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Reparixin
Cat No.
CEI-1496
Product Overview
Reparixin is a non-competitive allosteric inhibitor of CXCR1/2.CXCR is a 7-transmembrane G protein-coupled receptor. CXCR plays a critical role in the development of different models of ALI Following engagement of this receptor, the Gbg-complex dissociates from the Gai-subunit and can activate phosphoinositide-3 kinase, different subtypes of phospholipase C and P-Rex-1.The downstream effectors of these molecules initiate a broad range of functional responses, including arrest from rolling, cytoskeletal rearrangement, cell polarization, chemotaxis, degranulation and respiratory burst. Reperixin, specifically blocks CXCR1/2-mediated mouse and human neutrophil migration in vitro without affecting other receptors. Reparixin reduces ligand binding to human CXCR1 and CXCR2, calcium influx and downstream signalling in response to human CXCL8 and neutrophil recruitment into the liver in a mouse model of ischaemia-reperfusion injury. Reparixin reduced neutrophil recruitment and liver damage by approximately 30% and 80% in a model of ischaemiareperfusion injury. Reparixin reduced oligodendrocyte apoptosis, migration to the injury site of neutrophils and ED-1-positive cells. The best beneficial outcome of reparixin treatment will require 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 μg/ml. Methylprednisolone are used as a reference drug, and such treatment reduced cytokine production but failed to affect the rate of hind limb recovery.
CAS No.
266359-83-5
Molecular Weight
283.39
Purity
0.9987
Storage
Store at -20°C
Synonyms
Repertaxin; DF 1681Y
Targets
CXCL8 receptor; CXCR1/CXCR2 activation
Molecular Formula
C14H21NO3S
Chemical Name
(2R)-2-[4-(2-methylpropyl)phenyl]-N-methylsulfonylpropanamide
Solubility
Soluble in DMSO
Shipping Conditions
Evaluation sample solution: ship with blue ice. All other available size: ship with RT, or blue ice upon request
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