A KCC2 cotransporter activator (EC50 = 616 nM for chloride transport in NG108-cl cells); selective for KCC2 over GABAA receptors at 50 µM; increases the rate of chloride accumulation in spinal slices isolated from a rat model of PNI and BDNF control slices; increases mechanical withdrawal thresholds in a rat model of PNI and reverses morphine-induced hyperalgesia in rats at 100 mg/kg

CLP 257 – 1 mg

Brand:
Cayman
CAS:
1181081-71-9
Storage:
-20
UN-No:
Non-Hazardous - /

CLP 257 is a K+/Cl- cotransporter 2 (KCC2) activator.{57069,57070,57071} It induces chloride transport in NG108-cl cells that endogenously express low levels of KCC2 (EC50 = 616 nM).{57069} It is selective for KCC2 over GABAA receptors at 50 µM. CLP 257 (25 µM) increases the rate of chloride accumulation in spinal slices isolated from a rat model of peripheral nerve injury and BDNF control slices, which exhibit reduced levels of KCC2. In vivo, CLP 257 (100 mg/kg) increases mechanical and withdrawal thresholds in a rat model of peripheral nerve injury and reverses morphine-induced hyperalgesia in rats.{57069,57072}  

 

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SKU: 30948 - 1 mg Category:

Description

A KCC2 cotransporter activator (EC50 = 616 nM for chloride transport in NG108-cl cells); selective for KCC2 over GABAA receptors at 50 µM; increases the rate of chloride accumulation in spinal slices isolated from a rat model of PNI and BDNF control slices; increases mechanical withdrawal thresholds in a rat model of PNI and reverses morphine-induced hyperalgesia in rats at 100 mg/kg

Formal name: (5Z)-5-[(4-fluoro-2-hydroxyphenyl)methylene]-2-(tetrahydro-1(2H)-pyridazinyl)-4(5H)-thiazolone

Synonyms: 

Molecular weight: 307.3

CAS: 1181081-71-9

Purity: ≥98%

Formulation: A solid

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