化合物CLP257 T14984

Product Introduction
Bioactivity


英文名: CLP257

描述: 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。

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].

存储条件: Powder: -20°C for 3 years | In solvent: -80°C for 1 year

溶解度: DMSO : 17.86 mg/mL (58.11 mM)


关键字: Inhibitor | post-translationally | hypersensitivity | plasma | Potassium Channel | neuropathic | antihyperalgesic | CLP-257 | CLP 257 | membrane | KcsA | mechanical | sensitivity | KCC2 | CLP257 | inhibit

相关产品: APD668 | Mitiglinide calcium hydrate | Hydroxyhexamide | H3B-120 | Clofilium tosylate | Phenformin hydrochloride | Vm24-toxin | DPO-1 | AmmTX3 TFA | Dofetilide

相关库: Ion Channel Inhibitor Library | Anti-Cancer Compound Library | Bioactive Compounds Library Max | Bioactive Compound Library

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