化合物CLP257
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- CAS号:
- 1181081-71-9
- 英文名:
- CLP257
- 英文别名:
- CLP257;(Z)-5-(4-fluoro-2-hydroxybenzylidene)-2-(tetrahydropyridazin-1(2H)-yl)thiazol-4(5H)-one;(5Z)-5-[(4-Fluoro-2-hydroxyphenyl)methylene]-2-(tetrahydro-1-(2H)-pyridazinyl)-4(5H)-thiazolone;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
- 中文名:
- 化合物CLP257
- 中文别名:
- 化合物CLP257;化合物 T14984;CLP 257,KCC2激活剂
- CBNumber:
- CB94667761
- 分子式:
- C14H14FN3O2S
- 分子量:
- 307.34
- MOL File:
- 1181081-71-9.mol
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化合物CLP257化学性质
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沸点:
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473.3±55.0 °C(Predicted)
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密度:
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1.50±0.1 g/cm3(Predicted)
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储存条件:
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2-8°C
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溶解度:
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DMSO: 20 mg/ml
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酸度系数(pKa):
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7.23±0.40(Predicted)
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形态:
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powder
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颜色:
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white to yellow to light brown
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化合物CLP257性质、用途与生产工艺
CLP257 是一种选择性 K+-Cl− 共转运蛋白 KCC2 激活剂，EC50 为 616 nM。CLP257 对 NKCC1，GABAA 受体，KCC1，KCC3 和 KCC4 无活性。CLP257 恢复了 KCC2 活性减弱的神经元 Cl− 转运受损，并减轻了神经性疼痛大鼠的超敏反应。CLP257 在翻译后调节血浆中的 KCC2 蛋白转化。
There is no change in [Cl
−
]
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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.
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Animal Model:
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Adult male rats (300 g) injected with Morphine
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Dosage:
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100 mg/kg
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Administration:
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Intraperitoneal injection
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Result:
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Induced a significant increase in mechanical sensitivity.
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化合物CLP257
上下游产品信息
上游原料
下游产品
| 更新日期 | 产品编号 | 产品名称 | CAS编号 | 包装 | 价格 |
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| 2024/04/30 | HY-110143 | CLP257 | | 1 mg | 400元 |
| 2024/04/30 | HY-110143 | CLP257 | 1181081-71-9 | 5mg | 1000元 |
1181081-71-9, 化合物CLP257 相关搜索:
- 药靶配体
- CLP 257,KCC2激活剂
- 化合物CLP257
- 化合物 T14984
- 1181081-71-9
- (Z)-5-(4-fluoro-2-hydroxybenzylidene)-2-(tetrahydropyridazin-1(2H)-yl)thiazol-4(5H)-one
- Inhibitor,post-translationally,hypersensitivity,plasma,Potassium Channel,neuropathic,antihyperalgesic,CLP 257,membrane,KcsA,mechanical,sensitivity,CLP-257,CLP257,KCC2,inhibit
- 4(5H)-Thiazolone, 5-[(4-fluoro-2-hydroxyphenyl)methylene]-2-(tetrahydro-1(2H)-pyridazinyl)-, (5Z)-
- CLP257
- (5Z)-5-[(4-Fluoro-2-hydroxyphenyl)methylene]-2-(tetrahydro-1-(2H)-pyridazinyl)-4(5H)-thiazolone