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SR 12813 is a pregnane X receptor (PXR) agonist (EC50 values are 200 and 700 nM for human and rabbit PXR respectively). Activates the farnesoid X receptor (FXR) at μM concentrations. Displays hypocholesterolaemic activity via enchanced degradation of HMG-CoA reductase.
|Storage||Store at +4°C|
The technical data provided above is for guidance only. For batch specific data refer to the Certificate of Analysis.
Tocris products are intended for laboratory research use only, unless stated otherwise.
|Solvent||Max Conc. mg/mL||Max Conc. mM|
The following data is based on the product molecular weight 504.53. Batch specific molecular weights may vary from batch to batch due to the degree of hydration, which will affect the solvent volumes required to prepare stock solutions.
|Concentration / Solvent Volume / Mass||1 mg||5 mg||10 mg|
|1 mM||1.98 mL||9.91 mL||19.82 mL|
|5 mM||0.4 mL||1.98 mL||3.96 mL|
|10 mM||0.2 mL||0.99 mL||1.98 mL|
|50 mM||0.04 mL||0.2 mL||0.4 mL|
References are publications that support the biological activity of the product.
Berkhout et al (1996) The novel cholesterol-lowering drug SR-12813 inhibits cholesterol synthesis via an increased degradation of 3-hydroxy-3-methylglutaryl-coenzyme A reductase J.Biol.Chem. 271 14376 PMID: 8662919
Lemaire et al (2007) Discovery of a highly active ligand of human pregnane X receptor: a case study from pharmacophore modeling and virtual screening to "in vivo" biological activity. Mol.Pharmacol. 72 572 PMID: 17573484
Jones et al (2000) The pregnane X receptor: a promiscuous xenobiotic receptor that has diverged during evolution. Mol.Pharmacol. 14 27
If you know of a relevant reference for SR 12813, please let us know.
Keywords: SR 12813, SR 12813 supplier, Pregnane, X, receptor, PXR, agonists, Nuclear, Receptors, SR12813, HMG-CoA, Reductase, Receptor, 2969, Tocris Bioscience
Citations are publications that use Tocris products. Selected citations for SR 12813 include:
Delfosse et al (2015) Synergistic activation of human pregnane X receptor by binary cocktails of pharmaceutical and environmental compounds. Nat Commun 6 8089 PMID: 26333997
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