MK-0941
Based on 1 Customer Validation
MK-0941 is a selective, orally active, and allosteric glucokinase activator with EC50s of 240 and 65 nM for recombinant human glucokinase in the presence of 2.5 and 10 mM glucose, respectively. MK-0941 activates hexokinase subtype IV. MK-0941 can increase insulin secretion and glucose uptake. MK-0941 can be studied in research for type 2 diabetes.
Para uso exclusivo en investigación. No vendemos a pacientes.
- Pureza: 99.38%
- No. CAS: 1137916-97-2
- Fòrmula: C22H28N4O9S2
- Peso molecular:556.61
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Almacenamiento:
4°C, sealed storage, away from moisture
* In solvent : -80°C, 6 months; -20°C, 1 month (sealed storage, away from moisture)
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
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Metabolism/Protease Compound Library
HY-L012
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Anti-diabetic Compound Library
HY-L040
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Glycolysis Compound Library
HY-L058
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Orally Active Compound Library
HY-L061
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Anti-Cancer Metabolism Compound Library
HY-L083
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Glucose Metabolism Compound Library
HY-L092
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Metabolic Enzyme Compound Library
HY-L146
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Highly Selective Activators Library
HY-L159
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Bioactive Compound Library Max
HY-L181
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MCE Bioactive Compound Library
HY-L001V
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HY-L001
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High-Throughput Bioactive Compound Library
HY-L205
Actividad biológica
EC50: 240 nM (Recombinant human glucokinase, 2.5 mM glucose), 65 nM (Recombinant human glucokinase, 10 mM glucose)[1]
MK-0941 (1 μM) decreases the enzyme’s S0.5 for glucose from 6.9 to 1.4 mM[1].
MK-0941 (0.1-10 μM, 1.5 h) increases insulin secretion of isolated hepatocytes, dependent on MK-0941 and glucose concentrations[1].
MK-0941 (0.1-30 μM, 3 h) increases the phosphorylation by 18-fold with 30 μM concentration in hepatocytes[1].
MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.
MK-0941 (2-60 mg/kg, p.o., twice daily for 14 d) retains the glucose-lowering efficacy in HFD mice[1].
MK-0941 (3-10 mg/kg, p.o., single dose) reduces blood glucose and increases total plasma cholesterol in the db/db diabetic HFD/STZ mice[1].
MK-0941 (0.3-3 mg/kg, p.o., single dose) significantly reduces the plasma glucose concentration in healthy dogs dose-dependently[1].
MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.
Chemical Information
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No. CAS 1137916-97-2
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Appearance Solid
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Peso molecular 556.61
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Fòrmula C22H28N4O9S2
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Color Light yellow to yellow
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SMILES
CS(=O)(O)=O.O=C(NC1=NN(C)C=C1)C2=CC(O[C@@H](C)CO)=CC(OC3=CC=C(S(=O)(CC)=O)N=C3)=C2
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Envío
Room temperature in continental US; may vary elsewhere.
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Almacenamiento
4°C, sealed storage, away from moisture
* In solvent : -80°C, 6 months; -20°C, 1 month (sealed storage, away from moisture)
Solvente y solubilidad
DMSO : 100 mg/mL (179.66 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 (sealed storage, away from moisture). 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 (sealed storage, away from moisture). 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.
Add each solvent one by one: 10% DMSO 40% PEG300 5% Tween-80 45% Saline
Solubility: ≥ 2.17 mg/mL (3.90 mM); Clear solution
This protocol yields a clear solution of ≥ 2.17 mg/mL (saturation unknown).
Taking 1 mL working solution as an example, add 100 μL DMSO stock solution (21.7 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: ≥ 2.17 mg/mL (3.90 mM); Clear solution
This protocol yields a clear solution of ≥ 2.17 mg/mL (saturation unknown).
Taking 1 mL working solution as an example, add 100 μL DMSO stock solution (21.7 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. * In solvent : -80°C, 6 months; -20°C, 1 month (sealed storage, away from moisture)
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 (276 KB)
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SDS (252 KB)
- English - EN (252 KB)
- Français - FR (252 KB)
- Deutsch - DE (252 KB)
- Norwegian - NO (252 KB)
- Español - ES (252 KB)
- Swedish - SV (252 KB)
- Italian - IT (252 KB)
- Korean - KR (252 KB)
- Portuguese - PT (252 KB)
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Instrucciones de manejo (2659 KB)
Referencias
[1]. Eiki J, et al. Pharmacokinetic and pharmacodynamic properties of the glucokinase activator MK-0941 in rodent models of type 2 diabetes and healthy dogs. Mol Pharmacol. 2011 Dec;80(6):1156-65. [Content Brief]
[2]. Meininger, G. E., et al., (2011). Effects of MK-0941, a novel glucokinase activator, on glycemic control in insulin-treated patients with type 2 diabetes. Diabetes care, 34(12), 2560–2566. [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 (sealed storage, away from moisture). 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 | 1.7966 mL | 8.9830 mL | 17.9659 mL | 44.9148 mL |
| 5 mM | 0.3593 mL | 1.7966 mL | 3.5932 mL | 8.9830 mL | |
| 10 mM | 0.1797 mL | 0.8983 mL | 1.7966 mL | 4.4915 mL | |
| 15 mM | 0.1198 mL | 0.5989 mL | 1.1977 mL | 2.9943 mL | |
| 20 mM | 0.0898 mL | 0.4491 mL | 0.8983 mL | 2.2457 mL | |
| 25 mM | 0.0719 mL | 0.3593 mL | 0.7186 mL | 1.7966 mL | |
| 30 mM | 0.0599 mL | 0.2994 mL | 0.5989 mL | 1.4972 mL | |
| 40 mM | 0.0449 mL | 0.2246 mL | 0.4491 mL | 1.1229 mL | |
| 50 mM | 0.0359 mL | 0.1797 mL | 0.3593 mL | 0.8983 mL | |
| 60 mM | 0.0299 mL | 0.1497 mL | 0.2994 mL | 0.7486 mL | |
| 80 mM | 0.0225 mL | 0.1123 mL | 0.2246 mL | 0.5614 mL | |
| 100 mM | 0.0180 mL | 0.0898 mL | 0.1797 mL | 0.4491 mL |
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