Tolimidone (MLR-1023)

Catalog No.S8321 Batch:S832101

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Technical Data

Formula

C11H10N2O2
Molecular Weight 202.21 CAS No. 41964-07-2
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)
Clear solution
5%DMSO Corn oil
5.0mg/ml Taking the 1 mL working solution as an example, add 50 μL of 100 mg/ml clear DMSO stock solution to 950 μL of corn oil and mix evenly. The mixed solution should be used immediately for optimal results. 
* <1 mg/ml means slightly soluble or insoluble.
* 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.
* Room temperature shipping (Stability testing shows this product can be shipped without any cooling measures.)

Preparing Stock Solutions

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 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 Assay:

[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 10 μM
Animal Study:

[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.

Selleck's Tolimidone (MLR-1023) has been cited by 1 publication

Lyn attenuates sepsis-associated acute kidney injury by inhibition of phospho-STAT3 and apoptosis [ Biochemical Pharmacology, 2023, Volume 211] PubMed: None

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SHIPPING AND STORAGE
Selleck products are transported at room temperature. If you receive the product at room temperature, please rest assured, the Selleck Quality Inspection Department has conducted experiments to verify that the normal temperature placement of one month will not affect the biological activity of powder products. After collecting, please store the product according to the requirements described in the datasheet. Most Selleck products are stable under the recommended conditions.

NOT FOR HUMAN, VETERINARY DIAGNOSTIC OR THERAPEUTIC USE.