1. Membrane Transporter/Ion Channel
  2. Potassium Channel
  3. CLP257

CLP257 

Cat. No.: HY-110143
Handling Instructions

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.

For research use only. We do not sell to patients.

CLP257 Chemical Structure

CLP257 Chemical Structure

CAS No. : 1181081-71-9

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Based on 1 publication(s) in Google Scholar

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Description

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].

In Vivo

CLP257 (100 mg/kg; intraperitoneal injection; adult male rats) treatment induced a significant increase in mechanical sensitivity[2].

Animal Model: Adult male rats (300 g) injected with Morphine[2]
Dosage: 100 mg/kg
Administration: Intraperitoneal injection
Result: Induced a significant increase in mechanical sensitivity.
Molecular Weight

307.34

Formula

C₁₄H₁₄FN₃O₂S

CAS No.

1181081-71-9

SMILES

O=C1N=C(N2CCCCN2)S/C1=C\C3=CC=C(F)C=C3O

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Room temperature in continental US; may vary elsewhere.

Storage

Please store the product under the recommended conditions in the Certificate of Analysis.

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Keywords:

CLP257CLP 257CLP-257Potassium ChannelKcsAKCC2antihyperalgesicmechanicalsensitivityneuropathicplasmamembranepost-translationallyhypersensitivityInhibitorinhibitorinhibit

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CLP257
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