18711-16-5
中文名稱
3-肟-6,7-二氯-1H-吲哚-2,3-二酮
英文名稱
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 結構式
基本信息
中文別名
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
英文別名
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
常見問題列表
生物活性
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。靶點
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)
體外研究
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.
體內(nèi)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. |