Reparixin | CXCR 1/2 allosteric antagonist
NMR (Conforms)
Available Options
| Size : | Price | Quantity | |
|---|---|---|---|
| 5 mg | $52.00 | ||
| 25 mg | $208.00 |
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
References/Citations:
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
NMR (Conforms)
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Product Data Sheet:
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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
References/Citations:
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
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