| Size | Price | Stock | Qty |
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| 10mg |
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| 25mg |
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| 50mg |
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Purity: ≥98%
Tolimidone, formerly known as MLR-1023, is a novel and potent insulin receptor potentiator, and also a selective allosteric activator of Lyn kinase (EC50 of 63 nM).
| Targets |
Insulin Receptor; Lyn (EC50 = 63 nM)
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|---|---|
| ln Vitro |
Tolimidone (MLR-1023) exhibits a 50% increase in enzyme activity that is repeatable when incubated with Lyn kinase. Lyn kinase activation is increased in response to tolimidone in a concentration-dependent manner, increasing by 2.3 and 2.1 fold at concentrations of 3 and 10 μM, respectively. When Tolimidone (100 μM) is added, Lyn kinase activity increases threefold at every tested ATP concentration (Vmax=2601 U/mg). The length of the preincubation period in the absence of ATP determines how much Lyn kinase is activated by tolimidone[1].
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| ln Vivo |
Tolimidone (MLR-1023) (30 mg/kg i.p.) is administered, blood glucose levels are significantly (p<0.05) lowered to 148 and 158 mg/dL, respectively, 30 and 90 minutes later. Adiponectin production and adipocyte differentiation are both markedly increased by tolimidone, increasing them by 19 and 3.7 times, respectively[1]. A maximal effect of 30 mg/kg is observed when tolimidone is administered, eliciting a dose-dependent potentiation of the insulin response[2].
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| Enzyme Assay |
Tolimidone (MLR-1023) (10 μM) is preincubated with kinase and fluoroscein-labeled protein substrate for every kinase test. The amount of fluoroscein phosphopeptide is measured after the addition of ATP, at a concentration equal to or less than the Km for each kinase, starts the reaction. There are two assays performed[1].
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| Cell Assay |
In mouse 3T3-L1 cells, adipocyte differentiation is evaluated following an 8-day incubation period with either Tolimidone (MLR-1023) or Rosiglitazone (10 μM). Transiently transfected cells containing the appropriate DNA constructs (pGAL4/PPARα, σ, or γ) cotransfected with a luciferase reporter vector are used for PPAR (α, σ, and γ) transactivation studies. For twenty-four hours, transfected cells are incubated with tolimidone or a suitable reference compound. The level of PPARα, σ, and γ activation is measured by luciferase activity[1].
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| Animal Protocol |
Baseline glucose, glucose tolerance, and insulin levels are studied in male mice aged 8 to 10 weeks. Intraperitoneal injections of tolimidone (MLR-1023) are given at dose volumes ranging from 5 to 10 mL/kg. A tail snip is used to obtain 5 μL of blood, which is then immediately applied to a glucose test strip. Liquid chromatography/tandem mass spectrometry is used to measure the levels of Tolimidone in blood. The levels are then compared to a standard curve of Tolimidone prepared in blood[1].
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| References |
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| Molecular Formula |
C11H10N2O2
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|---|---|
| Molecular Weight |
202.2093
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| Exact Mass |
202.07
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| Elemental Analysis |
C, 65.34; H, 4.98; N, 13.85; O, 15.82
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| CAS # |
41964-07-2
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| Related CAS # |
41964-07-2
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| Appearance |
Solid powder
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| SMILES |
CC1=CC(=CC=C1)OC2=CNC(=O)N=C2
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| InChi Key |
HJQILFPVRNHTIG-UHFFFAOYSA-N
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| InChi Code |
InChI=1S/C11H10N2O2/c1-8-3-2-4-9(5-8)15-10-6-12-11(14)13-7-10/h2-7H,1H3,(H,12,13,14)
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| Chemical Name |
5-(3-methylphenoxy)-1H-pyrimidin-2-one
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| Synonyms |
CP 26,154; CP 26,154; CP 26,154; NSC 314335; MLR-1023; MLR 1023; MLR1023; 41964-07-2
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| HS Tariff Code |
2934.99.9001
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| Storage |
Powder -20°C 3 years 4°C 2 years In solvent -80°C 6 months -20°C 1 month |
| Shipping Condition |
Room temperature (This product is stable at ambient temperature for a few days during ordinary shipping and time spent in Customs)
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| Solubility (In Vitro) |
DMSO: 40~150 mg/mL (197.8~741.8 mM)
Ethanol: ~23 mg/mL (~113.7 mM) |
|---|---|
| Solubility (In Vivo) |
Solubility in Formulation 1: ≥ 2.5 mg/mL (12.36 mM) (saturation unknown) in 10% DMSO + 40% PEG300 + 5% Tween80 + 45% Saline (add these co-solvents sequentially from left to right, and one by one), clear solution.
For example, if 1 mL of working solution is to be prepared, you can add 100 μL of 25.0 mg/mL clear DMSO stock solution to 400 μL PEG300 and mix evenly; then add 50 μL Tween-80 to the above solution and mix evenly; then add 450 μL normal saline to adjust the volume to 1 mL. Preparation of saline: Dissolve 0.9 g of sodium chloride in 100 mL ddH₂ O to obtain a clear solution. Solubility in Formulation 2: ≥ 2.5 mg/mL (12.36 mM) (saturation unknown) in 10% DMSO + 90% (20% SBE-β-CD in Saline) (add these co-solvents sequentially from left to right, and one by one), clear solution. For example, if 1 mL of working solution is to be prepared, you can add 100 μL of 25.0 mg/mL clear DMSO stock solution to 900 μL of 20% SBE-β-CD physiological saline solution and mix evenly. Preparation of 20% SBE-β-CD in Saline (4°C，1 week): Dissolve 2 g SBE-β-CD in 10 mL saline to obtain a clear solution. View More
Solubility in Formulation 3: 2.5 mg/mL (12.36 mM) in 10% DMSO + 90% Corn Oil (add these co-solvents sequentially from left to right, and one by one), clear solution. Solubility in Formulation 4: 5%dmso+95%corn oil: 5mg/mL |
| Preparing Stock Solutions | 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 | |
| 10 mM | 0.4945 mL | 2.4727 mL | 4.9454 mL |
*Note: Please select an appropriate solvent for the preparation of stock solution based on your experiment needs. For most products, DMSO can be used for preparing stock solutions (e.g. 5 mM, 10 mM, or 20 mM concentration); some products with high aqueous solubility may be dissolved in water directly. Solubility information is available at the above Solubility Data section. Once the stock solution is prepared, aliquot it to routine usage volumes and store at -20°C or -80°C. Avoid repeated freeze and thaw cycles.
Calculation results
Working concentration： mg/mL；
Method for preparing DMSO stock solution： mg drug pre-dissolved in μL DMSO (stock solution 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 stock solution, next add μL PEG300, mix and clarify, next addμL Tween 80, mix and clarify, next add μL ddH2O，mix and clarify.
(1) Please be sure that the solution is clear before the addition of next solvent. Dissolution methods like vortex, ultrasound or warming and heat may be used to aid dissolving.
(2) Be sure to add the solvent(s) in order.
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