3-肟-6,7-二氯-1H-吲哚-2,3-二酮
| 中文名称 | 3-肟-6,7-二氯-1H-吲哚-2,3-二酮 |
|---|---|
| 中文同义词 | 3-肟-6,7-二氯-1H-吲哚-2,3-二酮;6,7-二氯-1H-吲哚-2,3-二酮-3-肟;化合物NS309;NS309,钙依赖性钾离子通道 SK/IK 的激活剂 |
| 英文名称 | NS309 |
| 英文同义词 | 1H-Indole-2,3-dione,6,7-dichloro-, 3-oxiMe;6,7-Dichloroindole-2,3-dione 3-oxime;6,7-Dichloroisatin 3-oxime;6,7-Dichloro-3-(hydroxyiMino)indolin-2-one;NS309;NS 309;NS-309;6,7-Dichloro-1H-indole-2,3-dione3-oxime;NS 309; NS-309;(Z)-6,7-dichloro-3-(hydroxyimino)indolin-2-one |
| CAS号 | 18711-16-5 |
| 分子式 | C8H4Cl2N2O2 |
| 分子量 | 231.04 |
| EINECS号 | |
| 相关类别 | 膜转运/离子通道;定制化学品;离子通道;膜转运 |
| Mol文件 | 18711-16-5.mol |
| 结构式 |  |
3-肟-6,7-二氯-1H-吲哚-2,3-二酮 性质
| 熔点 | 190-192℃ |
|---|---|
| 储存条件 | 2-8°C |
| 溶解度 | 二甲基亚砜：~22 mg/mL |
| 形态 | 固体 |
| 颜色 | 粘黄色 |
NS309 是一种有效、选择性的钙依赖性钾离子通道 SK/IK (Ca2+-activated SK/IK potassium channels) 的激活剂，但在 BK 通道上没有活性。
EC50: 0.62 µM (SK2), 0.3 μM (SK3), ∼20 nM (K Ca 3.1/SK4), ∼600 nM (K Ca 2/SK channels), 10 nM (hIK)
NS309 (40 nM) activates both hSK3 and hIK channels, with the largest effect on hIK channels (8.5-fold increase in current compares to 1.9-fold increase in current for hSK3 channels).
NS309 (10 μM) significantly increases the whole cell SK currents and hyperpolarized detrusor smooth muscle (DSM) cells resting membrane potential.
NS309 inhibits the spontaneous phasic contraction amplitude, force, frequency, duration and tone of isolated DSM strips in a concentration-dependent manner.
NS309 (2 mg/kg; i.p.) protects against SCI/R in rabbits.
| Animal Model: | Adult New Zealand white rabbits (2.5-3.0 kg) |
| Dosage: | 2 mg/kg |
| Administration: | Intraperitoneal injection |
| Result: | Significantly improved neurological outcome of SCI/R challenged rabbits. |