DC Chemicals Limited
China
Product Name: SR-12813（GW 485801）
Price: $250.0/100mg $500.0/250mg $1000.0/1g
Purity: 98.0%
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126411-39-0

126411-39-0 structure

126411-39-0 structure

Name: SR-12813
Chemical Name: sr12813
CAS Number: 126411-39-0
Molecular Formula: C₂₄H₄₂O₇P₂
Molecular Weight: 504.53400
Catalog: Signaling Pathways Metabolic Enzyme/Protease HMG-CoA Reductase (HMGCR)
Create Date: 2017-07-18 13:12:05
Modify Date: 2024-01-02 18:08:24
SR12813 is an inhibitor of 3-hydroxy-3-methylglutaryl-coenzyme A (HMG-CoA) reductase, with an IC50 value of 0.85 μM.

Name	sr12813
Synonyms	Tetraethyl 2-(3,5-di-tert-butyl-4-hydroxyphenyl)ethenyl-1,1-bisphosphonate SRL HTMT dimaleate 1ilh 4-[2,2-bis(diethoxyphosphoryl)ethenyl]-2,6-ditert-butylphenol BIDD:PXR0009 SR 12813

Description	SR12813 is an inhibitor of 3-hydroxy-3-methylglutaryl-coenzyme A (HMG-CoA) reductase, with an IC50 value of 0.85 μM.
Related Catalog	Signaling Pathways >> Metabolic Enzyme/Protease >> HMG-CoA Reductase (HMGCR) Research Areas >> Metabolic Disease
Target	IC50: 0.85 μM (HMG-CoA Reductase)
In Vitro	SR-12813 inhibits incorporation of tritiated water into cholesterol with an IC50 of 1.2 μM but has no effect on fatty acid synthesis. Furthermore, SR-12813 reduces cellular 3-hydroxy-3-methylglutaryl-coenzyme A (HMG-CoA) reductase activity with an IC50 of 0.85 μM[1]. Both 25-HC and SR-12813 can kill mammalian cells through blocking the synthesis of cholesterol, thereby they are ideal regents for lethal selection. SR-12813 kills HeLa cells at concentration range from 8 µM to 16 µM. SR-12813 kills wild type cells and mutant cells infected by Ad-Cre (SL-5+Cre), but the mutant SL-5 survives this condition. SR-12813 or 25-HC promotes the degradation of the 95-KDa full-length HMG-CoA reductase in wild type HeLa and SL-5 mutant cells[1].
Kinase Assay	Briefly, compounds are added to the cells in Me2SO (final concentration, 0.1%). After the experiment cells are lysed by the addition of 0.1 mL of 0.25% Brij 96, 0.1 M sucrose, 0.1 M KF, 50 mM KCl, 40 mM potassium dihydrophosphate, 30 mM EDTA, 5 mM dithiothreitol, pH 7.4 at room temperature. In some experiments KF is omitted to measure “total” HMG-CoA reductase activity. HMG-CoA reductase activity in the cell lysate is further determined.
References	[1]. Berkhout T, et al. 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. 1996 Jun 14;271(24):14376-82. [2]. Jiang W, et al. Forward genetic screening for regulators involved in cholesterol synthesis using validation-based insertional mutagenesis. PLoS One. 2014 Nov 26;9(11):e112632.

Density	1.117g/cm3
Boiling Point	552.6ºC at 760mmHg
Molecular Formula	C₂₄H₄₂O₇P₂
Molecular Weight	504.53400
Flash Point	288ºC
Exact Mass	504.24100
PSA	110.91000
LogP	7.81780
Vapour Pressure	8.02E-13mmHg at 25°C
Index of Refraction	1.504
Storage condition	-20℃

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