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SR-12813

PXR activator
 
BML-GR242-0010 10 mg 108.00 USD
 
BML-GR242-0050 50 mg 419.00 USD
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Potent and selective PXR agonist. (EC50=200 nM for human PXR). A weak activator of rat and mouse PXR. Inhibits cholesterol biosynthesis in a number of species.

Product Details

Alternative Name:Tetraethyl 2-(3,5-Di-t-butyl-4-hydroxyphenyl)ethenyl-1,1-bisphosphonate
 
Formula:C24H42O7P2
 
MW:504.5
 
Source:Synthetic.
 
CAS:126411-39-0
 
Purity:≥98% (TLC)
 
Appearance:White solid.
 
Solubility:Soluble in DMSO (25mg/ml).
 
Shipping:Ambient Temperature
 
Long Term Storage:Ambient
 
Regulatory Status:RUO - Research Use Only
 
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Product Literature References

Chemical regulators of epithelial plasticity reveal a nuclear receptor pathway controlling myofibroblast differentiation: J.M. Carthy, et al.; Sci. Rep. 6, 29868 (2016), Application(s): Screening of chemical compounds with HaCaT cells, Abstract; Full Text
3-Hydroxyflavone and structural analogues differentially activate pregnane X receptor: Implication for inflammatory bowel disease: A. Lau, et al. ; Pharmacol. Res. 100, 64 (2015), Application(s): Ligand Binding assay, Abstract;
The human nuclear xenobiotic receptor PXR: structural determinants of directed promiscuity: R. E. Watkins, et al.; Science 292, 2329 (2001), Abstract;
The pregnane X receptor: a promiscuous xenobiotic receptor that has diverged during evolution: S. A. Jones, et al.; Mol. Endocrinol. 14, 27 (2000), Abstract;
Induction of cytochrome P4503A by the antiglucocorticoid mifepristone and a novel hypocholesterolaemic drug: J. A. Williams, et al.; Drug Metab. Dispos. 25, 757 (1997), Abstract;
SR-12813 lowers plasma cholesterol in beagle dogs by decreasing cholesterol biosynthesis: T. A. Berkhout, et al.; Atherosclerosis 133, 203 (1997), Abstract;
The novel cholesterol-lowering drug SR-12813 inhibits cholesterol synthesis via an increased degradation of 3-hydroxy-3-methylglutaryl-coenzyme A reductase: T. A. Berkhout, et al.; J. Biol. Chem. 271, 14376 (1996), Abstract; Full Text

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