MLR-1023

Catalog No.S8321 Synonyms: Tolimidone, CP-26154

For research use only.

MLR-1023 (Tolimidone, CP-26154) 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.

MLR-1023 Chemical Structure

CAS No. 41964-07-2

Purity & Quality Control

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Biological Activity

Description MLR-1023 (Tolimidone, CP-26154) 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 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].

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].

Protocol (from reference)

Cell Research:[1]
  • 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 rosiglitazone (10 μM).
Animal Research:[1]
  • 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.

Solubility (25°C)

In vitro

In vivo

Add solvents to the product individually and in order
(Data is from Selleck tests instead of citations):
5%dmso+95%corn oil
For best results, use promptly after mixing.

5mg/mL

Chemical Information

Molecular Weight 202.21
Formula

C11H10N2O2

CAS No. 41964-07-2
Storage 3 years -20°C powder
2 years -80°C in solvent
Smiles CC1=CC(=CC=C1)OC2=CNC(=O)N=C2

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Method for preparing in vivo formulation: Take μL DMSO master liquid, next add μL Corn oil, mix and clarify.

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Molarity Calculator

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Clinical Trial Information

NCT Number Recruitment Interventions Conditions Sponsor/Collaborators Start Date Phases
NCT02317796 Completed Drug: MLR-1023 Type 2 Diabetes Melior Pharmaceuticals|Bukwang Pharmaceutical Co. Ltd. December 2014 Phase 2

(data from https://clinicaltrials.gov, updated on 2022-01-17)

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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