TCN 238
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- CAS号:
- 125404-04-8
- 英文名:
- TCN 238
- 英文别名:
- TCN 238;Lu AF32615;TCN 238; TCN-238;4-Styryl-pyrimidin-2-ylamine;(E)-4-(2-Phenylethenyl)-2-pyriMidinaMine;2-PyriMidinaMine, 4-(2-phenylethenyl)-, (E)-;2-PyriMidinaMine, 4-(2-phenylethenyl)-, (E)- (9CI);inhibit,TCN-238,mGluR,TCN238,Metabotropic glutamate receptors,Inhibitor
- 中文名:
- TCN 238
- 中文别名:
- 化合物TCN 238;TCN 238,MGLU4受体的正变构调节剂
- CBNumber:
- CB02546791
- 分子式:
- C12H11N3
- 分子量:
- 197.24
- MOL File:
- 125404-04-8.mol
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TCN 238化学性质
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储存条件:
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Store at -20°C
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溶解度:
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DMF: 25 mg/ml; DMSO: 25 mg/ml; DMSO:PBS(pH7.2) (1:1): 0.5 mg/ml; Ethanol: 5 mg/ml
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形态:
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Powder
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TCN 238性质、用途与生产工艺
TCN238 是一种口服有效的 mGlu4 受体的正变构调节物，EC50 值为 1 μM。
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mGlu4 Receptor
1 μM (EC
50
)
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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.
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.
用途
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鈥檚 disease. TCN 238 is orally bioavailable.
TCN 238
上下游产品信息
上游原料
下游产品
| 更新日期 | 产品编号 | 产品名称 | CAS编号 | 包装 | 价格 |
|---|
| 2024/01/25 | HY-14419 | TCN238 | | 1 mg | 240元 |
| 2024/01/25 | HY-14419 | TCN 238
TCN238 | 125404-04-8 | 5mg | 600元 |
125404-04-8, TCN 238 相关搜索:
- Pharmaceuticals
- Intermediates & Fine Chemicals
- Heterocycles
- Aromatics
- 合成有机化合物配体
- TCN 238,MGLU4受体的正变构调节剂
- 化合物TCN 238
- 125404-04-8
- inhibit,TCN-238,mGluR,TCN238,Metabotropic glutamate receptors,Inhibitor
- Lu AF32615
- 4-Styryl-pyrimidin-2-ylamine
- TCN 238; TCN-238
- 2-PyriMidinaMine, 4-(2-phenylethenyl)-, (E)-
- 2-PyriMidinaMine, 4-(2-phenylethenyl)-, (E)- (9CI)
- (E)-4-(2-Phenylethenyl)-2-pyriMidinaMine
- TCN 238