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ICA-27243 是选择性的,口服有效的 KCNQ2/Q3钾通道开放剂,EC50为 0.38 μM。对 KCNQ4 和 KCNQ3/Q5 的激活效果较差。它具有抗惊厥和抗癫痫作用。
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ICA-27243 是选择性的,口服有效的 KCNQ2/Q3钾通道开放剂,EC50为 0.38 μM。对 KCNQ4 和 KCNQ3/Q5 的激活效果较差。它具有抗惊厥和抗癫痫作用。
规格 | 价格 | 库存 | 数量 |
---|---|---|---|
1 mg | ¥ 248 | 现货 | |
2 mg | ¥ 355 | 现货 | |
5 mg | ¥ 579 | 现货 | |
10 mg | ¥ 892 | 现货 | |
25 mg | ¥ 1,780 | 现货 | |
50 mg | ¥ 2,670 | 现货 | |
100 mg | ¥ 3,890 | 现货 | |
1 mL x 10 mM (in DMSO) | ¥ 637 | 现货 |
产品描述 | ICA-27243 is less effective at activating KCNQ4 and KCNQ3/Q5. ICA-27243 is a potent and orally active KCNQ2/Q3 potassium channel opener (EC50: 0.38 μM). ICA-27243 also has antiepileptic and anticonvulsant effects. |
靶点活性 | KCNQ2/Q3 K+ channel:0.38 μM (EC50) |
体外活性 | ICA-27243 increases both 86Rb+ efflux (EC50 = 0.2 μM) and whole-cell currents in Chinese hamster ovary cells stably expressing heteromultimeric KCNQ2/Q3 channels (EC50 = 0.4 μM). ICA-27243 produces membrane potential hyperpolarization that could be prevented by coadministration with the M-current inhibitors XE-991 and Linopirdine, in SH-SY5Y human neuroblastoma cells [1]. |
体内活性 | In the mouse maximal electroshock epilepsy model, ICA-27243 (1-100 mg/kg; oral administration; male CD-1 mice) has anticonvulsant activity (ED50: 8.4 mg/kg)[1]. |
分子量 | 268.65 |
分子式 | C12H7ClF2N2O |
CAS No. | 325457-89-4 |
Smiles | Fc1ccc(cc1F)C(=O)Nc1ccc(Cl)nc1 |
密度 | 1.476 g/cm3 (Predicted) |
存储 | Powder: -20°C for 3 years | In solvent: -80°C for 1 year | Shipping with blue ice. | |||||||||||||||||||||||||||||||||||
溶解度信息 | DMSO: 247 mg/mL (919.41 mM), Sonication is recommended. | |||||||||||||||||||||||||||||||||||
溶液配制表 | ||||||||||||||||||||||||||||||||||||
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