E1231
Based on 1 publication(s) in Google Scholar
E1231 is an orally active activator of Sirtuin 1 (SIRT1) (EC50=0.83 μM), to modulate cholesterol and lipid metabolism. E1231 interactes with SIRT1 (KD=9.61 μM) and deacetylated liver X receptor-alpha (LXRα), and increases ATP-binding cassette transporter A1 (ABCA1) expression. E1231 also reduces atherosclerotic plaque development in ApoE-/- mice model. E1231 can be used for research in cholesterol and lipid disorder-related diseases.
Nur für Forschungszwecke. Wir verkaufen nicht an Patienten.
- Reinheit: 98.46%
- CAS. Nr.: 1031195-19-3
- Formel: C21H21N3O3
- Molecular Weight:363.41
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Speicherung:Powder -20°C, 3 years , 4°C, 2 years ; In solvent -80°C, 6 months , -20°C, 1 month
To place orders, for customer services and technical support, please contact: MedChemExpress USA
Tel: 609-228-6898 E-mail: [email protected] [email protected]
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Biologische Aktivität
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Chemical Information
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Publications Citing Use of MedChemExpress (MCE) E1231
More
Biologische Aktivität
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SIRT1 0.83 μM (EC50) |
E1231 (0.1-10 μM; 18 h) promotes cholesterol efflux and inhibits lipid accumulation in RAW 264.7 cells[1].
E1231 (10 μM; 6 h) significantly increases deacetylation of Doxo-induced p53 in HepG2 cells[1].
MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.
E1231 (25, 50, and 100 mg/kg, in 0.5% CMC-Na; po; once daily for 12 weeks) reduces atherosclerosis development, without hepatotoxicity ornephrotoxicity in ApoE-/- mice fed with atherogenic diet[1].
MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.
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Animal Model:HFD-diet Golden hamsters (80-90 g)[1]
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Dosage:40 mg/kg
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Administration:PO; once daily for 7 days
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Result:Increased SIRT1 protein expression but not SIRT3, SIRT6, or SIRT7. And reduced liver and serum cholesterol in hamsters.
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Animal Model:Atherogenic diet ApoE-/- mice[1]
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Dosage:25, 50, and 100 mg/kg
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Administration:PO; once daily for 12 weeks
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Result:Modulated plaque composition, immunofluorescence staining. And reduced CD68 positive areas while increasing ABCA1 expression in the aortic sinus.
Chemical Information
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CAS. Nr. 1031195-19-3
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Appearance Solid
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Molecular Weight 363.41
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Formel C21H21N3O3
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Color Off-white to light brown
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SMILES
CC(N1CCN(C(C2=CC(C3=CC=C(C)O3)=NC4=CC=CC=C24)=O)CC1)=O
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Synonyms
1-{4-[2-(5-Methylfuran-2-yl)quinoline-4-carbonyl]piperazin-1-yl}ethan-1-one
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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 6 months -20°C 1 month
Publications (1)
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Journal Impact Factor
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Most Recent
Lösungsmittel & Löslichkeit
DMSO : 100 mg/mL (275.17 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, 6 months; -20°C, 1 month. When stored at -80°C, please use it within 6 months. When stored at -20°C, please use it within 1 month.
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, 6 months; -20°C, 1 month. When stored at -80°C, please use it within 6 months. When stored at -20°C, please use it within 1 month.
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 (6.88 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 (6.88 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.
Reinheit & Dokumentation
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Data Sheet (291 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
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, 6 months; -20°C, 1 month. When stored at -80°C, please use it within 6 months. When stored at -20°C, please use it within 1 month.
| Optional Solvent | Concentration Solvent Mass | 1 mg | 5 mg | 10 mg | 25 mg |
|---|---|---|---|---|---|
| DMSO | 1 mM | 2.7517 mL | 13.7586 mL | 27.5171 mL | 68.7928 mL |
| 5 mM | 0.5503 mL | 2.7517 mL | 5.5034 mL | 13.7586 mL | |
| 10 mM | 0.2752 mL | 1.3759 mL | 2.7517 mL | 6.8793 mL | |
| 15 mM | 0.1834 mL | 0.9172 mL | 1.8345 mL | 4.5862 mL | |
| 20 mM | 0.1376 mL | 0.6879 mL | 1.3759 mL | 3.4396 mL | |
| 25 mM | 0.1101 mL | 0.5503 mL | 1.1007 mL | 2.7517 mL | |
| 30 mM | 0.0917 mL | 0.4586 mL | 0.9172 mL | 2.2931 mL | |
| 40 mM | 0.0688 mL | 0.3440 mL | 0.6879 mL | 1.7198 mL | |
| 50 mM | 0.0550 mL | 0.2752 mL | 0.5503 mL | 1.3759 mL | |
| 60 mM | 0.0459 mL | 0.2293 mL | 0.4586 mL | 1.1465 mL | |
| 80 mM | 0.0344 mL | 0.1720 mL | 0.3440 mL | 0.8599 mL | |
| 100 mM | 0.0275 mL | 0.1376 mL | 0.2752 mL | 0.6879 mL |
E1231 Related Classifications
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