CLP257
目录号: PL09979 纯度: ≥99%
CAS No. :1181081-71-9
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中文名称
CLP257
中文别名
CLP 257
英文名称
CLP257
英文别名
CLP 257;(5Z)-5-[(4-Fluoro-2-hydroxyphenyl)methylene]-2-(tetrahydro-1-(2H)-pyridazinyl)-4(5H)-thiazolone;CLP257;SKCADXVKQRCWTR-GHXNOFRVSA-N;CLP257, >=98% (HPLC);(5Z)-2-(1,2-diazinan-1-yl)-5-[(4-fluoro-2-hydroxyphenyl)methylidene]-4,5-dihydro-1,3-thiazol-4-one;(5Z)-2-(Diazinan-1-yl)-5-[(4-fluoro-2-hydroxyphenyl)methylidene]-1,3-thiazol-4-one
Cas No.
1181081-71-9
分子式
C14H14FN3O2S
分子量
307.34
包装储存
Powder -20°C 3 years;4°C 2 years
产品详情
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。
生物活性
CLP257 is a selective K-Cl cotransporter KCC2 activator with an EC 50 of 616 nM. CLP257 is inactive against NKCC1, GABAA receptors, KCC1, KCC3 or KCC4. CLP257 restores impaired Cl transport in neurons with diminished KCC2 activity. CLP257 alleviates hypersensitivity in rats with neuropathic pain. CLP257 modulates plasmalemmal KCC2 protein turnover post-translationally.
性状
Solid
IC50 & Target[1][2]
EC50: 616 nM (KCC2)
体外研究(In Vitro)
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. has not independently confirmed the accuracy of these methods. They are for reference only.
运输条件
Room temperature in continental US; may vary elsewhere.
储存方式
Powder -20°C 3 years;4°C 2 years
参考文献
[1]. Gagnon M, et al. Chloride extrusion enhancers as novel therapeutics for neurological diseases. Nat Med. 2013 Nov;19(11):1524-8.
溶解度数据
In Vitro: DMSO : 17.86 mg/mL (58.11 mM; Need ultrasonic)配制储备液
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1:一般建议:溶解度为Medlife测试数据,可能与文献描述存在差异。这是由于生产工艺和批次不同产生的正常现象。为了使其更好的溶解,请用37℃加热试管并在超声波水浴中震动片刻。不同批次产品溶解度各有差异,仅做参考,具体以实验方案为准。

2:储存条件:粉末-20°C一般情况可以保存3年,溶于溶剂-80°C一般情况可以保存1年。不同产品及不同批次产品可能存在差异,请细致阅读产品信息,并辅助参考相关文献描述。

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