Reparixin (L-Lysine salt)

Reparixin is a non-competitive allosteric inhibitor of the activation of CXCR1 and CXCR2 chemokine receptors by IL-8 (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 reduces blood pressure by inhibiting hypertension-related mediators, IL-8, 12-lipoxygenase, and endothelin-1.{28553} Reparixin blockade (100 nM) of CXCR1 depletes a cancer stem cell population in human breast cancer cell lines in vitro.{28554}