AVE5688
Based on 1 Customer Validation
AVE5688 is an inhibitor of glycogen phosphorylase (GP), with IC50s of 430 nM and 915 nM and Kds of 170 nM and 530 nM for rabbit muscle glycogen phosphorylase (rmGPb and rmGPa, respectively); AVE5688 can be used for the research of type 2 diabetes.
Nos produits utilisent uniquement pour la recherche. Nous ne vendons pas aux patients.
- Pureté: 98.79%
- CAS No.: 613260-13-2
- Formule: C16H8ClF5N2O5
- Masse moléculaire:438.69
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Stockage: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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Activité biologique
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Chemical Information
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Solvant et solubilité
- Protocole
- Pureté et documentation
- Références
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Help & FAQs
Activité biologique
IC50: 430 nM (rmGPb), 915 nM (rmGPa)[1]
Kd: 170 nM (rmGPb), 530 nM (rmGPa)[1]
AVE5688 is an inhibitor of glycogen phosphorylase (GP), with IC50s of 430 nM and 915 nM and Kds of 170 nM and 530 nM for rabbit muscle glycogen phosphorylase (rmGPb and rmGPa, respectively)[1].
MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.
Chemical Information
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CAS No. 613260-13-2
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Appearance Solid
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Masse moléculaire 438.69
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Formule C16H8ClF5N2O5
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Color White to off-white
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SMILES
O=C(O)C1=CC=C(NC(NC(C2=CC(F)=C(F)C=C2Cl)=O)=O)C(OC(F)(F)F)=C1
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Livraison
Room temperature in continental US; may vary elsewhere.
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Stockage
Powder -20°C 3 years 4°C 2 years In solvent -80°C 6 months -20°C 1 month
Solvant et solubilité
DMSO : 100 mg/mL (227.95 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)
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.
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.
Protocole
Glycogen phosphorylase activity is measured in the physiological direction of glycogen breakdown. rmGP is used for the kinetic characterization of the inhibitors (AVE5688). To routinely check the phosphorylation grade of enzyme batches, activity is measured in the direction of glycogen synthesis; the phosphorylation grade is estimated from the ratio of the activity in the presence of 0.5 mM caffeine to the activity in the presence of 2 mM AMP[1].
MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.
Pureté et documentation
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Fiche technique (272 KB)
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SDS (255 KB)
- English - EN (255 KB)
- Français - FR (255 KB)
- Deutsch - DE (255 KB)
- Norwegian - NO (255 KB)
- Español - ES (255 KB)
- Swedish - SV (255 KB)
- Italian - IT (255 KB)
- Korean - KR (255 KB)
- Portuguese - PT (255 KB)
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Instruction de manipulation (2659 KB)
Références
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 | 2.2795 mL | 11.3976 mL | 22.7951 mL | 56.9878 mL |
| 5 mM | 0.4559 mL | 2.2795 mL | 4.5590 mL | 11.3976 mL | |
| 10 mM | 0.2280 mL | 1.1398 mL | 2.2795 mL | 5.6988 mL | |
| 15 mM | 0.1520 mL | 0.7598 mL | 1.5197 mL | 3.7992 mL | |
| 20 mM | 0.1140 mL | 0.5699 mL | 1.1398 mL | 2.8494 mL | |
| 25 mM | 0.0912 mL | 0.4559 mL | 0.9118 mL | 2.2795 mL | |
| 30 mM | 0.0760 mL | 0.3799 mL | 0.7598 mL | 1.8996 mL | |
| 40 mM | 0.0570 mL | 0.2849 mL | 0.5699 mL | 1.4247 mL | |
| 50 mM | 0.0456 mL | 0.2280 mL | 0.4559 mL | 1.1398 mL | |
| 60 mM | 0.0380 mL | 0.1900 mL | 0.3799 mL | 0.9498 mL | |
| 80 mM | 0.0285 mL | 0.1425 mL | 0.2849 mL | 0.7123 mL | |
| 100 mM | 0.0228 mL | 0.1140 mL | 0.2280 mL | 0.5699 mL |
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