Tolimidone
Tolimidone Basic information
- Product Name:
- Tolimidone
- Synonyms:
-
- Tolimidone
- 5-(m-Tolyloxy)pyrimidin-2(1H)-one
- CP-26154
- 2(1H)-Pyrimidinone, 5-(3-methylphenoxy)-
- 5-(3-methylphenoxy)-1H-pyrimidin-2-one
- 5-(3-Methylphenoxy)-2(1H)-pyrimidinone
- NSC 314335
- MLR 1023
- CAS:
- 41964-07-2
- MF:
- C11H10N2O2
- MW:
- 202.21
- EINECS:
- 200-258-5
- Mol File:
- 41964-07-2.mol
Tolimidone Chemical Properties
- Melting point:
- 163-164℃
- Density
- 1.22
- storage temp.
- room temp
- solubility
- DMSO: soluble15mg/mL (clear solution)
- form
- powder
- pka
- 8.14±0.10(Predicted)
- color
- white to beige
Tolimidone Usage And Synthesis
Description
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.
Uses
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.
in vivo
Administration of Tolimidone (MLR-1023) (30 mg/kg i.p.) significantly (p<0.05) lowers blood glucose levels to 148 and 158 mg/dL, 30 and 90 min after administration, respectively. Tolimidone significantly increases adipocyte differentiation and adiponectin production by 3.7- and 19-fold, respectively[1]. Tolimidone elicits a dose-dependent potentiation of the insulin response, with a maximal effect observed with a dose level of 30 mg/kg[2].
storage
Store at +4°C
References
[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
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