Reparixin is a noncompetitive allosteric inhibitor of IL-8 (CXCL8) activation of CXCR1 and CXCR2 chemokine receptors (IC50 = 1 and 100 nM, respectively). It blocks a number of activities related to IL-8 signaling, including leukocyte recruitment (IC50 = 1 nM) without affecting receptor activation induced by other CXCR1 and CXCR2 agonists.1 In spontaneously hypertensive rats, 5 mg/kg reparixin administered daily for three weeks was shown to reduce blood pressure by inhibiting hypertension-related mediators.2 It attenuates inflammatory responses and promotes recovery of function after traumatic lesion to the spinal cord.3 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.4
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