Tolimidone
Based on 5 publication(s) in Google Scholar
Tolimidone is a potent and selective allosteric activator of Lyn kinase with an EC50 of 63 nM.
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- 純度: 99.98%
- CAS 番号: 41964-07-2
- 分子式: C11H10N2O2
- 分子量:202.21
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保管条件:Powder -20°C, 3 years , 4°C, 2 years ; In solvent -80°C, 2 years , -20°C, 1 year
To place orders, for customer services and technical support, please contact: MedChemExpress USA
Tel: 609-228-6898 E-mail: [email protected] [email protected]
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生物活性
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化学情報
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溶剤 & 溶解度
- プロトコル
- 純度とドキュメンテーション
- 参考文献
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MedChemExpress（MCE）の使用を引用している文献 Tolimidone
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生物活性
EC50: 63 nM (Lyn kinase)[1]
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.
MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.
| NCT Number | Sponsor | Condition | Start Date |
Phase
|
|---|---|---|---|---|
| NCT01329991 | Plexxikon| | 2011-05 | PHASE1 |
化学情報
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CAS 番号 41964-07-2
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性状 Solid
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分子量 202.21
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分子式 C11H10N2O2
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Color White to yellow
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SMILES
O=C1N=CC(OC2=CC=CC(C)=C2)=CN1
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別名
MLR-1023; トリミドン
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輸送条件
Room temperature in continental US; may vary elsewhere.
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保管条件
Powder -20°C 3 years 4°C 2 years In solvent -80°C 2 years -20°C 1 year
Publications (5)
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Journal Impact Factor
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Most Recent
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Burns Trauma
Asiaticoside-nitric oxide synergistically accelerate diabetic wound healing by regulating key metabolites and SRC/STAT3 signaling. [Abstract]2025 Mar 10:13:tkaf009. PMID: 40066291 -
Can J Cardiol
WITHDRAWN: SNX10 deficiency restricts foam cell formation and protects against atherosclerosis by suppressing CD36-Lyn axis. [Abstract]2020 May 16:S0828-282X(20)30456-6. PMID: 32428616 -
Neurochem Res
Treml4 Drives Microglial Activation via the Lyn/Syk/ERK Pathway in Sepsis-Associated Encephalopathy. [Abstract]2026 May 20;51(3):164. PMID: 42159801 -
FASEB J
Endothelial microparticles induced by cyclic stretch activate Src and modulate cell apoptosis. [Abstract]2020 Oct;34(10):13586-13596. PMID: 32856783 -
Food Chem Toxicol
2020 Jan:135:110924. PMID: 31672514
溶剤 & 溶解度
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)
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.
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.
濃度 (開始) × 体積 (開始) = 濃度 (終了) × 体積 (終了)
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.
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.
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.
Please enter the basic information of animal experiments:
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Recommended: Prepare an additional quantity of animals to account for potential losses during experiments.
Please enter your animal formula composition:
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%DMSO +
Recommended: Keep the proportion of DMSO in working solution below 2% if your animal is weak.
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%+
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+%Tween-80 + +
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%Saline +
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).
Working solution concentration: 0.22 mg/mL
Method for preparing stock solution: mg drug dissolved in μL DMSO. Stock solution concentration: mg/mL.
1. Take μL DMSO stock solution;
2. Add μL .
μL , mix evenly;
3. Then add μL Tween 80, mix evenly;
4. Then add μL
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.
プロトコル
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].
MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.
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].
MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.
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].
MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.
純度とドキュメンテーション
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データシート (277 KB)
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SDS (393 KB)
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取扱説明書 (2659 KB)
参考文献
[1]. Saporito MS, et al. MLR-1023 is a potent and selective allosteric activator of Lyn kinase in vitro that improves glucose tolerance in vivo. J Pharmacol Exp Ther. 2012 Jul;342(1):15-22. [Content Brief]
[2]. Ochman AR, et al. The Lyn kinase activator MLR-1023 is a novel insulin receptor potentiator that elicits a rapid-onset and durable improvement in glucose homeostasis in animal models of type 2 diabetes. J Pharmacol Exp Ther. 2012 Jul;342(1):23-32. [Content Brief]
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 |
Tolimidone 関連分類
HY-59047 関連分類
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