SR-12813

BML-GR242

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PXR activator

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.

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Product Details

Alternative Name	Tetraethyl 2-(3,5-Di-t-butyl-4-hydroxyphenyl)ethenyl-1,1-bisphosphonate
Appearance	White solid.
CAS	126411-39-0
Couple Target	PXR
Couple Type	Activator, Ligand
Formula	C₂₄H₄₂O₇P2
MW	504.5
Purity	≥98% (TLC)
Solubility	Soluble in DMSO (25mg/ml).
Source	Synthetic.

Handling & Storage

Use/Stability	As indicated on product label or CoA when stored as recommended.
Long Term Storage	Ambient
Shipping	Ambient Temperature

Regulatory Status	RUO – Research Use Only

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
Development of BODIPY FL vindoline as a novel and high-affinity pregnane X receptor fluorescent probe: Lin, W., Liu, J., et al.; Bioconjug. Chem. 25, 1664 (2014), Abstract
Human pregnane X receptor agonism by Ginkgo biloba extract: assessment of the role of individual ginkgolides: Lau, A. J., Yang, G., et al.; J. Pharmacol. Exp. Ther. 335, 771 (2010), 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
SR-12813 lowers plasma cholesterol in beagle dogs by decreasing cholesterol biosynthesis: T. A. Berkhout, et al.; Atherosclerosis 133, 203 (1997), 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
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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SR-12813

BML-GR242

Product Details

Handling & Storage

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