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Navarixin

CAS No. : 473727-83-2

MCE 站：Navarixin

产品活性：Navarixin (SCH 527123) 是一种有效的，具有口服活性的变构的 CXCR1 和 CXCR2 拮抗剂，对猕猴 CXCR1 的 K_d 值为 41 nM，对小鼠，大鼠和猕猴 CXCR2 的 K_d 值分别为 0.20 nM，0.20 nM 和 0.08 nM。

研究领域：GPCR/G Protein  |  Immunology/Inflammation

作用靶点：CXCR

In Vitro: Navarixin is a potent, allosteric antagonist of both CXCR1 and CXCR2, with K_d values of 41 nM for cynomolgus CXCR1 and 0.20 nM, 0.20 nM, 0.08 nM for mouse, rat and cynomolgus monkey CXCR2, respectivelly. Navarixin (1 nM) reduces CXCL8 potency in stimulating Ba/F3-hCXCR2 chemotaxis. Navarixin (3 nM) significantly inhibits the potency and efficacy of CXCL1-induced neutrophils (PMN) chemotaxis. Navarixin (300 nM) significantly decreases chemokine potency and slightly decreases maximal cell movement for Ba/F3-CXCR1 cells. Navarixin (25 μM) is sufficient to block IL-8-mediated CXCR2 activation in HCT116, E2, Caco2, and IIIe cells, in which phosphorylation of downstream kinases of CXCR2 is reduced in a concentration-dependent manner.

In Vivo: Navarixin (0.1-10 mg/kg, p.o.) blocks pulmonary neutrophilia (ED₅₀=1.2 mg/kg) and goblet cell hyperplasia (32-38% inhibition at 1-3 mg/kg) in mice following the intranasal lipopolysaccharide (LPS) administration. In rats, Navarixin (0.1-3 mg/kg p.o.) suppresses the pulmonary neutrophilia (ED_{=1.8 mg/kg) and increase in bronchoalveolar lavage (BAL) mucin content (ED50=0.1 mg/kg) induced by intratracheal (i.t.) LPS.}

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