2-PyriMidinaMine, 4-(2-phenylethenyl)-, (E)- (9CI)
TCN 238
CAS: 125404-04-8
Molecular Formula: C12H11N3
2-PyriMidinaMine, 4-(2-phenylethenyl)-, (E)- (9CI) - Names and Identifiers
2-PyriMidinaMine, 4-(2-phenylethenyl)-, (E)- (9CI) - Physico-chemical Properties
| Molecular Formula | C12H11N3 |
| Molar Mass | 197.24 |
| Storage Condition | 2-8℃ |
| In vitro study | In the rat mGlu4 PAM in vitro assay the EC 50 of TCN238 (Compound 11) is 1 μM which is comparable to the human assay. TCN238 is screened in rat and human mGlu5 assays, the IC 50 of 11 is >30 μM on human mGlu5and >10 μM on rat mGlu5. TCN238 is run in a receptor screening panel of 68 targets and no activity is observed at ≥50% at 10 μM for any of the receptors. In CaCo-2 cells, TCN238 is found to have good permeability with no apparent efflux issue. |
| In vivo study | TCN238 is highly CNS penetrant with a concentration of 33.8 μM in the brain. The plasma protein binding in rats is measured as 90% bound. The metabolic stability of TCN238 is assessed in rat and human microsomes and found to be 62% and 83% hepatic blood flow. The limited stability translated into a high in vivo clearance in rats of 75 mL/min/kg and TCN238 has a moderate volume of distribution (2.7 L/kg) with a short mean residence time (0.6 h) when dosed at 2 mg/kg via intravenous injection. TCN238 is orally bioavailable and 30 min following administration of a30 mg/kg dose, the plasma concentration is found to be 11.6 μM. TCN 238 does not affect the performance of the learned task. However, the expression level of GRM4 in the hippocampus is reliable down-regulated five days after treatment with TCN 238. In addition, the expression level of GABRA1, encoding GABAA α-subunit is downregulated five days after the treatment in the frontal cortex. |
2-PyriMidinaMine, 4-(2-phenylethenyl)-, (E)- (9CI) - Preparation solution concentration reference
| 1mg | 5mg | 10mg | |
|---|---|---|---|
| 1 mM | 5.07 ml | 25.35 ml | 50.7 ml |
| 5 mM | 1.014 ml | 5.07 ml | 10.14 ml |
| 10 mM | 0.507 ml | 2.535 ml | 5.07 ml |
| 5 mM | 0.101 ml | 0.507 ml | 1.014 ml |
Last Update：2024-01-02 23:10:35
2-PyriMidinaMine, 4-(2-phenylethenyl)-, (E)- (9CI) - Reference Information
| biological activity | TCN238 is an orally effective positive allosteric regulator of the mGlu4 receptor, the EC50 value was 1 μm. |
| purpose | TCN 238 allosteric modulator of the mGlu4 receptor. TCN 238 may be useful in the treatment of motor dysfunction and in the treatment of Parkinson. TCN 238 is orally bioavailable. |
Last Update：2024-04-10 22:29:15
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CAS: 125404-04-8
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CAS: 125404-04-8
Tel: 18301782025
Email: 3008007409@qq.com
Mobile: 18021002903
QQ: 3008007409
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