Details
Stereochemistry | ABSOLUTE |
Molecular Formula | C21H24N4O6S.CH4O3S |
Molecular Weight | 556.609 |
Optical Activity | UNSPECIFIED |
Defined Stereocenters | 1 / 1 |
E/Z Centers | 0 |
Charge | 0 |
SHOW SMILES / InChI
SMILES
CS(O)(=O)=O.CCS(=O)(=O)C1=CC=C(OC2=CC(=CC(O[C@@H](C)CO)=C2)C(=O)NC3=NN(C)C=C3)C=N1
InChI
InChIKey=PIDNRTWDGDJKSQ-UQKRIMTDSA-N
InChI=1S/C21H24N4O6S.CH4O3S/c1-4-32(28,29)20-6-5-16(12-22-20)31-18-10-15(9-17(11-18)30-14(2)13-26)21(27)23-19-7-8-25(3)24-19;1-5(2,3)4/h5-12,14,26H,4,13H2,1-3H3,(H,23,24,27);1H3,(H,2,3,4)/t14-;/m0./s1
Molecular Formula | CH4O3S |
Molecular Weight | 96.106 |
Charge | 0 |
Count |
|
Stereochemistry | ACHIRAL |
Additional Stereochemistry | No |
Defined Stereocenters | 0 / 0 |
E/Z Centers | 0 |
Optical Activity | NONE |
Molecular Formula | C21H24N4O6S |
Molecular Weight | 460.503 |
Charge | 0 |
Count |
|
Stereochemistry | ABSOLUTE |
Additional Stereochemistry | No |
Defined Stereocenters | 1 / 1 |
E/Z Centers | 0 |
Optical Activity | UNSPECIFIED |
MK-0941 is selective, allosteric glucokinase activator (GKA) that activates glucokinase (hexokinase subtype IV) with greater selectivity than over different hexokinase isoforms. In chronic oral toxicity studies in animals with MK-0941, cataracts were observed in rats and dogs at drug exposures of 3 and 1.5 times, respectively, the maximum predicted human exposure based on doses planned for further clinical development. No cataracts were observed in either species at drug exposures equal to the maximum predicted human exposure. In patients receiving stable-dose insulin glargine, the glucokinase activator MK-0941 led to improvements in glycemic control that were not sustained. MK-0941 was associated with an increased incidence of hypoglycemia and elevations in triglycerides and blood pressure.
Approval Year
Targets
Primary Target | Pharmacology | Condition | Potency |
---|---|---|---|
Target ID: CHEMBL3820 Sources: https://www.ncbi.nlm.nih.gov/pubmed/21994424 |
240.0 nM [EC50] | ||
Target ID: CHEMBL3820 Sources: https://www.ncbi.nlm.nih.gov/pubmed/21937665 |
65.0 nM [EC50] |
PubMed
Title | Date | PubMed |
---|---|---|
Effects of MK-0941, a novel glucokinase activator, on glycemic control in insulin-treated patients with type 2 diabetes. | 2011 Dec |
|
Pharmacokinetic and pharmacodynamic properties of the glucokinase activator MK-0941 in rodent models of type 2 diabetes and healthy dogs. | 2011 Dec |
Patents
Sample Use Guides
In Vivo Use Guide
Sources: https://www.ncbi.nlm.nih.gov/pubmed/21994424
10, 20, 30, or 40 mg/day for 40-weeks
Route of Administration:
Oral
Substance Class |
Chemical
Created
by
admin
on
Edited
Fri Dec 15 16:25:46 UTC 2023
by
admin
on
Fri Dec 15 16:25:46 UTC 2023
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Record UNII |
83OY2D8970
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Record Status |
Validated (UNII)
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Record Version |
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100000175115
Created by
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83OY2D8970
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1137916-97-2
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25235800
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admin on Fri Dec 15 16:25:46 UTC 2023 , Edited by admin on Fri Dec 15 16:25:46 UTC 2023
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ACTIVE MOIETY |