Home Protein Tyrosine Kinase Src activator Tolimidone (MLR-1023) For research use only.

Tolimidone (MLR-1023)

Synonyms: CP-26154

Tolimidone (MLR-1023) is a Lyn kinase activator and a novel insulin receptor potentiator that elicits a rapid-onset and durable improvement in glucose homeostasis in animal models of type 2 diabetes.

Tolimidone (MLR-1023) Chemical Structure

Tolimidone (MLR-1023) Chemical Structure

CAS No. 41964-07-2

Purity & Quality Control

Batch: S832101 DMSO]40 mg/mL]false]Ethanol]23 mg/mL]false]Water]Insoluble]false Purity: 99.92%
99.92

Tolimidone (MLR-1023) Related Products

Signaling Pathway

Src Signaling Pathways

Src Signaling Pathway

Biological Activity

Description Tolimidone (MLR-1023) is a Lyn kinase activator and a novel insulin receptor potentiator that elicits a rapid-onset and durable improvement in glucose homeostasis in animal models of type 2 diabetes.
Targets
Insulin Receptor [2] Lyn [1]
(Cell-free assay)
63 nM(EC50)
In vitro
In vitro

In an in vitro broad kinase screen MLR-1023 activated the nonreceptor-linked Src-related tyrosine kinase Lyn. MLR-1023 increased the Vmax of Lyn with an EC50 of 63 nM. This Lyn kinase activation was ATP binding site independent, indicating that MLR-1023 regulated the kinase through an allosteric mechanism[1].
Cell Research Cell lines Mouse 3T3-L1 cells
Concentrations 10 μM
Incubation Time 8 days
Method

Adipocyte differentiation is assessed in mouse 3T3-L1 cells after 8 days of incubation with MLR-1023 or 10 μM
In Vivo
In vivo

MLR-1023-mediated blood glucose lowering depends on Lyn kinase activity[1]. MLR-1023 is an insulin receptor-potentiating agent that produces a rapid-onset and durable blood glucose-lowering activity in diabetic animals[2].
Animal Research Animal Models CD1-ICR male mice; Lyn kinase knockout mice (129S4-Lyntm1Sor/J) and wild-type controls (129S1/SvImJ)
Dosages 5 to 10 ml/kg.
Administration i.p.
NCT Number Recruitment Conditions Sponsor/Collaborators Start Date Phases
NCT02317796 Completed
Type 2 Diabetes
Melior Pharmaceuticals|Bukwang Pharmaceutical Co. Ltd.
 December 2014 Phase 2

Chemical Information & Solubility

Molecular Weight 202.21 Formula

C11H10N2O2
CAS No. 41964-07-2 SDF Download Tolimidone (MLR-1023) SDF
Smiles CC1=CC(=CC=C1)OC2=CNC(=O)N=C2
Storage (From the date of receipt)

In vitro
Batch:

DMSO : 40 mg/mL ( (197.81 mM) Moisture-absorbing DMSO reduces solubility. Please use fresh DMSO.)

Ethanol : 23 mg/mL

Water : Insoluble


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In vivo
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Tech Support

Answers to questions you may have can be found in the inhibitor handling instructions. Topics include how to prepare stock solutions, how to store inhibitors, and issues that need special attention for cell-based assays and animal experiments.

Handling Instructions

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