Reparixin is a noncompetitive allosteric inhibitor of IL-8 (CXCL8) activation of CXCR1 and CXCR2 chemokine receptors (IC50s = 1 and 100 nM, respectively).{28557} It blocks a range of activities related to IL-8 signaling, including leukocyte recruitment (IC50 = 1 nM) and other inflammatory responses, without affecting receptor activation induced by other CXCR1 and CXCR2 agonists.{28557} In spontaneously hypertensive rats, 5 mg/kg reparixin administered daily for three weeks was shown to reduce blood pressure by inhibiting hypertension-related mediators, IL-8, 12-lipoxygenase, and endothelin-1.{28553} Reparixin blockade (100 nM) of CXCR1 has also been used to deplete a cancer stem cell population in human breast cancer cell lines in vitro.{28554}
产品描述
A noncompetitive allosteric inhibitor of IL-8/CXCL8 activation of CXCR1 and CXCR2 chemokine receptors (IC50s = 1 and 100 nM, respectively); blocks IL-8-induced leukocyte recruitment (IC50 = 1 nM) and other inflammatory responses, without affecting receptor activation induced by other CXCR1 and CXCR2 agonists; at 100 nM has been used to deplete a cancer stem cell population in human breast cancer cell lines in vitro
