including rats, dogs and primates[1].
Animal Research Animal Models beagle dogs
Dosages 10 mg/kg
Administration p.o.

Chemical Information & Solubility

Molecular Weight 504.53 Formula

C24H42O7P2
CAS No. 126411-39-0 SDF Download SR-12813 SDF
Smiles CCOP(=O)(C(=CC1=CC(=C(C(=C1)C(C)(C)C)O)C(C)(C)C)P(=O)(OCC)OCC)OCC
Storage (From the date of receipt)

In vitro
Batch:

DMSO : 100 mg/mL ( (198.2 mM) Moisture-absorbing DMSO reduces solubility. Please use fresh DMSO.)

Ethanol : 100 mg/mL

Water : Insoluble


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In vivo
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Method for preparing DMSO master liquid: mg drug pre-dissolved in μL DMSO ( Master liquid concentration mg/mL, Please contact us first if the concentration exceeds the DMSO solubility of the batch of drug. )

Method for preparing in vivo formulation: Take μL DMSO master liquid, next addμL PEG300, mix and clarify, next addμL Tween 80, mix and clarify, next add μL ddH2O, mix and clarify.

Method for preparing in vivo formulation: Take μL DMSO master liquid, next add μL Corn oil, mix and clarify.

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Tech Support

Answers to questions you may have can be found in the inhibitor handling instructions. Topics include how to prepare stock solutions, how to store inhibitors, and issues that need special attention for cell-based assays and animal experiments.

Handling Instructions

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