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: 41964-07-2

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

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

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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 rosiglitazone (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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