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MK-0941 

Cat. No. M27831
MK-0941  Structure
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Biological Activity

MK-0941 is a potent, 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 has potential in the treatment of type 2 diabetes.

Chemical Information
Molecular Weight 556.61
Formula C22H28N4O9S2
CAS Number 1137916-97-2
Form Solid
Solubility (25°C) DMSO 260 mg/mL (ultrasonic)
Storage 4°C, dry, sealed
Conversion of different model animals based on BSA (PMID: 27057123)
Species Mouse Rat Rabbit Guinea pig Hamster Dog
Weight (kg) 0.02 0.15 1.8 0.4 0.08 10
Body Surface Area (m2) 0.007 0.025 0.15 0.05 0.02 0.5
Km factor 3 6 12 8 5 20
Animal A (mg/kg) = Animal B (mg/kg) multiplied by  Animal B Km
Animal A Km

For example, to modify the dose of Compound A used for a mouse (20 mg/kg) to a dose based on the BSA for a rat, multiply 20 mg/kg by the Km factor for a mouse and then divide by the Km factor for a rat. This calculation results in a rat equivalent dose for Compound A of 10 mg/kg.

References

[1] Yoshinori Tsumura, et al. PLoS One. Disruptions in hepatic glucose metabolism are involved in the diminished efficacy after chronic treatment with glucokinase activator

[2] Filippos Kesisoglou, et al. AAPS J. Comparison of Deconvolution-Based and Absorption Modeling IVIVC for Extended Release Formulations of a BCS III Drυg Development Candidate

[3] Filippos Kesisoglou, et al. J Pharm Sci. Suitability of a minipig model in assessing clinical bioperformance of matrix and multiparticulate extended-release formulations for a BCS class III Drυg development candidate

[4] Gary E Meininger, et al. Diabetes Care. Effects of MK-0941, a novel glucokinase activator, on glycemic control in insulin-treated patients with type 2 diabetes

[5] Jun-ichi Eiki, et al. Mol Pharmacol. Pharmacokinetic and pharmacodynamic properties of the glucokinase activator MK-0941 in rodent models of type 2 diabetes and healthy dogs

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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.

  Catalog
Abmole Inhibitor Catalog




Keywords: MK-0941  supplier, Glucokinase (GK), inhibitors, activators


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