[CAS NO. 1137916-97-2] MK-0941

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Catalog:	HY-19843
Brand:	MCE
CAS:	1137916-97-2

Overview

MDL	-
Molecular Weight	556.61
Molecular Formula	C22H28N4O9S2
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

For research use only. We do not sell to patients.

Summary

MK-0941 is a potent, orally active and allosteric glucokinase activator, with EC ₅₀ s 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 ^[1] .

IC50 & Target

EC50: 240 nM (Recombinant human glucokinase, 2.5 mM glucose), 65 nM (Recombinant human glucokinase, 10 mM glucose) ^[1]

Clinical Trial

NCT Number	Sponsor	Condition	Start Date	Phase
NCT00767000	Merck Sharp & Dohme LLC	Diabetes Mellitus, Type 2	October 2008	Phase 2
NCT01106287	Merck Sharp & Dohme LLC	Type 2 Diabetes	October 2009	Phase 1
NCT00511472	Merck Sharp & Dohme LLC	Type 2 Diabetes Mellitus	July 2007	Phase 1
NCT00754130	Merck Sharp & Dohme LLC	Diabetes Mellitus, Non-Insulin-Dependent	September 2008	Phase 1
NCT00824616	Merck Sharp & Dohme LLC	Type 2 Diabetes Mellitus	January 2009	Phase 2
NCT00873821	Merck Sharp & Dohme LLC	Diabetes Mellitus, Type 2	December 2008	Phase 1
NCT00511667	Merck Sharp & Dohme LLC	Type 2 Diabetes Mellitus	May 2007	Phase 1
NCT00567112	Merck Sharp & Dohme LLC	Type 2 Diabetes Mellitus	November 2007	Phase 1
NCT00830791	Merck Sharp & Dohme LLC	Type 2 Diabetes	January 2009	Phase 1
NCT00912002	Merck Sharp & Dohme LLC	Type 2 Diabetes	October 2008	Phase 1
NCT00792935	Merck Sharp & Dohme LLC	Type 2 Diabetes Mellitus	January 2009	Phase 2

Appearance

Solid

Shipping

Room temperature in continental US; may vary elsewhere.

Storage

4°C, sealed storage, away from moisture

* In solvent : -80°C, 6 months; -20°C, 1 month (sealed storage, away from moisture)

Solvent & Solubility

In Vitro:

DMSO : 260 mg/mL ( 467.11 mM ; Need ultrasonic)

Preparing
Stock Solutions

Concentration Solvent Mass	1 mg	5 mg	10 mg

1 mM	1.7966 mL	8.9830 mL	17.9659 mL
5 mM	0.3593 mL	1.7966 mL	3.5932 mL
10 mM	0.1797 mL	0.8983 mL	1.7966 mL

* Please refer to the solubility information to select the appropriate solvent.

In Vivo:

1.

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
2.

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
3.

Add each solvent one by one: 10% DMSO >> 90% corn oil

Solubility: ≥ 2.17 mg/mL (3.90 mM); Clear solution

* All of the co-solvents are available by MCE.

References

[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.

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