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CLP257
本产品不向个人销售,仅用作科学研究,不用于任何人体实验及非科研性质的动物实验。
CLP257图片
CAS NO:1181081-71-9
包装与价格:
包装价格(元)
2 mg电议
5 mg电议
10 mg电议
25 mg电议
50 mg电议
100 mg电议
200 mg电议
1 mL*10 mM(in DMSO)电议

产品介绍
CLP257 是有效的K+-Cl- 协同转运蛋白 KCC2 选择性激活剂 (EC50: 616 nM)。它可减轻神经性疼痛大鼠的超敏反应,并在翻译后调节质膜 KCC2 蛋白周转。它在 KCC2 活性降低的神经元中恢复受损的 Cl- 转运。

产品描述

CLP257 is a selective K+-Cl– cotransporter KCC2 activator (EC50: 616 nM) and it is inactive against NKCC1, GABAA receptors, KCC1, KCC3 or KCC4. CLP257 alleviates hypersensitivity in rats with neuropathic painc and it also modulates plasmalemmal KCC2 protein turnover post-translationally. CLP257 restores impaired Cl– transport in neurons with diminished KCC2 activity.

体外活性

Oocyte pre-incubation with CLP257 (200 nM) increases KCC2 transport activity by 61%. However, it causes no change in other CCCs. There is no change in [Cl?]i in HEK293-cl cells when incubated with CLP257. CLP257 (50 μM) provokes< 0.2% of the effect of 5 μM muscimol in CHO cells transduced with recombinant α1β2γ2 GABAA receptors. Dose-dependent antagonism is also observed between CLP257 and the recently characterized KCC2 antagonist VU024055119 [1].

体内活性

CLP257 (100?mg/kg; i.p.; adult male rats) treatment causes an obvious increase in mechanical sensitivity [2].

Cas No.

1181081-71-9

分子式

C14H14FN3O2S

分子量

307.34

储存和溶解度

DMSO:17.86 mg/mL (58.11 mM),Need ultrasonic
Powder: -20°C for 3 years
In solvent: -80°C for 2 years