CLP257

产品编号 T14984Cas号 1181081-71-9

别名

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。

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产品编号 T14984Cas号 1181081-71-9

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生物活性

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.
靶点活性	KCC2:（EC50）616 nM
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].

化学信息

储存&溶解度

存储

Powder: -20°C for 3 years | In solvent: -80°C for 1 year | Shipping with blue ice.

溶解度信息

DMSO: 17.86 mg/mL (58.11 mM), Sonication is recommended.

溶液配制表

DMSO