346021
Glucokinase Activator, Cpd A
The Glucokinase Activator, Cpd A, also referenced under CAS 603108-44-7, modulates Glucokinase. This small molecule/inhibitor is primarily used for Activators/Inducers applications.
别名:
Glucokinase Activator, Cpd A, Hexokinase D Activator, Hexokinase IV Activator, 2-Amino-5-(4-methyl-4H-(1,2,4)-triazole-3-yl-sulfanyl)-N-(4-methyl-thiazole-2-yl)benzamide, Compound A
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关于此项目
经验公式（希尔记法）:
C14H14N6OS2
化学文摘社编号:
分子量:
346.43
MDL number:
NACRES:
NA.77
UNSPSC Code:
41121706
产品名称
Glucokinase Activator, Cpd A, The Glucokinase Activator, Cpd A, also referenced under CAS 603108-44-7, modulates Glucokinase. This small molecule/inhibitor is primarily used for Activators/Inducers applications.
assay
≥95% (HPLC)
form
solid
manufacturer/tradename
Calbiochem®
storage condition
OK to freeze
protect from light
color
off-white
solubility
DMSO: 5 mg/mL
shipped in
ambient
storage temp.
2-8°C
Quality Level
Disclaimer
Toxicity: Standard Handling (A)
General description
A cell-permeable thiazolylamide glucokinase (GK; Hexokinase IV/D) activator that reversibly targets a allosteric site that is only exposed for binding in the glucose-bound GK conformation, but not in the unbound "super-open" GK conformation or the GKRP- (GK Regulatory Protein) bound GK, and effectively stabilizes GK in an active conformation as well as prevents its interaction with and nuclear sequestration by GKRP, while exhibiting little effect against Hexokinase I/II/III. Compound A is shown to activate GK activity in cell-free assays (EC50 = 0.42 and 0.14 µM in the presence of 2.5 mM and 10 mM of glucose, respectively) and effectively induce cellular GK activation and increase glucose metabolism both in in rats (10 to 30 mg/kg, p.o.) in vivo and in rat islets and hepatocytes cultures (10 to 30 µM) in vitro.
Other Notes
Iino, T., et al. 2009. Bioorg. Med. Chem. Lett.19, 5531.
Mitsuya, M., et al. 2009. Bioorg. Med. Chem. Lett.19, 2718.
Nishimura, T., et al. 2009. Bioorg. Med. Chem. Lett.19, In press.
Futamura, M., et al. 2006. J. Biol. Chem.281, 1357.
Kamata, K., et al. 2004. Structure12, 429.
Mitsuya, M., et al. 2009. Bioorg. Med. Chem. Lett.19, 2718.
Nishimura, T., et al. 2009. Bioorg. Med. Chem. Lett.19, In press.
Futamura, M., et al. 2006. J. Biol. Chem.281, 1357.
Kamata, K., et al. 2004. Structure12, 429.
Packaging
Packaged under inert gas
Preparation Note
Following reconstitution, aliquot and freeze (-20°C). Stock solutions are stable for up to 6 months at -20°C.
Legal Information
CALBIOCHEM is a registered trademark of Merck KGaA, Darmstadt, Germany
存储类别
11 - Combustible Solids
wgk
WGK 1
flash_point_f
Not applicable
flash_point_c
Not applicable
Ryota Inoue et al.
iScience, 25(7), 104603-104603 (2022-07-09)
Uncoupling protein 2 (UCP2), a mitochondrial protein, is known to be upregulated in pancreatic islets of patients with type 2 diabetes (T2DM); however, the pathological significance of this increase in UCP2 expression is unclear. In this study, we highlight the
Sophie L Lewandowski et al.
Cell metabolism, 32(5), 736-750 (2020-11-05)
Pancreatic β cells couple nutrient metabolism with appropriate insulin secretion. Here, we show that pyruvate kinase (PK), which converts ADP and phosphoenolpyruvate (PEP) into ATP and pyruvate, underlies β cell sensing of both glycolytic and mitochondrial fuels. Plasma membrane-localized PK
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