GKA50
Based on 1 Customer Validation
GKA50 is a potent glucokinase activator (EC50=33 nM at 5 mM glucose). GKA50 stimulates insulin release from mouse islets of Langerhans. GKA50 is a glucose-like activator of beta-cell metabolism in rodent and human islets and a Ca2+-dependent modulator of insulin secretion. GKA50 shows significant glucose lowering in high fat fed female rats.
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- Pureza: 99.84%
- No. CAS: 851884-87-2
- Fòrmula: C26H28N2O6
- Peso molecular:464.51
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Almacenamiento:Powder -20°C, 3 years ; In solvent -80°C, 6 months , -20°C, 1 month
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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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Actividad biológica
GKA50 (0.01-100 μM; 24 hours) enhances INS-1 cell proliferation with EC50values ranging from 1 to 2 μM[2].
GKA50 (1.2 μM+40 μM glucose; 2-4 days) treatment reduces apoptosis induced by chronic high glucose in INS-1 cells[2].
GKA50 activates human glucokinase enzymatic activity with an EC50 of 0.022 μM. GKA50 stimulates insulin secretion in the pancreatic insulinoma cell line, INS-1, with an EC50 of 0.065 μM. GKA50 reduces chronic-high-glucose-induced apoptosis via modulation of glucokinase and apoptotic protein BAD[2].
MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.
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Cell Line:INS-1 cells (starved overnight with 3 μM glucose)
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Concentration:0.01-100 μM
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Incubation Time:24 hours
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Result:Stimulated cell proliferation in a dose-dependent manner, with EC50 values ranging from 1 to 2 μM.
MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.
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Animal Model:High-fat-fed obese female Zucker (fa/fa) rats[1]
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Dosage:1, 3, 10, 30 mg/kg
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Administration:Oral administration
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Result:Significant percentage glucose lowering.
Chemical Information
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No. CAS 851884-87-2
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Appearance Solid
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Peso molecular 464.51
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Fòrmula C26H28N2O6
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Color White to off-white
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SMILES
O=C(C1=CC=C(NC(C2=CC(O[C@@H](C)CC3=CC=CC=C3)=CC(O[C@@H](C)COC)=C2)=O)N=C1)O
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Envío
Room temperature in continental US; may vary elsewhere.
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Almacenamiento
Powder -20°C 3 years In solvent -80°C 6 months -20°C 1 month
Solvente y solubilidad
DMSO : 46 mg/mL (99.03 mM; Need ultrasonic and warming; 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)
Pureza y Documentación
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Ficha de datos (276 KB)
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SDS (392 KB)
- English - EN (392 KB)
- Français - FR (392 KB)
- Deutsch - DE (392 KB)
- Norwegian - NO (392 KB)
- Español - ES (392 KB)
- Swedish - SV (392 KB)
- Italian - IT (392 KB)
- Korean - KR (392 KB)
- Portuguese - PT (392 KB)
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Instrucciones de manejo (2659 KB)
Referencias
[1]. Coope GJ, et al. Predictive blood glucose lowering efficacy by Glucokinase activators in high fat fed female Zucker rats. Br J Pharmacol. 2006 Oct;149(3):328-35. [Content Brief]
[2]. McGlasson L, et al. The glucokinase activator GKA50 causes an increase in cell volume and activation of volume-regulated anion channels in rat pancreatic β-cells. Mol Cell Endocrinol. 2011 Aug 6;342(1-2):48-53. [Content Brief]
[3]. Johnson D, et al. Glucose-dependent modulation of insulin secretion and intracellular calcium ions by GKA50, a glucokinase activator. Diabetes. 2007;56(6):1694-1702. [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 |
|---|---|---|---|---|---|
| DMSO | 1 mM | 2.1528 mL | 10.7640 mL | 21.5281 mL | 53.8202 mL |
| 5 mM | 0.4306 mL | 2.1528 mL | 4.3056 mL | 10.7640 mL | |
| 10 mM | 0.2153 mL | 1.0764 mL | 2.1528 mL | 5.3820 mL | |
| 15 mM | 0.1435 mL | 0.7176 mL | 1.4352 mL | 3.5880 mL | |
| 20 mM | 0.1076 mL | 0.5382 mL | 1.0764 mL | 2.6910 mL | |
| 25 mM | 0.0861 mL | 0.4306 mL | 0.8611 mL | 2.1528 mL | |
| 30 mM | 0.0718 mL | 0.3588 mL | 0.7176 mL | 1.7940 mL | |
| 40 mM | 0.0538 mL | 0.2691 mL | 0.5382 mL | 1.3455 mL | |
| 50 mM | 0.0431 mL | 0.2153 mL | 0.4306 mL | 1.0764 mL | |
| 60 mM | 0.0359 mL | 0.1794 mL | 0.3588 mL | 0.8970 mL | |
| 80 mM | 0.0269 mL | 0.1346 mL | 0.2691 mL | 0.6728 mL |
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