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TCN238  ≥98%

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包装规格：5mg 10mg 25mg 50mg 100mg in glass bottle
溶解性：溶于DMSO(≥150mg/mL）
产品描述：基本信息 产品编号： T11463 产品名称： TCN238 CAS: 125404-04-8   储存条件 粉末 -20℃ 四年     分子式： C12H11N3 溶于液体 -80℃ 6个月 分子量 197.24 -20℃ 1个月 化学名：  3-cyclohexyl-5-fluoro-6-methyl-7-(2-morpholin-4-ylethoxy)-4h-chromen-4-one Solubility (25°C)：   体外:   DMSO   Ethanol   Water   体内(现配现用):   ＜1mg/ml表示微溶或不溶。 普西唐提供的所有化合物浓度为内部测试所得，实际溶液度可能与公布值有所偏差，属于正常的批间细微差异现象。 请根据产品在不同溶剂中的溶解度选择合适的溶剂配制储备液；⼀旦配成溶液，请分装保存，避免反复冻融造成的产品失效。   制备储备液   浓度   溶液体积 质量   1mg   5mg   10mg 1mM 5.0700mL 25.3498mL 50.6997mL 5mM 1.0140mL 5.0700mL 10.1399mL 10mM 0.5070mL 2.5350mL 5.0700mL   生物活性 产品描述 一种口服有效的 mGlu4 受体的正变构调节物，EC50 值为 1μM。 靶点 mGlu4 Receptor 1μM (EC50)   体外研究 In the rat mGlu4 PAM in vitro assay the EC50 of TCN238 (Compound 11) is 1μM which is comparable to the human assay.TCN238 is screened in rat and human mGlu5 assays,the IC50 of 11 is >30μM on human mGlu5and >10μM on rat mGlu5.TCN238 is run in a receptor screening panel of 68 targets and no activity is observed at≥50% at 10μM for any of the receptors.In CaCo-2 cells,TCN238 is found to have good permeability with no apparent efflux issue. 体内研究 TCN238 is highly CNS penetrant with a concentration of 33.8μM 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 75mL/min/kg and TCN238 has a moderate volume of distribution (2.7L/kg) with a short mean residence time (0.6h) when dosed at 2mg/kg via intravenous injection.TCN238 is orally bioavailable and 30 min following administration of a 30mg/kg dose,the plasma concentration is found to be 11.6μM.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. 推荐实验方法(仅供参考) 动物实验:   Rats: TCN 238 is administered subcutaneously at a dose of 2mg/kg (volume of 0.5mL) four times in two days (morning and evening).Retrieval of the task is tested 30min after the first and third injections of TCN 238,and 5 days after the last injection of the substance.During the retrieval test the animals are placed to the start box,the door is opened, and the latent period of response is registered.
保存条件：-20℃

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