CLP 257

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.Formal Name: (5Z)-5-[(4-fluoro-2-hydroxyphenyl)methylene]-2-(tetrahydro-1(2H)-pyridazinyl)-4(5H)-thiazolone. CAS Number: 1181081-71-9. Molecular Formula: C14H14FN3O2S. Formula Weight: 307.3. Purity: >98%. Formulation: (Request formulation change), A solid. Solubility: DMSO: 20 mg/ml. SMILES: FC1=CC=C(/C=C2SC(N3NCCCC3)=NC\2=O)C(O)=C1. InChi Code: InChI=1S/C14H14FN3O2S/c15-10-4-3-9(11(19)8-10)7-12-13(20)17-14(21-12)18-6-2-1-5-16-18/h3-4,7-8,16,19H,1-2,5-6H2/b12-7-. InChi Key: SKCADXVKQRCWTR-GHXNOFRVSA-N.