Retigabine
| 规格 | 价格 | 货期 | 数量 |
|---|---|---|---|
| 1mL(10 mM in DMSO) | ¥454.00 | 现货 | |
| 5mg | ¥422.00 | 现货 | |
| 10mg | ¥676.00 | 现货 | |
| 50mg | ¥1732.00 | 现货 | |
| 100mg | ¥3026.00 | 现货 |
特色产品
- 用于免疫印迹和质谱分析等后续操作
- 适用于30 KDa-130 KDa大小的蛋白
- 可将信号灵敏度提高100倍
- 同时保持稳定的特异性和分辨率
- 提供更高的转录效率并抑制免疫激活
- 使用5-moUTP和Cy5-utp修饰
产品描述
Retigabine is a positive allosteric modulator of KCNQ2-5 (KV7.2-7.5) ion channels, with EC50 values being 1.4, 1.6 and 5.2 μM for KCNQ3/5, KCNQ2/3 and KCNQ4, respectively. Retigabine is the first neuronal potassium channel opener used for the treatment of epilepsy. KCNQ2-5 channels, predominantly expressed in neurons, are important determinants of cellular excitability. The occurrence of human genetic mutations in KCNQ2/3 channels are associated with the syndrome of benign familial neonatal convulsions.
References:
1. Gunthorpe MJ, Large CH, Sankar R. The mechanism of action of retigabine (ezogabine), a first-in-class K+ channel opener for the treatment of epilepsy. Epilepsia, 2012, 53(3): 412-424.
2. Stas JI, Bocksteins E, Jensen CS, et al. The anticonvulsant retigabine suppresses neuronal KV2-mediated currents. Scientific Reports, 2016, 6: 35080.
3. De Sarro G, Di Paola ED, Conte G, et al. Influence of retigabine on the anticonvulsant activity of some antiepileptic drugs against audiogenic seizures in DBA/2 mice. Naunyn-Schmiedeberg's Archives of Pharmacology, 2001, 363(3): 330-336.
产品性质
| 物理外观 | A solid |
| CAS号 | 150812-12-7 |
| 分子式 | C16H18FN3O2 |
| 分子量 | 303.33 |
| 化学名称 | (E)-ethyl hydrogen (2-amino-4-((4-fluorobenzyl)amino)phenyl)carbonimidate |
| 溶解度 | insoluble in H2O; ≥11.1 mg/mL in EtOH with ultrasonic; ≥12.95 mg/mL in DMSO |
| SMILES | CCO/C(\O)=N/c(ccc(NCc(cc1)ccc1F)c1)c1N |
| 存储条件 | -20°C |
| 运输条件 | 蓝冰 |
产品应用 (实验数据来自文献,APExBIO并未验证,仅供参考)
IC50和靶点
| 生物活性描述 | 雷替加滨是一种新型抗惊厥药,已被证明能调节重组人 KCNQ2 和 KCNQ3 的 Kv7 钾通道电流。参考文献:Molecular Pharmacology. 2000; 58 (2), 253-262. |
| 靶点 | Potassium Channel |



沪公网安备 31011002003500