Glucokinase Activator, Cpd A-CAS 603108-44-7-Calbiochem

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一般描述

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 ?M 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 vivoand in rat islets and hepatocytes cultures (10 to 30 ?M)in vitro.

包装

5 mg in Plastic ampoule
Packaged under inert gas

警告

Toxicity: Standard Handling (A)

重悬

Following reconstitution, aliquot and freeze (-20°C). Stock solutions are stable for up to 6 months at -20°C.

其他说明

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.

法律信息

CALBIOCHEM is a registered trademark of Merck KGaA, Darmstadt, Germany

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