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125404-04-8

中文名稱 TCN 238
英文名稱 TCN 238
CAS 125404-04-8
分子式 C12H11N3
分子量 197.24
MOL 文件 125404-04-8.mol
更新日期 2024/12/03 15:40:37
125404-04-8 結構式 125404-04-8 結構式

基本信息

中文別名
化合物TCN 238
英文別名
TCN 238
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)
所屬類別
醫(yī)藥中間體:嘧啶類化合物

物理化學性質

儲存條件-20°C儲存
溶解度DMF: 25 mg/ml; DMSO: 25 mg/ml; DMSO:PBS(pH7.2) (1:1): 0.5 mg/ml; Ethanol: 5 mg/ml
形態(tài)粉末
顏色White to off-white

應用領域

用途1
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.

常見問題列表

生物活性
TCN238 是一種口服有效的 mGlu4 受體的正變構調節(jié)物,EC50 值為 1 μM。
靶點

mGlu4 Receptor

1 μM (EC 50 )

體外研究

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.

體內研究

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.

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