MK-0941 free base
MK-0941 free base is an orally active 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 free base exhibits strong glucose-lowering activity and is a potential therapeutic agent for treatment of type 2 diabetes.
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- CAS. Nr.: 752240-01-0
- Formel: C21H24N4O6S
- Molecular Weight:460.50
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Speicherung:
Please store the product under the recommended conditions in the Certificate of Analysis.
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Biologische Aktivität
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Chemical Information
- Reinheit & Dokumentation
- Verweise
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Help & FAQs
Biologische Aktivität
MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.
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Animal Model:Male db/db and db/+ (lean) mice (9-10 weeks of age, weighing 43-45 g) [1].
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Dosage:3 or 10 mg/kg.
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Administration:Oral gavage, single dose.
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Result:Resulted in significant reduction in blood glucose. These two doses lowered blood glucose similarly at 1 h after dosing, suggesting that saturation of effect was approached.
| NCT Number | Sponsor | Condition | Start Date |
Phase
|
|---|---|---|---|---|
| NCT01329991 | Plexxikon| | 2011-05 | PHASE1 |
Chemical Information
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CAS. Nr. 752240-01-0
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Molecular Weight 460.50
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Formel C21H24N4O6S
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SMILES
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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Versand
Room temperature in continental US; may vary elsewhere.
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Speicherung
Please store the product under the recommended conditions in the Certificate of Analysis.
Reinheit & Dokumentation
Verweise
[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 GE, et al. Effects of MK-0941, a novel glucokinase activator, on glycemic control in insulin-treated patients with type 2 diabetes. Diabetes Care. 2011 Dec;34(12):2560-6. [Content Brief]
Calculators
Konzentration (Stammlösung) × Volumen (Stammlösung) = Konzentration (Ziellösung) × Volumen (Ziellösung)
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