Glucokinase

Glucokinase activators act on hexokinase IV, the glucose sensor of pancreatic beta cells and the liver. Glucokinase (GK) phosphorylates glucose to glucose-6-phosphate with low affinity and without inhibition by its product. Its activity therefore rises and falls with blood glucose over the physiological range. A 1995 study of knockout mice showed that beta-cell glucokinase is required to maintain glucose homeostasis. In 2003 Ro 28-1675 was described as an allosteric activator that binds outside the active site and increases glucose affinity. Later activators in the catalogue include piragliatin, MK-0941 and globalagliatin. PF-04991532 is a hepatoselective activator used to separate liver effects from those in islets.

1 Item

  • PF-04279405
    Cat. No.
    A74946

    PF-04279405

    PF-04279405 is a potent glucokinase (GK) agonist with an EC50 of 23 nM. Glucokinase is crucial for glucose metabolism, facilitating the conversion of glucose to glucose-6-phosphate and contributing to glucose homeostasis. This compound is valuable for research applications targeting type 2 diabetes, offering insights into therapeutic mechanisms and metabolic regulation.

    25 mg
    $1,275.00
    50 mg
    $1,625.00
    All 3 sizes

1 Item

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