MLR-1023

For research use only.

Catalog No.S8321 Synonyms: Tolimidone, CP-26154

MLR-1023 Chemical Structure

CAS No. 41964-07-2

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.

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Biological Activity

Description 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
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

Cell Research:[1]
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  • 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).
    (Only for Reference)
Animal Research:[1]
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  • 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.
    (Only for Reference)

Solubility (25°C)

In vitro DMSO 40 mg/mL (197.81 mM)
Ethanol 23 mg/mL (113.74 mM)
Water Insoluble
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

* Please note that Selleck tests the solubility of all compounds in-house, and the actual solubility may differ slightly from published values. This is normal and is due to slight batch-to-batch variations.

Chemical Information

Molecular Weight 202.21
Formula

C11H10N2O2

CAS No. 41964-07-2
Storage powder
in solvent
Synonyms Tolimidone, CP-26154
Smiles CC1=CC(=CC=C1)OC2=CNC(=O)N=C2

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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

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Src Signaling Pathway Map

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Cell Lines Assay Type Concentration Incubation Time Formulation Activity Description PMID