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 Reparixin (CAS 266359-83-5)是一种抑制IL-8 (CXCL8)激活CXCR1和CXCR2趋化因子受体的非竞争性变构抑制剂(IC50分别为1和100 nM)。 它阻断了许多与IL-8信号相关的活性,包括白细胞招募(IC50 = 1 nM),而不影响其他CXCR1和CXCR2激动剂诱导的受体激活 在自发性高血压大鼠中,连续三周每天给药5 mg/kg雷比欣可通过抑制高血压相关介质来降低血压 减轻脊髓损伤后的炎症反应,促进功能恢复 CXCR1的Reparixin封锁(100 nM)也被用于体外消耗人类乳腺癌细胞系中的癌症干细胞群。
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:
10-2427
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
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