化合物CLP-290 T5444

Product Introduction
Bioactivity


英文名: CLP290

描述: CLP-290 是一种神经特异性 K+-Cl−共转运体 KCC2的口服激活剂，在多种神经和精神疾病方面具有研究潜力。CLP290 能显著降低 STZ 大鼠的血液中 AVP 和血糖水平。

动物实验: Morphine sulfate (50 mg/ml) was diluted in saline sterile solution immediately before injection.?Morphine or saline were subcutaneously injected twice a day (10 mg/kg;?9 a.m. 6 p.m.) in na?ve adult rats.?The KCC2 enhancer CLP257 and its carbamate pro-drug CLP290 were freshly diluted in 20% 2-hydroxypropyl-β-cyclodextrin (HPCD) prior injection.?CLP257 or vehicle were delivered intraperitoneally after 7 8 days of morphine or saline, as described (100 mg/kg).?CLP290 or vehicle were delivered orally by gavage twice a day for the whole duration of the morphine/saline treatment (100 mg/kg).

体内活性: In vivo co-treatment with morphine and oral CLP290 prevented membrane KCC2 downregulation in SDH neurons.?Concurrently, co-treatment with CLP290 significantly mitigated MIH and acute administration of CLP257 in established MIH restored normal nociceptive behavior.

存储条件: Powder: -20°C for 3 years | In solvent: -80°C for 1 year

溶解度: DMSO : 12 mg/mL (29.67 mM)


关键字: inhibit | Potassium Channel | CLP290 | Inhibitor | CLP 290 | KcsA

相关产品: Butamben | ICA | Hongotoxin-1 | Celivarone | Ropivacaine hydrochloride monohydrate | Chlorzoxazone | Kv2-IN-A1 | BDS-I | RL648_81 | Stauntosaponin A

相关库: Ion Channel Inhibitor Library | Potassium Channel Blocker Library | Anti-Cancer Compound Library | Membrane Protein-targeted Compound Library | Bioactive Compounds Library Max | Orally Active Compound Library | Covalent Inhibitor Library | Bioactive Compound Library

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