2. Protein Tyrosine Kinase/RTK
  3. Src
  4. Tolimidone

Tolimidone  (Synonyms: MLR-1023)

Cat. No.: HY-59047 Purity: 99.93%
COA Handling Instructions

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Tolimidone is a potent and selective allosteric activator of Lyn kinase with an EC50 of 63 nM.

For research use only. We do not sell to patients.

Tolimidone Chemical Structure

Tolimidone Chemical Structure

CAS No. : 41964-07-2

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Based on 3 publication(s) in Google Scholar

Tolimidone Related Antibodies

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Lck Fyn Blk

  • Biological Activity

  • Protocol

  • Purity & Documentation

  • References

  • Customer Review

Description

Tolimidone is a potent and selective allosteric activator of Lyn kinase with an EC50 of 63 nM.

IC50 & Target

EC50: 63 nM (Lyn kinase)[1]
In Vitro

Incubation of Tolimidone (MLR-1023) with Lyn kinase elicits a repeatable 50% increase in enzyme activity. Tolimidone elicits a concentration-dependent increase in Lyn kinase activation with a 2.3- and 2.1-fold increase achieved at concentrations of 3 and 10 μM, respectively. Inclusion of Tolimidone (100 μM) increases Lyn kinase activity by 3-fold at each ATP concentration tested (Vmax=2601 U/mg). Tolimidone-mediated activation of Lyn kinase increases in proportion to the length of preincubation period in the absence of ATP[1].

MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.

Tolimidone Related Antibodies
In Vivo

Administration of Tolimidone (MLR-1023) (30 mg/kg i.p.) significantly (p<0.05) lowers blood glucose levels to 148 and 158 mg/dL, 30 and 90 min after administration, respectively. Tolimidone significantly increases adipocyte differentiation and adiponectin production by 3.7- and 19-fold, respectively[1]. Tolimidone elicits a dose-dependent potentiation of the insulin response, with a maximal effect observed with a dose level of 30 mg/kg[2].

MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.
Clinical Trial
Molecular Weight

202.21

Formula

C11H10N2O2
CAS No.
Appearance

Solid

Color

White to yellow

SMILES

O=C1N=CC(OC2=CC=CC(C)=C2)=CN1
Shipping

Room temperature in continental US; may vary elsewhere.
Storage
Powder -20°C 3 years
4°C 2 years
In solvent -80°C 2 years
-20°C 1 year
Solvent & Solubility
In Vitro: 

DMSO : 150 mg/mL (741.80 mM; Need ultrasonic; Hygroscopic DMSO has a significant impact on the solubility of product, please use newly opened DMSO)

Preparing
Stock Solutions
Concentration Solvent Mass 1 mg 5 mg 10 mg
1 mM 4.9454 mL 24.7268 mL 49.4535 mL
5 mM 0.9891 mL 4.9454 mL 9.8907 mL
View the Complete Stock Solution Preparation Table

* Please refer to the solubility information to select the appropriate solvent. Once prepared, please aliquot and store the solution to prevent product inactivation from repeated freeze-thaw cycles.
Storage method and period of stock solution: -80°C, 2 years; -20°C, 1 year. When stored at -80°C, please use it within 2 years. When stored at -20°C, please use it within 1 year.

  • Molarity Calculator

  • Dilution Calculator

Mass (g) = Concentration (mol/L) × Volume (L) × Molecular Weight (g/mol)

Mass
=
Concentration
×
Volume
×
Molecular Weight *

Concentration (start) × Volume (start) = Concentration (final) × Volume (final)

This equation is commonly abbreviated as: C1V1 = C2V2

Concentration (start)

C1

×
Volume (start)

V1

=
Concentration (final)

C2

×
Volume (final)

V2

In Vivo:

Select the appropriate dissolution method based on your experimental animal and administration route.

For the following dissolution methods, please ensure to first prepare a clear stock solution using an In Vitro approach and then sequentially add co-solvents:
To ensure reliable experimental results, the clarified stock solution can be appropriately stored based on storage conditions. As for the working solution for in vivo experiments, it is recommended to prepare freshly and use it on the same day.
The percentages shown for the solvents indicate their volumetric ratio in the final prepared solution. If precipitation or phase separation occurs during preparation, heat and/or sonication can be used to aid dissolution.

  • Protocol 1

    Add each solvent one by one:  10% DMSO    40% PEG300    5% Tween-80    45% Saline

    Solubility: ≥ 2.5 mg/mL (12.36 mM); Clear solution

    This protocol yields a clear solution of ≥ 2.5 mg/mL (saturation unknown).

    Taking 1 mL working solution as an example, add 100 μL DMSO stock solution (25.0 mg/mL) to 400 μL PEG300, and mix evenly; then add 50 μL Tween-80 and mix evenly; then add 450 μL Saline to adjust the volume to 1 mL.

    Preparation of Saline: Dissolve 0.9 g sodium chloride in ddH₂O and dilute to 100 mL to obtain a clear Saline solution.
  • Protocol 2

    Add each solvent one by one:  10% DMSO    90% (20% SBE-β-CD in Saline)

    Solubility: ≥ 2.5 mg/mL (12.36 mM); Clear solution

    This protocol yields a clear solution of ≥ 2.5 mg/mL (saturation unknown).

    Taking 1 mL working solution as an example, add 100 μL DMSO stock solution (25.0 mg/mL) to 900 μL 20% SBE-β-CD in Saline, and mix evenly.

