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Tolimidone (MLR-1023) Src activator

Name: Tolimidone (MLR-1023)
Brand: Selleck Chemicals
SKU: S8321
Availability: InStock
Rating: 5 (2 reviews)

Cat.No.S8321

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.

Chemical Structure

Molecular Weight: 202.21

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Quality Control

Batch: S832101 DMSO]100 mg/mL]false]Ethanol]23 mg/mL]false]Water]Insoluble]false Purity: 99.92%

Cited in Nature Medicine for its top-tier quality
COA
NMR
SDS
Datasheet

99.92

Related Targets	EGFR VEGFR PDGFR FGFR c-Met MEK CSF-1R FLT3 HER2 c-Kit
Other Src Products	WH-4-023 Saracatinib (AZD0530) PP2 (AGL 1879) SU6656 PP1 Src Inhibitor 1 RK 24466 Myristic Acid eCF506 UM-164

Solubility

In vitro
Batch:

DMSO : 100 mg/mL (494.53 mM)
(Moisture-contaminated DMSO may reduce solubility. Use fresh, anhydrous DMSO.)

Ethanol : 23 mg/mL

Water : Insoluble

Molarity Calculator

Mass	Concentration	Volume	Molecular Weight
Mass value Mass unit	Concentration value Concentration unit	Volume value Volume unit	Molecular weight (g/mol)

Dilution Calculator Molecular Weight Calculator

In vivo batch selection In vivo Batch:
Homogeneous suspension	CMC-NA	≥5mg/ml	Taking the 1 mL working solution as an example, add 5 mg of this product to 1 ml of CMC-Na solution, mix evenly to obtain a homogeneous suspension with a final concentration of 5 mg/ml.
Clear solution	5%DMSO 1 Corn oil Validated by Selleck labs. Should you need adjustments to this formulation, contact our sales team for custom testing.	5.000mg/ml (24.73mM)	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.
Clear solution	5%DMSO 1 40%PEG300 2 5%Tween80 3 50%ddH2O Validated by Selleck labs. Should you need adjustments to this formulation, contact our sales team for custom testing.	5.000mg/ml (24.73mM)	Taking the 1 mL working solution as an example, add 50 μL of 100 mg/ml clarified DMSO stock solution to 400 μL of PEG300, mix evenly to clarify it; add 50 μL of Tween80 to the above system, mix evenly to clarify; then continue to add 500 μL of ddH2O to adjust the volume to 1 mL. The mixed solution should be used immediately for optimal results.

In vivo Formulation Calculator (Clear solution)

Step 1: Enter information below (Recommended: An additional animal making an allowance for loss during the experiment)

Dosage: mg/kg

Average weight of animals: g

Dosing volume per animal: μL

Number of animals:

Step 2: Enter the in vivo formulation (This is only the calculator, not formulation. Please contact us first if there is no in vivo formulation at the solubility Section.)

% DMSO

% Tween 80

% ddH₂O

% DMSO

Calculation results:

Working concentration: mg/ml;

Method for preparing DMSO master liquid: mg drug pre-dissolved in μL DMSO ( Master liquid concentration mg/mL, Please contact us first if the concentration exceeds the DMSO solubility of the batch of drug. )

Method for preparing in vivo formulation: Take μL DMSO master liquid, next addμL PEG300, mix and clarify, next addμL Tween 80, mix and clarify, next add μL ddH₂O, mix and clarify.

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

Note: 1. Please make sure the liquid is clear before adding the next solvent.
2. Be sure to add the solvent(s) in order. You must ensure that the solution obtained, in the previous addition, is a clear solution before proceeding to add the next solvent. Physical methods such
as vortex, ultrasound or hot water bath can be used to aid dissolving.

Chemical Information, Storage & Stability

Molecular Weight	202.21	Formula	C₁₁H₁₀N₂O₂	Storage (From the date of receipt)	3 years-20°Cpowder
CAS No.	41964-07-2	Download SDF		Storage of Stock Solutions	1 year-80°Cin solvent 1 month-20°Cin solvent
Synonyms	CP-26154			Smiles	CC1=CC(=CC=C1)OC2=CNC(=O)N=C2

Mechanism of Action

Targets/IC₅₀/Ki	Insulin Receptor Lyn (Cell-free assay) 63 nM(EC50)
In vitro	In an in vitro broad kinase screen, Tolimidone (MLR-1023) activated the nonreceptor-linked Src-related tyrosine kinase Lyn. This compound increased the Vmax of Lyn with an EC50 of 63 nM. This Lyn kinase activation was ATP binding site independent, indicating that it regulated the kinase through an allosteric mechanism.
In vivo	Tolimidone (MLR-1023) is an insulin receptor-potentiating agent that produces a rapid-onset and durable blood glucose-lowering activity in diabetic animals. Its blood glucose lowering depends on Lyn kinase activity.
References	[1] https://pubmed.ncbi.nlm.nih.gov/22473614/ [2] https://pubmed.ncbi.nlm.nih.gov/22431203/

Clinical Trial Information

(data from https://clinicaltrials.gov, updated on 2024-05-22)

NCT Number	Recruitment	Conditions	Sponsor/Collaborators	Start Date	Phases
NCT02317796	Completed	Type 2 Diabetes	Melior Pharmaceuticals\|Bukwang Pharmaceutical Co. Ltd.	December 2014	Phase 2

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