Reparixin is a noncompetitive allosteric inhibitor of IL-8 (CXCL8) activation of CXCR1 and CXCR2 chemokine receptors with IC50 of 1 and 100 nM, respectively. Reparixin effectively decreased systolic blood pressure and increased the blood flow. Treatment with reparixin significantly counteracts secondary degeneration by reducing oligodendrocyte apoptosis, migration to the injury site of neutrophils and ED-1-positive cells.
|Body Surface Area (m2)||0.007||0.025||0.15||0.05||0.02||0.5|
|Animal A (mg/kg) = Animal B (mg/kg) multiplied by||Animal B Km|
|Animal A Km|
For example, to modify the dose of resveratrol used for a mouse (22.4 mg/kg) to a dose based on the BSA for a rat, multiply 22.4 mg/kg by the Km factor for a mouse and then divide by the Km factor for a rat. This calculation results in a rat equivalent dose for resveratrol of 11.2 mg/kg.
Reparixin, an inhibitor of CXCR1 and CXCR2 receptor activation, attenuates blood pressure and hypertension-related mediators expression in spontaneously hypertensive rats.
Kim HY, et al. Biol Pharm Bull. 2011;34(1):120-7. PMID: 21212529.
Design of noncompetitive interleukin-8 inhibitors acting on CXCR1 and CXCR2.
Moriconi A, et al. J Med Chem. 2007 Aug 23;50(17):3984-4002. PMID: 17665889.
|Related CXCR Products|
AMD-070 is a potent and selective antagonist of CXCR4 with an IC50 value of 13 nM in a CXCR4 125I-SDF inhibition binding assay, and inhibits the replication of T-tropic HIV-1 (NL4.3 strain) in MT-4 cells and PBMCs.
GSK1325756 (Danirixin) is a non-peptide, high affinity, selective and reversible CXCR2 antagonist.
MSX-122 is a novel small molecule and partial CXCR4 antagonist, with potent inhibition of CXCR4/CXCL12 actions (IC50 = 10 nM).
SB225002 is a potent and selective non-peptide inhibitor of CXCR2 with IC50 of 22 nM and >150-fold selectivity over CXCR1 and four other 7-TMRs.
Plerixafor 8HCl (AMD3100 8HCl) is a chemokine receptor antagonist for CXCR4 and CXCL12-mediated chemotaxis with IC50 of 44 nM and 5.7 nM, respectively.
Products are for research use only. Not for human use. We do not sell to patients.
© Copyright 2010-2017 AbMole BioScience. All Rights Reserved.