2 years -20°C Powder, 2 weeks 4°C in DMSO, 6 months -80°C in DMSO
生物活性
Description
In Vivo
In Vitro
化合物的使用
Kinase Assay
Cell Assay
Animal Administration
参考文献
Reparixin(DF 1681Y) is an inhibitor of CXCL8 receptor, also inhibit CXCR1 and CXCR2 activation, which has been shown to attenuate inflammatory responses in various injury models.
in vitro: 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.
in vivo: 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.
