化合物CLP257
| 中文名称 | 化合物CLP257 |
|---|---|
| 中文同义词 | 化合物 T14984;化合物CLP257;CLP 257,KCC2激活剂;(Z)-5-(4-氟-2-羟基苄亚基)-2-(四氢哒嗪-1(2H)-基)噻唑-4(5H)-酮 |
| 英文名称 | CLP257 |
| 英文同义词 | (5Z)-5-[(4-Fluoro-2-hydroxyphenyl)methylene]-2-(tetrahydro-1-(2H)-pyridazinyl)-4(5H)-thiazolone;CLP257;4(5H)-Thiazolone, 5-[(4-fluoro-2-hydroxyphenyl)methylene]-2-(tetrahydro-1(2H)-pyridazinyl)-, (5Z)-;Inhibitor,post-translationally,hypersensitivity,plasma,Potassium Channel,neuropathic,antihyperalgesic,CLP 257,membrane,KcsA,mechanical,sensitivity,CLP-257,CLP257,KCC2,inhibit;(Z)-5-(4-fluoro-2-hydroxybenzylidene)-2-(tetrahydropyridazin-1(2H)-yl)thiazol-4(5H)-one |
| CAS号 | 1181081-71-9 |
| 分子式 | C14H14FN3O2S |
| 分子量 | 307.34 |
| EINECS号 | |
| 相关类别 | |
| Mol文件 | 1181081-71-9.mol |
| 结构式 |  |
化合物CLP257 性质
| 沸点 | 473.3±55.0 °C(Predicted) |
|---|---|
| 密度 | 1.50±0.1 g/cm3(Predicted) |
| 储存条件 | 2-8°C |
| 溶解度 | 二甲基亚砜：20mg/mL |
| 酸度系数(pKa) | 7.23±0.40(Predicted) |
| 形态 | 粉末 |
| 颜色 | 白色至黄色至浅棕色 |
EC50: 616 nM (KCC2)
There is no change in [Cl − ] i in HEK293-cl cells when incubated with CLP257, indicating inactivity on NKCC1, KCC1, KCC3 or KCC4. Oocyte pre-incubation with CLP257 (200 nM) increases KCC2 transport activity by 61%, but causes no change in other CCCs. Functional, dose-dependent antagonism is also observed between CLP257 and the recently characterized KCC2 antagonist VU024055119. CLP257 (50 μM) provokes < 0.2% of the effect of 5 μM muscimol in CHO cells transduced with recombinant α1β2γ2 GABAA receptors, indicating negligible agonist activity of CLP257 on GABAA receptors.
CLP257 (100 mg/kg; intraperitoneal injection; adult male rats) treatment induced a significant increase in mechanical sensitivity.
| Animal Model: | Adult male rats (300 g) injected with Morphine |
| Dosage: | 100 mg/kg |
| Administration: | Intraperitoneal injection |
| Result: | Induced a significant increase in mechanical sensitivity. |
安全信息
| 更新日期 | 产品编号 | 产品名称 | CAS号 | 包装 | 价格 |
|---|---|---|---|---|---|
| 2024/04/30 | HY-110143 | CLP257 | 1 mg | 400元 | |
| 2024/04/30 | HY-110143 | CLP257 | 1181081-71-9 | 5mg | 1000元 |