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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

CLP257

🥰Excellent
Purity: 99.5%
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 SizePriceUSA WarehouseGlobal WarehouseQuantity
1 mg$38In StockIn Stock
2 mg$54In StockIn Stock
5 mg$89In StockIn Stock
10 mg$143In StockIn Stock
25 mg$298In StockIn Stock
50 mg$490In StockIn Stock
100 mg$723In StockIn Stock
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In Stock Estimated shipping dateUSA Warehouse[1-2 days] Global Warehouse[5-7 days]
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Purity:99.5%
Appearance:Solid
Color:Yellow
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Product Introduction

Bioactivity
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].
Chemical Properties
Molecular Weight307.34
FormulaC14H14FN3O2S
Cas No.1181081-71-9
SmilesOc1cc(F)ccc1\C=C1/SC(=NC1=O)N1CCCCN1
Relative Density.1.50 g/cm3 (Predicted)
Storage & Solubility Information
StoragePowder: -20°C for 3 years | Shipping with blue ice/Shipping at ambient temperature.
Solubility Information
DMSO: 17.86 mg/mL (58.11 mM), Sonication is recommended.
In Vivo Formulation
10% DMSO+40% PEG300+5% Tween 80+45% Saline: 1 mg/mL (3.25 mM), Sonication is recommended.
Please add the solvents sequentially, clarifying the solution as much as possible before adding the next one. Dissolve by heating and/or sonication if necessary. Working solution is recommended to be prepared and used immediately. The formulation provided above is for reference purposes only. In vivo formulations may vary and should be modified based on specific experimental conditions.
Solution Preparation Table
DMSO
1mg5mg10mg50mg
1 mM3.2537 mL16.2686 mL32.5373 mL162.6863 mL
5 mM0.6507 mL3.2537 mL6.5075 mL32.5373 mL
10 mM0.3254 mL1.6269 mL3.2537 mL16.2686 mL
20 mM0.1627 mL0.8134 mL1.6269 mL8.1343 mL
50 mM0.0651 mL0.3254 mL0.6507 mL3.2537 mL

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Please enter your animal experiment information in the following box and click Calculate to obtain the stock solution preparation method and in vivo formula preparation method:
TargetMol | Animal experiments For example, if the intended dosage is 10 mg/kg for animals weighing 20 g , with a dosing volume of 100 μL per animal, TargetMol | Animal experiments and a total of 10 animals are to be administered, using a formulation of TargetMol | reagent 10% DMSO+ 40% PEG300+ 5% Tween 80+ 45% Saline/PBS/ddH2O , the resulting working solution concentration would be 2 mg/mL.
Stock Solution Preparation:

Dissolve 2 mg of the compound in 100 μL DMSOTargetMol | reagent to obtain a stock solution at a concentration of 20 mg/mL . If the required concentration exceeds the compound's known solubility, please contact us for technical support before proceeding.

Preparation of the In Vivo Formulation:

1) Add 100 μL of the DMSOTargetMol | reagent stock solution to 400 μL PEG300TargetMol | reagent and mix thoroughly until the solution becomes clear.

2) Add 50 μL Tween 80 and mix well until fully clarified.

3) Add 450 μL Saline,PBS or ddH2OTargetMol | reagent and mix thoroughly until a homogeneous solution is obtained.

This example is provided solely to demonstrate the use of the In Vivo Formulation Calculator and does not constitute a recommended formulation for any specific compound. Please select an appropriate dissolution and formulation strategy based on your experimental model and route of administration.
All co-solvents required for this protocol, includingDMSO, PEG300/PEG400, Tween 80, SBE-β-CD, and Corn oil, are available for purchase on the TargetMol website.
1 Enter information below:
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2 Enter the in vivo formulation:
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