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Flucopride (Compound 4a) 作为一种有效的AChE抑制剂 (IC50: 24 nM),具备部分 5-HT4R 激动功能 (在 (h)5-HT4R 上的 Ki 值为 9.6 nM)。此外,Flucopride 在COS-7细胞中促进了表达 (h)5-HT4R 的 APP 非淀粉样变性加工 (EC50: 23.0 nM)。实验指出,Flucopride 在胃肠道 (GIT) 和血脑屏障 (BBB) 均显示出良好的渗透性,这一特性通过PAMPA实验得以证实。
Flucopride (Compound 4a) 作为一种有效的AChE抑制剂 (IC50: 24 nM),具备部分 5-HT4R 激动功能 (在 (h)5-HT4R 上的 Ki 值为 9.6 nM)。此外,Flucopride 在COS-7细胞中促进了表达 (h)5-HT4R 的 APP 非淀粉样变性加工 (EC50: 23.0 nM)。实验指出,Flucopride 在胃肠道 (GIT) 和血脑屏障 (BBB) 均显示出良好的渗透性,这一特性通过PAMPA实验得以证实。
规格 | 价格 | 库存 | 数量 |
---|---|---|---|
10 mg | 询价 | 10-14周 | |
50 mg | 询价 | 10-14周 |
产品描述 | Flucopride (Compound 4a) acts as an acetylcholinesterase inhibitor (AChE) with an IC50 value of 24 nM and serves as a partial agonist for the human 5-HT4 receptor (5-HT4R) with a Ki of 9.6 nM for (h)5-HT4R. It promotes non-amyloidogenic processing of APP in COS-7 cells transiently expressing (h)5-HT4R with an EC50 of 23.0 nM. Flucopride is also likely to exhibit significant gastrointestinal tract (GIT) penetration and blood-brain barrier (BBB) permeability, as determined in PAMPA experiments. |
靶点活性 | AChE:24nM(IC50), 5-HT4C receptor (human):9.6nM(ki) |
分子量 | 376.51 |
分子式 | C22H33FN2O2 |
CAS No. | 1639925-34-0 |
存储 | Powder: -20°C for 3 years | In solvent: -80°C for 1 year | Shipping with blue ice. |
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