
SR 12813 NEW
Price | $5 | $4 | $2 |
Package | 1kg | 10kg | 100kg |
Min. Order: | 1kg |
Supply Ability: | 100kg |
Update Time: | 2025-06-17 |
Product Details
Product Name: SR 12813 | CAS No.: 126411-39-0 |
Min. Order: 1kg | Purity: 99% |
Supply Ability: 100kg | Release date: 2025/06/17 |
Lead time: in stock | Packaging: bag/bottle/drum//IBC, as request |
Delivery: By sea, by air, by express | Origin: Manufacturer |
Name: Tina |
PRODUCT INFORMATION
Name | sr12813 |
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Synonym | More Synonyms |
Description | SR12813 is an inhibitor of 3-hydroxy-3-methylglutaryl-coenzyme A (HMG-CoA) reductase, with an IC50 value of 0.85 μM. |
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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 |
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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℃ |
Personal Protective Equipment | Eyeshields;Gloves;type N95 (US);type P1 (EN143) respirator filter |
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RIDADR | NONH for all modes of transport |
Dehydroepiandrosterone induces human CYP2B6 through the constitutive androstane receptor. Drug Metab. Dispos. 35 , 1495-501, (2007) Dehydroepiandrosterone (DHEA), the major precursor of androgens and estrogens, has several beneficial effects on the immune system, on memory function, and in modulating the effects of diabetes, obesi... | |
Cyclin-dependent kinase 2 negatively regulates human pregnane X receptor-mediated CYP3A4 gene expression in HepG2 liver carcinoma cells. J. Biol. Chem. 283 , 30650-7, (2008) The human pregnane X receptor (hPXR) regulates the expression of critical drug metabolism enzymes. One of such enzymes, cytochrome P450 3A4 (CYP3A4), plays critical roles in drug metabolism in hepatoc... | |
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. J. Biol. Chem. 279 , 43136-47, (2004) Insig-1 and Insig-2 are membrane proteins of the endoplasmic reticulum that regulate lipid metabolism by the following two actions: 1) sterol-induced binding to 3-hydroxy-3-methylglutaryl-coenzyme A r... |
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