Reparixin
CXCR 1/2 allosteric antagonist / 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
Biochemicals & reagents
266359-83-5
DF 1681Y; Repertaxin
1) Bertini et al. (2004), Non-competetitive allosteric inhibitors of the inflammatory cytokine receptors CXCR1 and CXCR2: prevention of reperfusion injury; Proc. Natl. Acad. Sci. USA, 101 11791 2) Kim et al. (2011), Reparixin, an inhibitor of CXCR1 and CXCR2 receptor activation, attenuates blood pressure and hypertension-related mediators expression in spontaneously hypertensive rats; Biol. Pharm. Bull., 34 120 3) Gorio et al. (2007), Reparixin, an inhibitor of CXCR2 function, attenuates inflammatory responses and promotes recovery of function after traumatic lesion to the spinal cord; J. Pharmacol. Exp. Ther., 322 973 4) Ginestier et al. (2010), CXCR1 blockade selectively targets human breast cancer stem cells in vitro and in xenografts; J. Clin. Invest., 120 485
-20°C
TARGET: GPCR -- PATHWAY: Cytokine -- RESEARCH AREA: Cancer Stem Cells -- DISEASE AREA: Cancer; HypertensionInflammation