MLR-1023 is an allosteric activator of Lyn kinase (EC50 = 63 nM). It has no significant activity against a panel of related kinases. MLR-1023 is orally bioavailable and reduces blood glucose levels in mice subjected to an oral glucose tolerance test. This effect is insulin-dependent, with MLR-1023 increasing insulin receptor sensitivity. MLR-1023 produces a dose-dependent and durable glucose-lowering effect in chronically treated db/db mice without causing weight gain.
Tolimidone (MLR-1023) is an allosteric Lyn kinase activator that has been shown to reduce blood glucose levels in mice. Studies show that Tolimidone is an effective insulin receptor-potentiating agent that is potentially capable of producing durable blood glucose-lowering activity in diabetics. Tolimidone is a candidate for the treatment of type 2 diabetes.
