Glucokinase Activator, Cpd A ≥95% (by HPLC), Calbiochem®, Sigma-Aldrich®

Leverandør: Merck Millipore Calbiochem


M-Clarity™ quality level = MQ100

346021-5MG
346021-5MGEA 3375 NOK
346021-5MG
Glucokinase Activator, Cpd A ≥95% (by HPLC), Calbiochem®, Sigma-Aldrich®
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.


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.


Forpakning: Packaged under inert gas

Formel: C₁₄H₁₄N₆OS₂
Lagringstemperatur: Kjøleskap
CAS-nummer: 603108-44-7

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