SR-12813

Catalog No.S8302 Batch:S830201

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Technical Data

Formula

C24H42O7P2
Molecular Weight 504.53 CAS No. 126411-39-0
Solubility (25°C)* In vitro DMSO 100 mg/mL (198.2 mM)
Ethanol 100 mg/mL (198.2 mM)
Water Insoluble
* <1 mg/ml means slightly soluble or insoluble.
* Please note that Selleck tests the solubility of all compounds in-house, and the actual solubility may differ slightly from published values. This is normal and is due to slight batch-to-batch variations.
* Room temperature shipping (Stability testing shows this product can be shipped without any cooling measures.)

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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 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].

Protocol (from reference)

Cell Assay:[2]
  • 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.
Animal Study:[3]
  • Animal Models

    beagle dogs

  • Dosages

    10 mg/kg

  • Administration

    p.o.

Selleck's SR-12813 has been cited by 2 publications

Protective Effect of NGR1 against Glutamate-Induced Cytotoxicity in HT22 Hippocampal Neuronal Cells by Upregulating the SIRT1/Wnt/β-Catenin Pathway [ Evid Based Complement Alternat Med, 2021, 2021:4358163] PubMed: 34956378
Targeting the COX2/MET/TOPK signaling axis induces apoptosis in gefitinib-resistant NSCLC cells. [ Cell Death Dis, 2019, 10(10):777] PubMed: 31611604

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SHIPPING AND STORAGE
Selleck products are transported at room temperature. If you receive the product at room temperature, please rest assured, the Selleck Quality Inspection Department has conducted experiments to verify that the normal temperature placement of one month will not affect the biological activity of powder products. After collecting, please store the product according to the requirements described in the datasheet. Most Selleck products are stable under the recommended conditions.

NOT FOR HUMAN, VETERINARY DIAGNOSTIC OR THERAPEUTIC USE.