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CLP257
🥰Excellent
Catalog No. T14984Cas No. 1181081-71-9
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.
CLP257
🥰Excellent
Purity: 98.13%
Catalog No. T14984Cas No. 1181081-71-9
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 | 36 € | In Stock | |
| 2 mg | 51 € | In Stock | |
| 5 mg | 84 € | In Stock | |
| 10 mg | 135 € | In Stock | |
| 25 mg | 283 € | In Stock | |
| 50 mg | 465 € | In Stock | |
| 100 mg | 686 € | In Stock |
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Purity:98.13%
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All TargetMol products are for research purposes only and cannot be used for human consumption. We do not provide products or services to individuals. Please comply with the intended use and do not use TargetMol products for any other purpose.Product Introduction
Bioactivity
Chemical Properties
| 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) |
Storage & Solubility Information
| Storage | Powder: -20°C for 3 years | In solvent: -80°C for 1 year | Shipping with blue ice. | ||||||||||||||||||||||||||||||
| Solubility Information | DMSO: 17.86 mg/mL (58.11 mM), Sonication is recommended. | ||||||||||||||||||||||||||||||
Solution Preparation Table | |||||||||||||||||||||||||||||||
DMSO
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(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.Preparation method for in vivo formula: Take 50 μL DMSO main solution, add 300 μLPEG300 mix well and clarify, then add 50 more μL Tween 80, mix well and clarify, then add 600 more μLddH2O mix well and clarify
main solution, add 300 μLPEG300 mix well and clarify, then add 50 more μL Tween 80, mix well and clarify, then add 600 more μLddH2O mix well and clarifyFor Reference Only. Please develop an appropriate dissolution method based on your laboratory animals and route of administration.
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