Basic information Safety Supplier Related

Tolimidone

Basic information Safety Supplier Related

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
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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
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Safety Information

Hazard Codes 
Xi
Risk Statements 
36
Safety Statements 
26
WGK Germany 
3
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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

TolimidoneSupplier

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