| Identification | Back Directory | [Name]
Tolimidone | [CAS]
41964-07-2 | [Synonyms]
100568
CP-26154
MLR 1023
CID-39065
Tolimidone
NSC 314335
MLR 1023 - Tolimidone | CP 26154
5-(m-Tolyloxy)pyrimidin-2(1H)-one
5-(3-methylphenoxy)-1H-pyrimidin-2-one
5-(3-Methylphenoxy)-2(1H)-pyrimidinone
2(1H)-Pyrimidinone, 5-(3-methylphenoxy)-
5-(3-Methylphenoxy)-2(1H)-pyrimidinone, 95+% | [EINECS(EC#)]
200-258-5 | [Molecular Formula]
C11H10N2O2 | [MDL Number]
MFCD00866900 | [MOL File]
41964-07-2.mol | [Molecular Weight]
202.212 |
| Chemical Properties | Back Directory | [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 | [InChI]
1S/C11H10N2O2/c1-8-3-2-4-9(5-8)15-10-6-12-11(14)13-7-10/h2-7H,1H3,(H,12,13,14) | [InChIKey]
HJQILFPVRNHTIG-UHFFFAOYSA-N | [SMILES]
Cc1cccc(OC2=CNC(=O)N=C2)c1 |
| Safety Data | Back Directory | [Hazard Codes ]
Xi | [Risk Statements ]
36 | [Safety Statements ]
26 | [WGK Germany ]
3 | [Storage Class]
11 - Combustible Solids | [Hazard Classifications]
Eye Irrit. 2 |
| Hazard Information | Back Directory | [Description]
MLR-1023 is an allosteric activator of Lyn kinase (EC50 = 63 nM).1 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.1 This effect is insulin-dependent, with MLR-1023 increasing insulin receptor sensitivity.2 MLR-1023 produces a dose-dependent and durable glucose-lowering effect in chronically treated db/db mice without causing weight gain.2 | [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. | [Synthesis]
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 | [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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