3-肟-6,7-二氯-1H-吲哚-2,3-二酮
| 中文名稱 | 3-肟-6,7-二氯-1H-吲哚-2,3-二酮 |
|---|---|
| 中文同義詞 | 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,鈣依賴性鉀離子通道 SK/IK 的激活劑;NS309,K+ CHANNEL活化劑 |
| 英文名稱 | NS309 |
| 英文同義詞 | 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號 | 18711-16-5 |
| 分子式 | C8H4Cl2N2O2 |
| 分子量 | 231.04 |
| EINECS號 | |
| 相關(guān)類別 | 膜轉(zhuǎn)運/離子通道;定制化學品;離子通道;膜轉(zhuǎn)運 |
| Mol文件 | 18711-16-5.mol |
| 結(jié)構(gòu)式 |  |
3-肟-6,7-二氯-1H-吲哚-2,3-二酮 性質(zhì)
| 熔點 | 190-192℃ |
|---|---|
| 儲存條件 | 2-8°C |
| 溶解度 | 二甲基亞砜：~22 mg/mL |
| 形態(tài) | 固體 |
| 顏色 | 粘黃色 |
NS309 是一種有效、選擇性的鈣依賴性鉀離子通道 SK/IK (Ca2+-activated SK/IK potassium channels) 的激活劑，但在 BK 通道上沒有活性。
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. |