Reparixin
Reparixin
Reparixin
| Catalog | Description | Size | Price (USD) | Qty |
|---|---|---|---|---|
| GBM-2527-5MG | Reparixin | 5mg | $110.00 | |
| GBM-2527-25MG | Reparixin | 25mg | $437.00 |
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Description
CXCR1/2 allosteric antagonist
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Specifications
Bioassays Specification Bio-Activity CXCR1/2 allosteric antagonist Chemical Name αR-Methyl-4-(2-methylpropyl)-N-(methylsulfonyl)-benzeneacetamide Function / Pharmacology 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 CAS# 266359-83-5 MW 283.39 Molecular Formula C14H21NO3S Solubility Soluble in DMSO (up to 100 mg/ml) or in Ethanol up to 25 mg/ml) Supplied powder Storage as supplied -20°C Ship temp Ambient References 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 Antibody Specification Alternate Names DF 1681Y; Repertaxin Protein Specification Purity >98% - Reviews
| Bioassays Specification | |
| Bio-Activity | CXCR1/2 allosteric antagonist |
| Chemical Name | αR-Methyl-4-(2-methylpropyl)-N-(methylsulfonyl)-benzeneacetamide |
| Function / Pharmacology | 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 |
| CAS# | 266359-83-5 |
| MW | 283.39 |
| Molecular Formula | C14H21NO3S |
| Solubility | Soluble in DMSO (up to 100 mg/ml) or in Ethanol up to 25 mg/ml) |
| Supplied | powder |
| Storage as supplied | -20°C |
| Ship temp | Ambient |
| References | 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 |
| Antibody Specification | |
| Alternate Names | DF 1681Y; Repertaxin |
| Protein Specification | |
| Purity | >98% |