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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.

| Pack Size | Price | Availability | Quantity | 
|---|---|---|---|
| 1 mg | $38 | In Stock | |
| 2 mg | $54 | In Stock | |
| 5 mg | $89 | In Stock | |
| 10 mg | $143 | In Stock | |
| 25 mg | $298 | In Stock | |
| 50 mg | $490 | In Stock | |
| 100 mg | $723 | In Stock | 
| Description | 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. | 
| Targets&IC50 |  KCC2:(EC50)616 nM | 
| In vitro | 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]. | 
| In vivo | CLP257 (100?mg/kg; i.p.; adult male rats) treatment causes an obvious increase in mechanical sensitivity [2]. | 
| Molecular Weight | 307.34 | 
| Formula | C14H14FN3O2S | 
| Cas No. | 1181081-71-9 | 
| Smiles | Oc1cc(F)ccc1\C=C1/SC(=NC1=O)N1CCCCN1 | 
| Relative Density. | 1.50 g/cm3 (Predicted) | 
| Color | Yellow | 
| Appearance | Solid | 
| Storage | Powder: -20°C for 3 years | In solvent: -80°C for 1 year | Shipping with blue ice/Shipping at ambient temperature. | ||||||||||||||||||||||||||||||
| Solubility Information | DMSO: 17.86 mg/mL (58.11 mM), Sonication is recommended.  | ||||||||||||||||||||||||||||||
| Solution Preparation Table | |||||||||||||||||||||||||||||||
| DMSO 
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 For example, your dosage is 10 mg/kg Each animal weighs 20 g, and the dosage volume is 100 μL .
For example, your dosage is 10 mg/kg Each animal weighs 20 g, and the dosage volume is 100 μL .  A total of 10 animals were administered, and the formula you used is 5%
 A total of 10 animals were administered, and the formula you used is 5%  DMSO+30% PEG300+5% Tween 80+60% Saline/PBS/ddH2O. So your working solution concentration is 2 mg/mL。
DMSO+30% PEG300+5% Tween 80+60% Saline/PBS/ddH2O. So your working solution concentration is 2 mg/mL。 (mother liquor concentration of 40 mg/mL), if you need to configure a concentration that exceeds the solubility of the product, please contact us first.
 (mother liquor concentration of 40 mg/mL), if you need to configure a concentration that exceeds the solubility of the product, please contact us first. main solution, add 300 μLPEG300
 main solution, add 300 μLPEG300 mix well and clarify, then add 50 more μL Tween 80, mix well and clarify, then add 600 more μLSaline/PBS/ddH2O
 mix well and clarify, then add 50 more μL Tween 80, mix well and clarify, then add 600 more μLSaline/PBS/ddH2O mix well and clarify
 mix well and clarify
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