|Description||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.|
|Synonyms||Repertaxin L-lysine salt|
AZ 10397767 is a potent CXCR2 antagonist (IC50 = 1 nM). It significantly reduced the numbers of infiltrating neutrophils into both in vitro and in vivo tumor mo...
Reparixin L-lysine salt
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 u...
Plerixafor is a chemokine receptor antagonist for CXCR4 and CXCL12-mediated chemotaxis with IC50 of 44 nM and 5.7 nM, respectively.
NVP CXCR2 20
Potent and selective CXCR2 antagonist
CXCR2-IN-1 is a CXCR2 antagonists (pIC50= 9.3) with favorable central nervous system penetration property (Br/Bl>0.45).
A novel, potent and non-competitive small molecule CXCR3 antagonist with Ki of 0.4 nM
A CXCR2 ligand
A small molecule antagonist for CXCR3