| Bioactivity | CLP257 is a selective K+-Cl− cotransporter KCC2 activator with an EC50 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[1][2]. | ||||||
| Target | EC50: 616 nM (KCC2) | ||||||
| Invitro | 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[1]. | ||||||
| Name | CLP257 | ||||||
| CAS | 1181081-71-9 | ||||||
| Formula | C14H14FN3O2S | ||||||
| Molar Mass | 307.34 | ||||||
| Appearance | Solid | ||||||
| Transport | Room temperature in continental US; may vary elsewhere. | ||||||
| Storage |
*该产品在溶液状态不稳定，建议您现用现配，即刻使用。 |
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| Reference | [1]. Gagnon M, et al. Chloride extrusion enhancers as novel therapeutics for neurological diseases. Nat Med. 2013 Nov;19(11):1524-8. |