Reparixin L-lysine salt - CAS 266359-93-7
Catalog number: 266359-93-7
Category: Inhibitor
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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.
Repertaxin L-lysine salt
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1.Species differences in the pharmacokinetics and metabolism of reparixin in rat and dog.
Midgley I1, Fitzpatrick K, Wright SJ, John BA, Peard AJ, Major RM, Holding JD, McBurney A, Anacardio R, Novellini R, Ferrari MP. Xenobiotica. 2006 May;36(5):419-40.
The pharmacokinetics and metabolism of reparixin (formerly repertaxin), a potent and specific inhibitor of the chemokine CXCL8, were investigated in rats and dogs after intravenous administration of [14C]-reparixin L-lysine salt. Protein binding of reparixin was investigated in vitro in rat, dog, rabbit, cynomolgus monkey and human plasma. Plasma protein binding of reparixin was >99% in the laboratory animals and humans up to 50 microg ml-1, but lower at higher concentrations. Although radioactivity was rapidly distributed into rat tissues, Vss was low (about 0.15 l kg-1) in both rat and dog. Nevertheless, reparixin was more rapidly eliminated in rats (t1/2 approximately 0.5 h) than in dogs (t1/2 approximately 10 h). Systemic exposure in dog was due primarily to parent drug, but metabolites played a more prominent role in rat. Oxidation of the isobutyl side-chain was the major metabolic pathway in rat, whereas hydrolysis of the amide bond predominated in dog.
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