CLP 257 is a K+/Cl- cotransporter 2 (KCC2) activator. It induces chloride transport in NG108-cl cells that endogenously express low levels of KCC2 (EC50 = 616 nM). 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.
CLP 257 is a K+/Cl- cotransporter 2 (KCC2) activator. It induces chloride transport in NG108-cl cells that endogenously express low levels of KCC2 (EC50 = 616 nM). 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.
Shipping & Handling
Shipped In
Room Temperature in continental US; may vary elsewhere
Safety & Storage
Storage Temperature
-20°C
Safety Statement
WARNING This product is not for human or veterinary use. Information provided in the product description is from published literature. Due to the nature of scientific experimentation, your results (e.g., selectivity and effective concentrations) or specific application for this product may differ. If you have questions about how this product fits your application, please contact our technical support staff.
Room Temperature in continental US; may vary elsewhere
Safety & Storage
Storage Temperature
-20°C
Safety Statement
WARNING This product is not for human or veterinary use. Information provided in the product description is from published literature. Due to the nature of scientific experimentation, your results (e.g., selectivity and effective concentrations) or specific application for this product may differ. If you have questions about how this product fits your application, please contact our technical support staff.
Regulatory & Compliance
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We’re currently in BETA - Interested in joining? Let us know and we’ll get you set up with early access.