CLP257
CAS No. : 1181081-71-9
| Size | Price | Stock |
|---|---|---|
| 5mg | $110 | In-stock |
| 10mg | $176 | In-stock |
| 25mg | $363 | In-stock |
| 50mg | $605 | In-stock |
| 100mg | $1045 | In-stock |
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| 500 mg | Get quote | |
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| Cat. No. : | HY-110143 |
| M.Wt: | 307.34 |
| Formula: | C14H14FN3O2S |
| Purity: | >98 % |
| Solubility: | DMSO : 17.86 mg/mL (ultrasonic) |
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]. IC50 & Target:EC50: 616 nM (KCC2)[1] 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[1].
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