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AZD1981

CAS No. 802904-66-1

AZD1981 ( AZD1981; AZD-1981; AZD 1981 )

产品货号. M17599 CAS No. 802904-66-1

AZD1981 is an effective and specific CRTh2 (DP2) receptor antagonist (IC50: 4 nM), showing >1000-fold selectivity over more than 340 other enzymes and receptors.

纯度: 98%

COA Datasheet HNMR HPLC MSDS Handing Instructions
规格 价格/人民币 库存 数量
5MG ¥332 有现货
10MG ¥640 有现货
25MG ¥1320 有现货
50MG ¥2592 有现货
100MG ¥3904 有现货
200MG 获取报价 有现货
500MG 获取报价 有现货
1G 获取报价 有现货

生物学信息

  • 产品名称
    AZD1981
  • 注意事项
    本公司产品仅用于科研实验,不得用于人体或动物的临床与诊断
  • 产品简述
    AZD1981 is an effective and specific CRTh2 (DP2) receptor antagonist (IC50: 4 nM), showing >1000-fold selectivity over more than 340 other enzymes and receptors.
  • 产品描述
    AZD1981is an orally available selective CRTH or DP2 antagonist currently in clinical development for asthma. AZD1981 blocks functional responses in eosinophils, Th2 cells and basophils. AZD1981 displaced radio-labelled PGD2 from human recombinant DP2 with high potency (pIC50 = 8.4). Binding was reversible, non-competitive and highly selective against a panel of more than 340 other enzymes and receptors, including DP1 (>1000-fold selective). AZD1981 inhibited DP2 -mediated shape change and CD11b up-regulation in human eosinophils, shape change in basophils and chemotaxis of human eosinophils and Th2 cells with similar potency. AZD1981 exhibited good cross-species binding activity against mouse, rat, guinea pig, rabbit and dog DP2 . Evaluation in mouse, rat or rabbit cell systems was not possible as they did not respond to DP2 agonists. Agonist responses were seen in guinea pig and dog, and AZD1981 blocked DP2 -mediated eosinophil shape change. Such responses were more robust in the guinea pig, where AZD1981 also blocked DP2 -dependent eosinophil emigration from bone marrow.
  • 同义词
    AZD1981; AZD-1981; AZD 1981
  • 通路
    Metabolic Enzyme/Protease
  • 靶点
    Dehydrogenase
  • 受体
    CRTh2 (DP2) receptor
  • 研究领域
    Inflammation/Immunology
  • 适应症
    ——

化学信息

  • CAS Number
    802904-66-1
  • 分子量
    388.87
  • 分子式
    C19H17ClN2O3S
  • 纯度
    98%
  • 溶解度
    DMSO : ≥ 31 mg/mL; 79.72 mM
  • SMILES
    Cc1c(c2c(n1CC(=O)O)cccc2NC(=O)C)Sc1ccc(cc1)Cl
  • 化学全称
    2-(4-acetamido-3-((4-chlorophenyl)thio)-2-methyl-1H-indol-1-yl)acetic acid

运输与储存

  • 储存条件
    (-20℃)
  • 运输条件
    With Ice Pack
  • 稳定性
    ≥ 2 years

参考文献

1. Luker T, et al. Bioorg Med Chem Lett. 2011, 21(21), 6288-6292.
产品手册
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