Network Version
Navarixin Data Sheet
| Product Name: | Navarixin |
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|---|---|---|
| CAS No.: | 473727-83-2 | |
| Cat. No.: | HY-10198 | |
| MWt: | 397.42 | |
| Formula: | C21H23N3O5 | |
| Purity : | >98% | |
| Solubility: | DMSO : ≥ 50 mg/mL (125.81 mM) | |
| Mechanisms: | Target: Cancer Endocrinology Inflammation/Immunology | |
| Biological Activity: | ||
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Navarixin (SCH 527123) is a potent, allosteric and orally active antagonist of both CXCR1 and CXCR2, with Kd 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[1][2].
IC50 & Target: Kd: 41 nM (cynomolgus CXCR1), 0.20 nM (mouse CXCR2), 0.20 nM (rat CXCR2), 0.08 nM (cynomolgus monkey CXCR2)[1]
In Vitro: Navarixin is a potent, allosteric antagonist of both CXCR1 and CXCR2, with Kd 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[1]. 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[2]. 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[3].
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 |
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