Synonym
MK-0941; MK 0941; MK0941; MK-0941 mesylate.
IUPAC/Chemical Name
3-((6-(ethylsulfonyl)-3-pyridinyl)oxy)-5-((1S)-2-hydroxy-1-methylethoxy)-N-(1-methyl-1H-pyrazol-3-yl)benzamide mesylate
InChi Key
PIDNRTWDGDJKSQ-UQKRIMTDSA-N
InChi Code
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
SMILES Code
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.OS(=O)(C)=O
Purity
>98% (or refer to the Certificate of Analysis)
Shipping Condition
Shipped under ambient temperature as non-hazardous chemical. This product is stable enough for a few weeks during ordinary shipping and time spent in Customs.
Storage Condition
Dry, dark and at 0 - 4 C for short term (days to weeks) or -20 C for long term (months to years).
Solubility
Soluble in DMSO
Shelf Life
>2 years if stored properly
Drug Formulation
This drug may be formulated in DMSO
Stock Solution Storage
0 - 4 C for short term (days to weeks), or -20 C for long term (months).
HS Tariff Code
2934.99.9001
More Info
Related CAS#
1137916-97-2 (MK-0941 mesylate)
752240-01-0 (MK-0941 Free)
Biological target:
MK-0941 is a potent, orally active and allosteric glucokinase activator.
In vitro activity:
Incubated in vitro with recombinant human glucokinase, 1 μM MK-0941 lowered the S(0.5) of this enzyme for glucose from 6.9 to 1.4 mM and increased the maximum velocity of glucose phosphorylation by 1.5-fold. In 2.5 and 10 mM glucose, the EC(50) values for activation of GK by MK-0941 were 0.240 and 0.065 μM, respectively.
Reference: Mol Pharmacol. 2011 Dec;80(6):1156-65. https://pubmed.ncbi.nlm.nih.gov/21937665/
In vivo activity:
MK-0941 exhibited strong glucose-lowering activity in C57BL/6J mice maintained on a high-fat diet (HFD), db/db mice, HFD plus low-dose streptozotocin-treated mice, and nondiabetic dogs.
Reference: Mol Pharmacol. 2011 Dec;80(6):1156-65. https://pubmed.ncbi.nlm.nih.gov/21937665/
|
Solvent |
mg/mL |
mM |
comments |
| Solubility |
| DMF |
20.0 |
35.93 |
|
| DMSO |
140.0 |
251.52 |
|
| Ethanol |
5.0 |
8.98 |
|
Note: There can be variations in solubility for the same chemical from different vendors or different batches from the same vendor. The following factors can affect the solubility of the same chemical: solvent used for crystallization, residual solvent content, polymorphism, salt versus free form, degree of hydration, solvent temperature. Please use the solubility data as a reference only. Warming and sonication will facilitate dissolving. Still have questions? Please contact our Technical Support scientists.
Preparing Stock Solutions
The following data is based on the
product
molecular weight
556.61
Batch specific molecular weights may vary
from batch to batch
due to the degree of hydration, which will
affect the solvent
volumes required to prepare stock solutions.
| Concentration / Solvent Volume / Mass |
1 mg |
5 mg |
10 mg |
| 1 mM |
1.15 mL |
5.76 mL |
11.51 mL |
| 5 mM |
0.23 mL |
1.15 mL |
2.3 mL |
| 10 mM |
0.12 mL |
0.58 mL |
1.15 mL |
| 50 mM |
0.02 mL |
0.12 mL |
0.23 mL |
Formulation protocol:
Eiki J, Nagata Y, Futamura M, Sasaki-Yamamoto K, Iino T, Nishimura T, Chiba M, Ohyama S, Yoshida-Yoshimioto R, Fujii K, Hosaka H, Goto-Shimazaki H, Kadotani A, Ohe T, Lin S, Langdon RB, Berger JP. 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. doi: 10.1124/mol.111.074401. Epub 2011 Sep 21. PMID: 21937665.
In vitro protocol:
Eiki J, Nagata Y, Futamura M, Sasaki-Yamamoto K, Iino T, Nishimura T, Chiba M, Ohyama S, Yoshida-Yoshimioto R, Fujii K, Hosaka H, Goto-Shimazaki H, Kadotani A, Ohe T, Lin S, Langdon RB, Berger JP. 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. doi: 10.1124/mol.111.074401. Epub 2011 Sep 21. PMID: 21937665.
In vivo protocol:
Eiki J, Nagata Y, Futamura M, Sasaki-Yamamoto K, Iino T, Nishimura T, Chiba M, Ohyama S, Yoshida-Yoshimioto R, Fujii K, Hosaka H, Goto-Shimazaki H, Kadotani A, Ohe T, Lin S, Langdon RB, Berger JP. 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. doi: 10.1124/mol.111.074401. Epub 2011 Sep 21. PMID: 21937665.
1: Kesisoglou F, Xia B, Agrawal NG. Comparison of Deconvolution-Based and Absorption Modeling IVIVC for Extended Release Formulations of a BCS III Drug Development Candidate. AAPS J. 2015 Nov;17(6):1492-500. doi: 10.1208/s12248-015-9816-7. PubMed PMID: 26290380; PubMed Central PMCID: PMC4627461.
2: Kesisoglou F, Xie IH, Manser K, Wu Y, Hardy I, Fitzpatrick S. Suitability of a minipig model in assessing clinical bioperformance of matrix and multiparticulate extended-release formulations for a BCS class III Drug development candidate. J Pharm Sci. 2014 Feb;103(2):636-42. doi: 10.1002/jps.23837. PubMed PMID: 24382706.
3: Meininger GE, Scott R, Alba M, Shentu Y, Luo E, Amin H, Davies MJ, Kaufman KD, Goldstein BJ. 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. doi: 10.2337/dc11-1200. PubMed PMID: 21994424; PubMed Central PMCID: PMC3220852.
4: Eiki J, Nagata Y, Futamura M, Sasaki-Yamamoto K, Iino T, Nishimura T, Chiba M, Ohyama S, Yoshida-Yoshimioto R, Fujii K, Hosaka H, Goto-Shimazaki H, Kadotani A, Ohe T, Lin S, Langdon RB, Berger JP. 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. doi: 10.1124/mol.111.074401. PubMed PMID: 21937665.
