18711-16-5
中文名称
3-肟-6,7-二氯-1H-吲哚-2,3-二酮
英文名称
NS309
CAS
18711-16-5
分子式
C8H4Cl2N2O2
分子量
231.04
MOL 文件
18711-16-5.mol
更新日期
2024/06/03 10:24:05
18711-16-5 结构式
基本信息
中文别名
6,7-二氯-1H-吲哚-2,3-二酮-3-肟3-肟-6,7-二氯-1H-吲哚-2,3-二酮
英文别名
NS 309NS-309
NS309
NS 309
NS-309
6,7-Dichloroisatin 3-oxime
6,7-Dichloroindole-2,3-dione 3-oxime
6,7-Dichloro-1H-indole-2,3-dione3-oxime
6,7-Dichloro-3-(hydroxyiMino)indolin-2-one
1H-Indole-2,3-dione,6,7-dichloro-, 3-oxiMe
常见问题列表
生物活性
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。靶点
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)
体外研究
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.
体内研究
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. |