41964-07-2

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.

Fill a 3-liter 3-neck flask equipped with a pressure dropping funnel. Add 99.1 g (1.5 mol) of 85% KOH pellets to an O-head stirrer and a condenser with solvent lead-in. The dry flask was heated and 170.0 g (1.5 mol) of m-cresol was added to the stirred ho

Store at +4°C

[1] MICHAEL S SAPORITO. MLR-1023 is a potent and selective allosteric activator of Lyn kinase in vitro that improves glucose tolerance in vivo.[J]. ACS Applied Electronic Materials, 2012: 15-22. DOI: 10.1124/jpet.112.192096
[2] ALEXANDER R OCHMAN. The Lyn kinase activator MLR-1023 is a novel insulin receptor potentiator that elicits a rapid-onset and durable improvement in glucose homeostasis in animal models of type 2 diabetes.[J]. Journal of Pharmacology and Experimental Therapeutics, 2012, 342 1: 23-32. DOI: 10.1124/jpet.112.192187