Molecular structure of SR 12813, CAS Number: 126411-39-0
SR 12813 (CAS 126411-39-0)
Alternate Names:
4-[2,2-bis(diethoxyphosphoryl)ethenyl]-2,6-ditert-butylphenol
Application:
SR 12813 is a PXR agonist that activates the farnesoid X receptor (FXR) at μM concentrations
CAS Number:
126411-39-0
Purity:
98%
Molecular Weight:
504.53
Molecular Formula:
C24H42O7P2
For Research Use Only. Not Intended for Diagnostic or Therapeutic Use.
* Refer to Certificate of Analysis for lot specific data.
QUICK LINKS
Ordering Information
Description
Technical Information
Safety Information
SDS & Certificate of Analysis
SR 12813 is a PXR (pregnane X receptor) agonist (EC50 values are 200 and 700 nM for human and rabbit PXR respectively). SR 12813 activates the FXR (farnesoid X receptor) at muM concentrations. SR 12813 is an inhibitor of HMGCR.
SR 12813 (CAS 126411-39-0) References
- The nuclear receptors FXR and LXRalpha: potential targets for the development of drugs affecting lipid metabolism and neoplastic diseases. | Niesor, EJ., et al. 2001. Curr Pharm Des. 7: 231-59. PMID: 11254888
- Isolation of mutant cells lacking Insig-1 through selection with SR-12813, an agent that stimulates degradation of 3-hydroxy-3-methylglutaryl-coenzyme A reductase. | Sever, N., et al. 2004. J Biol Chem. 279: 43136-47. PMID: 15247248
- Mutations within the membrane domain of HMG-CoA reductase confer resistance to sterol-accelerated degradation. | Lee, PC., et al. 2007. J Lipid Res. 48: 318-27. PMID: 17090658
- Dehydroepiandrosterone induces human CYP2B6 through the constitutive androstane receptor. | Kohalmy, K., et al. 2007. Drug Metab Dispos. 35: 1495-501. PMID: 17591676
- Regulation of CYP3A4 and CYP2B6 expression by liver X receptor agonists. | Duniec-Dmuchowski, Z., et al. 2007. Biochem Pharmacol. 74: 1535-40. PMID: 17825266
- Construction and characterization of a fully active PXR/SRC-1 tethered protein with increased stability. | Wang, W., et al. 2008. Protein Eng Des Sel. 21: 425-33. PMID: 18456871
- Polycyclic aromatic hydrocarbons stimulate human CYP3A4 promoter activity via PXR. | Luckert, C., et al. 2013. Toxicol Lett. 222: 180-8. PMID: 23845848
- Forward genetic screening for regulators involved in cholesterol synthesis using validation-based insertional mutagenesis. | Jiang, W., et al. 2014. PLoS One. 9: e112632. PMID: 25426949
- Utility of an appropriate reporter assay: Heliotrine interferes with GAL4/upstream activation sequence-driven reporter gene systems. | Luckert, C., et al. 2015. Anal Biochem. 487: 45-8. PMID: 26212314
- Pregnane X receptors regulate CYP2C8 and P-glycoprotein to impact on the resistance of NSCLC cells to Taxol. | Chen, Y., et al. 2016. Cancer Med. 5: 3564-3571. PMID: 27878971
- The novel cholesterol-lowering drug SR-12813 inhibits cholesterol synthesis via an increased degradation of 3-hydroxy-3-methylglutaryl-coenzyme A reductase. | Berkhout, TA., et al. 1996. J Biol Chem. 271: 14376-82. PMID: 8662919
- Induction of cytochrome P4503A by the antiglucocorticoid mifepristone and a novel hypocholesterolaemic drug. | Williams, JA., et al. 1997. Drug Metab Dispos. 25: 757-61. PMID: 9193879
- SR-12813 lowers plasma cholesterol in beagle dogs by decreasing cholesterol biosynthesis. | Berkhout, TA., et al. 1997. Atherosclerosis. 133: 203-12. PMID: 9298680
Inhibitor of:
HMGCR.Activator of:
FXR, and PXR.Ordering Information
| Product Name | Catalog # | UNIT | Price | Qty | FAVORITES | |
SR 12813, 10 mg | sc-204296 | 10 mg | $89.00 | |||
SR 12813, 50 mg | sc-204296A | 50 mg | $338.00 |