Repertaxin L-赖氨酸盐

  • 化学数据
CAS号 266359-93-7 货号 BCP30625
中文名 Repertaxin L-赖氨酸盐
英文名 Repertaxin L-lysine salt
中文别名
英文别名 Reparixin L-lysine;Repertaxin L-lysine salt;(2S)-2,6-diaminohexanoic acid;(2R)-2-[4-(2-methylpropyl)phenyl]-N-methylsulfonylpropanamide;
分子式 C14H21NO3S.C6H14N2O2 分子量 429.58
  • 用途
生物活性 The efficacy of RPX (tested in a wide range of concentrations (1-1000 nM)) was lower in cells expressing Ile43Val CXCR1 mutant (IC50 values of 0.0056 and 0.08 uM for CXCR1 weight and CXCR1 Ile43Val, respectively). Treatment with reparixin significantly counteracts secondary degeneration by reducing oligodendrocyte apoptosis, migration to the injury site of neutrophils and ED-1-positive cells. The best beneficial outcome of reparixin treatment required 7-day administration either by i.p. route (15 mg/kg) or subcutaneous infusion via osmotic pumps (10 mg/kg), reaching a steady blood level of 8 microg/ml. Reparixin effectively decreased systolic blood pressure and increased the blood flow. The thoracic aorta wall thickness was significantly decreased in SHR-R compared to SHR-N. Pre-treatment with reparixin reduced the motor deficits observed in this model of ischemia and reperfusion. Myeloperoxidase activity and IL-iβ were reduced in the reparixin-treated group. Histological analysis revealed that ischemic injury was also attenuated by reparixin pre-treatment.
信号通路 GPCR/G Protein 
靶 点 CXCR 

结构式

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