SR12813
Based on 7 publication(s) in Google Scholar
SR12813 (GW 485801) is an inhibitor of 3-hydroxy-3-methylglutaryl-coenzyme A (HMG-CoA) reductase, with an IC50 value of 0.85 μM. SR12813 is also an efficient agonist of human pregnane X receptor (hPXR). SR12813 can strongly bind to hPXR but not to mouse PXR (mPXR).
Nur für Forschungszwecke. Wir verkaufen nicht an Patienten.
- Reinheit: 99.84%
- CAS. Nr.: 126411-39-0
- Formel: C24H42O7P2
- Molecular Weight:504.53
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Speicherung:Powder -20°C, 3 years , 4°C, 2 years ; In solvent -80°C, 2 years , -20°C, 1 year
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Biologische Aktivität
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Chemical Information
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Lösungsmittel & Löslichkeit
- Protokoll
- Reinheit & Dokumentation
- Verweise
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Publications Citing Use of MedChemExpress (MCE) SR12813
More- Nat Commun. 2025 Nov 6;16(1):9805. [Abstract]
- J Med Chem. 2022 Feb 10;65(3):2571-2592. [Abstract]
- Eur J Med Chem. 2024 Apr 5:269:116344. [Abstract]
- Liver Int. 2025 Feb;45(2):e16246. [Abstract]
- J Pharm Biomed Anal. 2026 Jan 15:268:117219. [Abstract]
- Biochem Biophys Res Commun. 2024 May 28:710:149841. [Abstract]
- Biochem Biophys Res Commun. 2023 Oct 15:677:13-19. [Abstract]
Biologische Aktivität
IC50: 0.85 μM (HMG-CoA Reductase)
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Cell Line
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Type | Value | Description | References |
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| HEK293 | EC50 |
80 nM
Compound: SR12813
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Agonist activity at human pregnane X receptor expressed in HEK293 cells by luciferase reporter gene assay
Agonist activity at human pregnane X receptor expressed in HEK293 cells by luciferase reporter gene assay
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[PMID: 25305688] |
| LS180 | IC50 |
>30 μM
Compound: 6a
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Cytotoxicity against human LS180 cells assessed as reduction in cell viability after 24 hrs by MTT assay
Cytotoxicity against human LS180 cells assessed as reduction in cell viability after 24 hrs by MTT assay
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10.1039/C6MD00300A |
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].
MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.
Chemical Information
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CAS. Nr. 126411-39-0
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Appearance Solid
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Molecular Weight 504.53
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Formel C24H42O7P2
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Color White to off-white
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SMILES
OC1=C(C(C)(C)C)C=C(/C=C(P(OCC)(OCC)=O)/P(OCC)(OCC)=O)C=C1C(C)(C)C
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Synonyms
GW 485801
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Versand
Room temperature in continental US; may vary elsewhere.
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Speicherung
Powder -20°C 3 years 4°C 2 years In solvent -80°C 2 years -20°C 1 year
Publications (7)
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Journal Impact Factor
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Most Recent
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Nat Commun
PROTAC repurposing uncovers a noncanonical binding surface that mediates chemical degradation of nuclear receptors. [Abstract]2025 Nov 6;16(1):9805. PMID: 41198675 -
J Med Chem
Design, Synthesis, and Biological Evaluation of Triazolone Derivatives as Potent PPARα/δ Dual Agonists for the Treatment of Nonalcoholic Steatohepatitis. [Abstract]2022 Feb 10;65(3):2571-2592. PMID: 35060744 -
Eur J Med Chem
Design, synthesis, and biological evaluation of piperazine derivatives as pan-PPARs agonists for the treatment of liver fibrosis. [Abstract]2024 Apr 5:269:116344. PMID: 38522113 -
Liver Int
miR-18a-5p/PXR/SREBP2 Was Involved in MAFLD Associated With Methyl Tert-Butyl Ether Among Petrol Station Workers. [Abstract]2025 Feb;45(2):e16246. PMID: 39821525 -
J Pharm Biomed Anal
A novel screening method for cytochrome P450 induction in early drug discovery using advanced biomimetic chromatography targeting the pregnane X receptor. [Abstract]2026 Jan 15:268:117219. PMID: 41205497 -
Biochem Biophys Res Commun
Overcoming statin resistance in prostate cancer cells by targeting the 3-hydroxy-3-methylglutaryl-CoA-reductase. [Abstract]2024 May 28:710:149841. PMID: 38588613 -
Biochem Biophys Res Commun
HMG-CoA reductase degrader, SR-12813, counteracts statin-induced upregulation of HMG-CoA reductase and augments the anticancer effect of atorvastatin. [Abstract]2023 Oct 15:677:13-19. PMID: 37541087
Lösungsmittel & Löslichkeit
DMSO : 50 mg/mL (99.10 mM; Need ultrasonic; Hygroscopic DMSO has a significant impact on the solubility of product, please use newly opened DMSO)
Please refer to the solubility information to select the appropriate solvent. Once prepared, please aliquot and store the solution to prevent product inactivation from repeated freeze-thaw cycles.
Storage method and period of stock solution: -80°C, 2 years; -20°C, 1 year. When stored at -80°C, please use it within 2 years. When stored at -20°C, please use it within 1 year.
Please refer to the solubility information to select the appropriate solvent. Once prepared, please aliquot and store the solution to prevent product inactivation from repeated freeze-thaw cycles.
Storage method and period of stock solution: -80°C, 2 years; -20°C, 1 year. When stored at -80°C, please use it within 2 years. When stored at -20°C, please use it within 1 year.
