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.
Cell Death Dis. 2020 May 29;11(5):405.
|Source||Cell Death & Disease (2020 May). Figure 3. Reparixin (Abmole Bioscience, US)|
|Cell Lines||Six-week-old BALB/c male nude mice|
|Incubation Time||once a day|
|Results||Interestingly, we found that using Reparixin alone could also inhibit the migration and invasion ability of HNSCC cells. These results suggested that Reparixin may block both the exogenous IL-8 and autocrine IL-8 of tumor 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 Compound A used for a mouse (20 mg/kg) to a dose based on the BSA for a rat, multiply 20 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 Compound A of 10 mg/kg.
|Solubility||DMSO: ≥ 25 mg/mL|
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|
LY2510924 is a potent and selective CXCR4 antagonist, which blocks SDF-1 binding to CXCR4 with IC50 of 0.079 nM.
Motixafortide (BL-8040) is an antagonist of CXCR4 with IC50 value of 1 nM.
ATI-2341 is a potent and functionally selective allosteric agonist of C-X-C chemokine receptor type 4 (CXCR4).
SX-682 is a potent and selective CXCR1/2 allosteric inhibitor, it may be useful for castration-resistant prostate cancer.
VUF11207 fumarate is a CXCR7 agonist and a high-potency CXCR7 ligand (pKi=8.1).
Products are for research use only. Not for human use. We do not sell to patients.
© Copyright 2010-2020 AbMole BioScience. All Rights Reserved.