    Preparation of 20% SBE-β-CD in Saline (4°C, storage for one week): 2 g SBE-β-CD powder is dissolved in 10 mL Saline, completely dissolve until clear.
In Vivo Dissolution Calculator
Please enter the basic information of animal experiments:

Dosage

mg/kg

Animal weight
(per animal)

g

Dosing volume
(per animal)

μL

Number of animals

Recommended: Prepare an additional quantity of animals to account for potential losses during experiments.
Please enter your animal formula composition:
%
DMSO +
% 
+
%
Tween-80 +
%
Saline
Recommended: Keep the proportion of DMSO in working solution below 2% if your animal is weak.
The co-solvents required include: DMSO, . All of co-solvents are available by MedChemExpress (MCE). , Tween 80. All of co-solvents are available by MedChemExpress (MCE).
Calculation results:
Working solution concentration: mg/mL
Method for preparing stock solution: mg drug dissolved in μL  DMSO (Stock solution concentration: mg/mL).
The concentration of the stock solution you require exceeds the measured solubility. The following solution is for reference only. If necessary, please contact MedChemExpress (MCE).
Method for preparing in vivo working solution for animal experiments: Take μL DMSO stock solution, add μL . μL , mix evenly, next add μL Tween 80, mix evenly, then add μL Saline.
 If the continuous dosing period exceeds half a month, please choose this protocol carefully.
Please ensure that the stock solution in the first step is dissolved to a clear state, and add co-solvents in sequence. You can use ultrasonic heating (ultrasonic cleaner, recommended frequency 20-40 kHz), vortexing, etc. to assist dissolution.
Purity & Documentation

Purity: 99.93%

COA (246 KB) HNMR (220 KB) LCMS (136 KB)

Handling Instructions (2659 KB)
References
Kinase Assay
[1]

For each kinase assay, Tolimidone (MLR-1023) (10 μM) is preincubated with kinase and fluoroscein-labeled protein substrate. The reaction is initiated with the addition of ATP (at a concentration at or below the Km for each kinase), and the level of fluoroscein phosphopeptide is measured. The assays are conducted in duplicate[1].

MCE has not independently confirmed the accuracy of these methods. They are for reference only.
Cell Assay
[1]

Adipocyte differentiation is assessed in mouse 3T3-L1 cells after 8 days of incubation with Tolimidone (MLR-1023) or rosiglitazone (10 μM). PPAR (α, σ and γ) transactivation studies are conducted in transiently transfected cells containing the appropriate DNA constructs (pGAL4/PPARα, σ or γ) cotransfected with a luciferase reporter vector. Tolimidone or an appropriate reference compound is incubated with transfected cells for 24 h. Luciferase activity is monitored as a measure of PPARα, σ and γ activation[1].

MCE has not independently confirmed the accuracy of these methods. They are for reference only.
Animal Administration
[1]

Male mice, 8 to 10 weeks of age, are used in studies of baseline glucose, glucose tolerance, and insulin levels. Tolimidone (MLR-1023) is administered intraperitoneally at dose volumes of 5 to 10 mL/kg. Blood (5 μL) is acquired from a tail snip and directly applied to a glucose test strip. Blood levels of Tolimidone are measured by liquid chromatography/tandem mass spectrometry, and levels are determined by comparing them with a standard curve of Tolimidone prepared in blood[1].

MCE has not independently confirmed the accuracy of these methods. They are for reference only.
References

Complete Stock Solution Preparation Table

* Please refer to the solubility information to select the appropriate solvent. Once prepared, please aliquot and store the solution to prevent product inactivation from repeated freeze-thaw cycles.
Storage method and period of stock solution: -80°C, 2 years; -20°C, 1 year. When stored at -80°C, please use it within 2 years. When stored at -20°C, please use it within 1 year.

Optional Solvent Concentration Solvent Mass 1 mg 5 mg 10 mg 25 mg
DMSO 1 mM 4.9454 mL 24.7268 mL 49.4535 mL 123.6338 mL
5 mM 0.9891 mL 4.9454 mL 9.8907 mL 24.7268 mL
10 mM 0.4945 mL 2.4727 mL 4.9454 mL 12.3634 mL
15 mM 0.3297 mL 1.6485 mL 3.2969 mL 8.2423 mL
20 mM 0.2473 mL 1.2363 mL 2.4727 mL 6.1817 mL
25 mM 0.1978 mL 0.9891 mL 1.9781 mL 4.9454 mL
30 mM 0.1648 mL 0.8242 mL 1.6485 mL 4.1211 mL
40 mM 0.1236 mL 0.6182 mL 1.2363 mL 3.0908 mL
50 mM 0.0989 mL 0.4945 mL 0.9891 mL 2.4727 mL
60 mM 0.0824 mL 0.4121 mL 0.8242 mL 2.0606 mL
80 mM 0.0618 mL 0.3091 mL 0.6182 mL 1.5454 mL
100 mM 0.0495 mL 0.2473 mL 0.4945 mL 1.2363 mL
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Tolimidone Related Classifications

Help & FAQs
  • Do most proteins show cross-species activity?

    Species cross-reactivity must be investigated individually for each product. Many human cytokines will produce a nice response in mouse cell lines, and many mouse proteins will show activity on human cells. Other proteins may have a lower specific activity when used in the opposite species.

Keywords:

Tolimidone41964-07-2MLR-1023MLR1023MLR 1023SrcInhibitorinhibitorinhibit

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