MDL-811
Based on 1 Customer Validation
MDL-811 is a selective allosteric activator of SIRT6 with an EC50 of 5.7 μM. MDL-811 possesses anti-inflammatory, antitumor, and neuroprotective activities. MDL-811 can be used for the research of diseases such as colorectal cancer and ischemic stroke.
Para uso exclusivo en investigación. No vendemos a pacientes.
- Pureza: 99.68%
- No. CAS: 2275619-98-0
- Fòrmula: C25H25BrCl2FN3O5S2
- Peso molecular:681.42
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Almacenamiento: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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Actividad biológica
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Chemical Information
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Solvente y solubilidad
- Pureza y Documentación
- Referencias
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Help & FAQs
Actividad biológica
Descripciòn
IC50 & Target
[1]|
SIRT6 5.7 μM (EC50) |
IL-1β |
In Vitro
MDL-811 (0-100 μM; 48 h) inhibits the proliferation of multiple colorectal cancer cell lines (IC50: 4.7-61.0 μM) and induces cell cycle arrest[1].
MDL-811 (0-20 μM; 0-48 h) decreases the levels of H3K9Ac, H3K18Ac and H3K56Ac in a dose-dependent manner in colorectal cancer cell lines[1].
MDL-811 (0.1-5 μM; 4 h) inhibits LPS (HY-D1056)-induced TNF-α protein release and reduces the expression of inflammatory factors such as TNF-α and IL-1β in RAW264.7 macrophages[2].
MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.
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Cell Line:HCT116 cells
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Concentration:0, 2.5, 5, 10 and 20 μM
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Incubation Time:48 h
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Result:Inhibited the levels of H3K9Ac, H3K18Ac and H3K56Ac.
In Vivo
MDL-811 (1-10 mg/kg; intravenous injection; 3 times) has improving effects in a mouse model of ischemic stroke[2].
MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.
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Animal Model:Male BALB/c nude mice aged 6 weeks old treated HCT116 cells[1]
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Dosage:20 and 30 mg/kg
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Administration:Intraperitoneal injection; every other day; 16 days
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Result:Significantly suppressed tumor growth in a dose-dependent manner, with reduced Ki67 staining and increased histone H3 deacetylation (H3K9Ac, H3K18Ac, H3K56Ac) in xenograft tissues.
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Animal Model:Male ICR mice aged 8-10 weeks old (22-26 g) treated transient middle cerebral artery occlusion[2]
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Dosage:1 and 10 mg/kg
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Administration:Intravenous injection; 3 times: 1, 24 and 48 h after the surgery respectively
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Result:Reduced infarct size and improved neurological deficits.
Reduced activated IBA1+CD16+ cells in the peri-infarct area.
Reduced pro-inflammatory gene expression (TNF-α, IL-1β) and enhanced anti-inflammatory gene expression (arginase1, CD206).
Chemical Information
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No. CAS 2275619-98-0
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Appearance Solid
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Peso molecular 681.42
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Fòrmula C25H25BrCl2FN3O5S2
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Color White to off-white
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SMILES
CC(C=C(C(Br)=C1)F)=C1NS(=O)(C2=C(C=C(C=C2)NS(=O)(C3=CC(Cl)=CC(Cl)=C3)=O)CN4[C@@H](COCC4)C)=O
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Envío
Room temperature in continental US; may vary elsewhere.
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Almacenamiento
Powder -20°C 3 years 4°C 2 years In solvent -80°C 6 months -20°C 1 month
Solvente y solubilidad
In Vitro:
DMSO : 100 mg/mL (146.75 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.
Concentration (start) × Volume (start) = Concentration (final) × Volume (final)
In Vivo:
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: ≥ 5 mg/mL (7.34 mM); Clear solution
This protocol yields a clear solution of ≥ 5 mg/mL (saturation unknown).
Taking 1 mL working solution as an example, add 100 μL DMSO stock solution (50.0 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.
In Vivo Dissolution Calculator
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.
Pureza y Documentación
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Ficha de datos (279 KB)
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SDS (251 KB)
- English - EN (251 KB)
- Français - FR (251 KB)
- Deutsch - DE (251 KB)
- Norwegian - NO (251 KB)
- Español - ES (251 KB)
- Swedish - SV (251 KB)
- Italian - IT (251 KB)
- Korean - KR (251 KB)
- Portuguese - PT (251 KB)
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Instrucciones de manejo (2659 KB)
Referencias
[1]. Jialin Shang, et al. Small-molecule activating SIRT6 elicits therapeutic effects and synergistically promotes anti-tumor activity of vitamin D3 in colorectal cancer. Theranostics. 2020 Apr 27;10(13):5845-5864. [Content Brief]
[2]. He T, et al. A novel SIRT6 activator ameliorates neuroinflammation and ischemic brain injury via EZH2/FOXC1 axis. Acta Pharm Sin B. 2021 Mar;11(3):708-726. [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, 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 |
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| DMSO | 1 mM | 1.4675 mL | 7.3376 mL | 14.6752 mL | 36.6881 mL |
| 5 mM | 0.2935 mL | 1.4675 mL | 2.9350 mL | 7.3376 mL | |
| 10 mM | 0.1468 mL | 0.7338 mL | 1.4675 mL | 3.6688 mL | |
| 15 mM | 0.0978 mL | 0.4892 mL | 0.9783 mL | 2.4459 mL | |
| 20 mM | 0.0734 mL | 0.3669 mL | 0.7338 mL | 1.8344 mL | |
| 25 mM | 0.0587 mL | 0.2935 mL | 0.5870 mL | 1.4675 mL | |
| 30 mM | 0.0489 mL | 0.2446 mL | 0.4892 mL | 1.2229 mL | |
| 40 mM | 0.0367 mL | 0.1834 mL | 0.3669 mL | 0.9172 mL | |
| 50 mM | 0.0294 mL | 0.1468 mL | 0.2935 mL | 0.7338 mL | |
| 60 mM | 0.0245 mL | 0.1223 mL | 0.2446 mL | 0.6115 mL | |
| 80 mM | 0.0183 mL | 0.0917 mL | 0.1834 mL | 0.4586 mL | |
| 100 mM | 0.0147 mL | 0.0734 mL | 0.1468 mL | 0.3669 mL |
MDL-811 Related Classifications
HY-156757 Related Classifications
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