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Navarixin

Cat. No.:YN320210

  • CAS No. :473727-83-2

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    • 参考文献
    • 产品名称: Navarixin
      CAS No.: 473727-83-2
      Chemical Name: 2-hydroxy-N,N-dimethyl-3-[[2-[[(1R)-1-(5-methyl-2-furanyl)propyl]amino]-3,4-dioxo-1-cyclobuten-1-yl]amino]-benzamide
      Synonyms:SCH 527123; MK-7123
      分子量:397.42
      分子式:C₂₁H₂₃N₃O₅
      SMILES:O=C1C(C(NC2=CC=CC(C(N(C)C)=O)=C2O)=C1N[C@H](CC)C3=CC=C(O3)C)=O
      存储:Please store the product under the recommended conditions in theCertificate of Analysis.
      运输:Room temperature in continental US; may vary elsewhere.
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      Purity: 98%
    • 产品描述: 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。
      IC50和靶点: [{name:"125I-CXCL8-CXCR2:0.97 nM (IC50)"},{name: "Cynomolgus CXCR2:0.08 nM (Kd)"},{name: "Mouse CXCR2:0.2 nM (Kd)"},{name: "Rat CXCR2:0.2 nM (Kd)"},{name: "125I-CXCL8-CXCR1:43 nM (IC50)"},{name: "Cynomolgus CXCR1:41 nM (Kd)"}]
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    • Gonsiorek, W., Fan, X., Hesk, D., et al.Pharmacological characterization of Sch527123, a potent allosteric CXCR1/CXCR2 antagonist.J. Pharmacol. Exp. Ther.322(2),477-485(2007)

      Chapman, R.W., Minnicozzi, M., Celly, C.S., et al.A novel, orally active CXCR1/2 receptor antagonist, Sch527123, inhibits neutrophil recruitment, mucus production, and goblet cell hyperplasia in animal models of pulmonary inflammationJ. Pharmacol. Exp. Ther.322(2),486-493(2007)

      Ning, Y., Labonte, M.J., Zhang, W., et al.The CXCR2 antagonist, SCH-527123, shows antitumor activity and sensitizes cells to oxaliplatin in preclinical colon cancer modelsMol. Cancer Ther.11(6),1353-1364(2012)

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