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 |
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10MG | ¥640 | 有现货 |
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25MG | ¥1320 | 有现货 |
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50MG | ¥2592 | 有现货 |
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100MG | ¥3904 | 有现货 |
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200MG | 获取报价 | 有现货 |
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500MG | 获取报价 | 有现货 |
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1G | 获取报价 | 有现货 |
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生物学信息
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产品名称AZD1981
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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
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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.
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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.
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同义词AZD1981; AZD-1981; AZD 1981
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通路Metabolic Enzyme/Protease
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靶点Dehydrogenase
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受体CRTh2 (DP2) receptor
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研究领域Inflammation/Immunology
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适应症——
化学信息
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CAS Number802904-66-1
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分子量388.87
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分子式C19H17ClN2O3S
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纯度98%
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溶解度DMSO : ≥ 31 mg/mL; 79.72 mM
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SMILESCc1c(c2c(n1CC(=O)O)cccc2NC(=O)C)Sc1ccc(cc1)Cl
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化学全称2-(4-acetamido-3-((4-chlorophenyl)thio)-2-methyl-1H-indol-1-yl)acetic acid
运输与储存
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储存条件(-20℃)
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运输条件With Ice Pack
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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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