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CAS No. : 473727-83-2
MCE 国际站: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 Kd 值为 41 nM,对小鼠,大鼠和猕猴 CXCR2 的 Kd 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 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. 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.
相关产品:Drug Repurposing Compound Library Plus | Clinical Compound Library Plus | Bioactive Compound Library Plus | GPCR/G Protein Compound Library | Immunology/Inflammation Compound Library | Anti-Cancer Compound Library | Clinical Compound Library | Small Molecule Immuno-Oncology Compound Library | Drug Repurposing Compound Library | Endocrinology Compound Library | Anti-COVID-19 Compound Library | Orally Active Compound Library | Anti-Prostate Cancer Compound Library | Chemokine Compound Library | Heterocyclic Compound Library | Membrane Protein-targeted Compound Library | Membrane Receptor-targeted Compound Library | Highly Selective Inhibitors Library | Nicotinamide N-oxide | SX-517 | AMG 487 (S-enantiomer) | TC14012 | CTCE-9908 | CXCR2 antagonist 3 | Kynurenic acid-d5 | (R,R)-CXCR2-IN-2 | IT1t dihydrochloride | NUCC-390 | Ac-Pro-Gly-Pro-OH | Vimnerixin | NBI-74330 | CXCR4 antagonist 9 | Quetmolimab | PS372424 hydrochloride | SCH 546738 | vMIP-II (1-21) | CXCR2-IN-1 | Mavorixafor | Reparixin L-lysine salt | VUF11207 fumarate | NoxaBH3 | Kynurenic acid | CXCR4 antagonist 2 | Balixafortide | Plerixafor octahydrochloride | Ladarixin
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