Konzentration (Stammlösung) × Volumen (Stammlösung) = Konzentration (Ziellösung) × Volumen (Ziellösung)
Select the appropriate dissolution method based on your experimental animal and administration route.
- For the following dissolution methods, please ensure to first prepare a clear stock solution using an In Vitro approach and then sequentially add co-solvents:
- To ensure reliable experimental results, the clarified stock solution can be appropriately stored based on storage conditions. As for the working solution for In Vivo experiments, it is recommended to prepare freshly and use it on the same day.
- The percentages shown for the solvents indicate their volumetric ratio in the final prepared solution. If precipitation or phase separation occurs during preparation, heat and/or sonication can be used to aid dissolution.
Add each solvent one by one: 10% DMSO 40% PEG300 5% Tween-80 45% Saline
Solubility: ≥ 2.5 mg/mL (4.96 mM); Clear solution
This protocol yields a clear solution of ≥ 2.5 mg/mL (saturation unknown).
Taking 1 mL working solution as an example, add 100 μL DMSO stock solution (25.0 mg/mL) to 400 μL PEG300, and mix evenly; then add 50 μL Tween-80 and mix evenly; then add 450 μL Saline to adjust the volume to 1 mL.
Preparation of Saline: Dissolve 0.9 g sodium chloride in ddH₂O and dilute to 100 mL to obtain a clear Saline solution.
Add each solvent one by one: 10% DMSO 90% (20% SBE-β-CD in Saline)
Solubility: ≥ 2.5 mg/mL (4.96 mM); Clear solution
This protocol yields a clear solution of ≥ 2.5 mg/mL (saturation unknown).
Taking 1 mL working solution as an example, add 100 μL DMSO stock solution (25.0 mg/mL) to 900 μL 20% SBE-β-CD in Saline, and mix evenly.
Preparation of 20% SBE-β-CD in Saline (4°C, storage for one week): 2 g SBE-β-CD powder is dissolved in 10 mL Saline, completely dissolve until clear.
Please enter the basic information of animal experiments:
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Recommended: Prepare an additional quantity of animals to account for potential losses during experiments.
Please enter your animal formula composition:
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%DMSO +
Recommended: Keep the proportion of DMSO in working solution below 2% if your animal is weak.
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%+
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+%Tween-80 + +
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%Saline +
The co-solvents required include: DMSO, . All of co-solvents are available by MedChemExpress (MCE). , Tween 80. All of co-solvents are available by MedChemExpress (MCE).
Working solution concentration: 0.22 mg/mL
Method for preparing stock solution: mg drug dissolved in μL DMSO. Stock solution concentration: mg/mL.
1. Take μL DMSO stock solution;
2. Add μL .
μL , mix evenly;
3. Then add μL Tween 80, mix evenly;
4. Then add μL
Please ensure that the stock solution in the first step is dissolved to a clear state, and add co-solvents in sequence. You can use ultrasonic heating (ultrasonic cleaner, recommended frequency 20-40 kHz), vortexing, etc. to assist dissolution.
Protokoll
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.
MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.
Reinheit & Dokumentation
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Data Sheet (281 KB)
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SDS (393 KB)
- English - EN (393 KB)
- Français - FR (393 KB)
- Deutsch - DE (393 KB)
- Norwegian - NO (393 KB)
- Español - ES (393 KB)
- Swedish - SV (393 KB)
- Italian - IT (393 KB)
- Korean - KR (393 KB)
- Portuguese - PT (393 KB)
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Handling Instructions (2659 KB)
Verweise
[1]. Berkhout TA, 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. [Content Brief]
[2]. Wei Jiang, et al. Forward genetic screening for regulators involved in cholesterol synthesis using validation-based insertional mutagenesis. PLoS One. 2014 Nov 26;9(11):e112632. [Content Brief]
Complete Stock Solution Preparation Table
Please refer to the solubility information to select the appropriate solvent. Once prepared, please aliquot and store the solution to prevent product inactivation from repeated freeze-thaw cycles.
Storage method and period of stock solution: -80°C, 2 years; -20°C, 1 year. When stored at -80°C, please use it within 2 years. When stored at -20°C, please use it within 1 year.
| Optional Solvent | Concentration Solvent Mass | 1 mg | 5 mg | 10 mg | 25 mg |
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| DMSO | 1 mM | 1.9820 mL | 9.9102 mL | 19.8204 mL | 49.5511 mL |
| 5 mM | 0.3964 mL | 1.9820 mL | 3.9641 mL | 9.9102 mL | |
| 10 mM | 0.1982 mL | 0.9910 mL | 1.9820 mL | 4.9551 mL | |
| 15 mM | 0.1321 mL | 0.6607 mL | 1.3214 mL | 3.3034 mL | |
| 20 mM | 0.0991 mL | 0.4955 mL | 0.9910 mL | 2.4776 mL | |
| 25 mM | 0.0793 mL | 0.3964 mL | 0.7928 mL | 1.9820 mL | |
| 30 mM | 0.0661 mL | 0.3303 mL | 0.6607 mL | 1.6517 mL | |
| 40 mM | 0.0496 mL | 0.2478 mL | 0.4955 mL | 1.2388 mL | |
| 50 mM | 0.0396 mL | 0.1982 mL | 0.3964 mL | 0.9910 mL | |
| 60 mM | 0.0330 mL | 0.1652 mL | 0.3303 mL | 0.8259 mL | |
| 80 mM | 0.0248 mL | 0.1239 mL | 0.2478 mL | 0.6194 mL |
SR12813 Related Classifications
HY-100793 Related Classifications
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