41964-07-2
41964-07-2 structure
- Name: tolimidone
- Chemical Name: 5-(3-methylphenoxy)-1H-pyrimidin-2-one
- CAS Number: 41964-07-2
- Molecular Formula: C11H10N2O2
- Molecular Weight: 202.209
- Catalog: Signaling Pathways Protein Tyrosine Kinase/RTK Src
- Create Date: 2018-07-07 16:24:35
- Modify Date: 2025-08-20 07:46:22
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Tolimidone is a potent and selective allosteric activator of Lyn kinase with an EC50 of 63 nM.
| Name | 5-(3-methylphenoxy)-1H-pyrimidin-2-one |
|---|---|
| Synonyms |
T6N CNJ BQ EOR C1
tolimidone QCR-285 5-(3-Methylphenoxy)-2(1H)-pyrimidinone Tolimidone (USAN) 5-(m-Tolyloxy)-2-(1H)-pyrimidinon 2(1H)-Pyrimidinone, 5-(3-methylphenoxy)- UNII-MU3JD8E9IS 5-m-tolyloxy-1H-pyrimidin-2-one T6MVNJ EOR C1 Tolimidone [USAN:INN] 5-(3-Methylphenoxy)- 2(1H)-pyrimidinone CP 26154 |
| Description | Tolimidone is a potent and selective allosteric activator of Lyn kinase with an EC50 of 63 nM. |
|---|---|
| Related Catalog | |
| 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]. |
| 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]. |
| Kinase Assay | 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]. |
| Cell Assay | 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]. |
| Animal Admin | 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]. |
| References |
| Density | 1.2±0.1 g/cm3 |
|---|---|
| Melting Point | 163-164ºC |
| Molecular Formula | C11H10N2O2 |
| Molecular Weight | 202.209 |
| Exact Mass | 202.074234 |
| PSA | 54.98000 |
| LogP | 1.37 |
| Index of Refraction | 1.598 |
| Storage condition | -20℃ |
| Symbol |
GHS07 |
|---|---|
| Signal Word | Warning |
| Hazard Statements | H319 |
| Precautionary Statements | P305 + P351 + P338 |
| Hazard Codes | N |
| RIDADR | NONH for all modes of transport |
| HS Code | 2933599090 |
| Precursor 2 | |
|---|---|
| DownStream 0 | |
| HS Code | 2933599090 |
|---|---|
| Summary | 2933599090. other compounds containing a pyrimidine ring (whether or not hydrogenated) or piperazine ring in the structure. VAT:17.0%. Tax rebate rate:13.0%. . MFN tariff:6.5%. General tariff:20.0% |