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Reparixin | CXCR 1/2 allosteric antagonist

Reparixin (CAS 266359-83-5) 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


1) Bertini et al. (2004), Non-competitive 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

Focus Biomolecules cell signaling supplier, chemical structure Reparixin | CXCR 1/2 allosteric antagonist | CAS 266359-83-5

Catalog#  10-2527-0005

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Catalog Number:
CXCR 1/2 allosteric antagonist
Chemical Name:
Alternate Names:
DF 1681Y; Repertaxin
Molecular Weight:
Molecular Formula:
Soluble in DMSO (up to 100 mg/ml) or in Ethanol (up to 25 mg/ml)
Physical Properties:
White solid
99% by HPLC
NMR (Conforms)
Storage Temperature:
-20°C (des.)
Stable for 1 year as supplied. Solutions in DMSO or ethanol may be stored at -20°C for up to 3 months.
Shipping Code:
Materials provided by Focus Biomolecules are for laboratory research use only and are not intended for human or veterinary applications.

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