[CAS NO. 126411-39-0] SR-12813

Name: SR-12813
Brand: Arctom Scientific
SKU: SLK-S8302

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PRODUCTS SPECIFICATIONS [126411-39-0]

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Catalog

SLK-S8302

Brand

Selleck

CAS

126411-39-0

DESCRIPTION [126411-39-0]

Overview

MDL	MFCD00888473
Molecular Weight	504.53
Molecular Formula	C24H42O7P2
SMILES	P(C(P(OCC)(OCC)=O)=CC1=CC(C(C)(C)C)=C(O)C(C(C)(C)C)=C1)(OCC)(OCC)=O

For research use only.

Storage

3 years,-20°C,powder
1 years,-80°C,in solvent

Shipping

Room temperature shipping(Stability testing shows this product can be shipped without any cooling measures.)

Preparing Stock Solutions

Concentration Volume Mass	1 mg	5 mg	10 mg
1 mM	1.9820 mL	9.9102 mL	19.8204 mL
5 mM	0.3964 mL	1.9820 mL	3.9641 mL
10 mM	0.1982 mL	0.9910 mL	1.9820 mL
50 mM	0.0396 mL	0.1982 mL	0.3964 mL

Description

SR-12813 is a agonist and 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. 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.

In vivo

The bisphosphonate ester SR12813 lowers cholesterol levels in a range of species including rats, dogs and primates.

References

[1] Jones SA, et al. Mol Endocrinol. 2000, 14(1):27-39.
[2] Berkhout TA, et al. J Biol Chem. 1996, 271(24):14376-82.
[3] Berkhout TA, et al. Atherosclerosis. 1997, 133(2):203-12.

Synonyms

Phosphonic acid, P,P′-[[3,5-bis(1,1-dimethylethyl)-4-hydroxyphenyl]ethenylidene]bis-, P,P,P′,P′-tetraethyl ester

Phosphonic acid, [[3,5-bis(1,1-dimethylethyl)-4-hydroxyphenyl]ethenylidene]bis-, tetraethyl ester

P,P,P′,P′-Tetraethyl P,P′-[[3,5-bis(1,1-dimethylethyl)-4-hydroxyphenyl]ethenylidene]bis[phosphonate]

SR 12813

GW 485801