Reparixin | CXCR 1/2 allosteric antagonist

CAS:
266359-83-5
Catalog Number:
10-2527
Activity:
CXCR 1/2 allosteric antagonist
Chemical Name:
αR-Methyl-4-(2-methylpropyl)-N-(methylsulfonyl)-benzeneacetamide
Alternate Names:
DF 1681Y; Repertaxin
Molecular Weight:
283.39
Molecular Formula:
C14H21NO3S
Solubility:
Soluble in DMSO (up to 100 mg/ml) or in Ethanol (up to 25 mg/ml)
Physical Properties:
White solid
Purity:
99% by HPLC
NMR (Conforms)
Storage Temperature:
-20°C
Stability:
Stable for 1 year from date of purchase as supplied. Solutions in DMSO or ethanol may be stored at -20°C for up to 3 months.
Shipping Code:
RT

Available Options

Size :PriceQuantity 
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

CAS:
266359-83-5
Catalog Number:
10-2527
Activity:
CXCR 1/2 allosteric antagonist
Chemical Name:
αR-Methyl-4-(2-methylpropyl)-N-(methylsulfonyl)-benzeneacetamide
Alternate Names:
DF 1681Y; Repertaxin
Molecular Weight:
283.39
Molecular Formula:
C14H21NO3S
Solubility:
Soluble in DMSO (up to 100 mg/ml) or in Ethanol (up to 25 mg/ml)
Physical Properties:
White solid
Purity:
99% by HPLC
NMR (Conforms)
Storage Temperature:
-20°C
Stability:
Stable for 1 year from date of purchase as supplied. Solutions in DMSO or ethanol may be stored at -20°C for up to 3 months.
Shipping Code:
RT

Safety Data Sheet:

N/A

Product Data Sheet:

Materials provided by Focus Biomolecules are for laboratory research use only and are not intended for human or veterinary applications. Please note that we do not sell to individuals and that all orders placed by non-research organizations will incur a $20 restocking/refund fee

20% OFF

For Postdoc
Customers!