AZD1981
CAS No. 802904-66-1
AZD1981 ( AZD1981; AZD-1981; AZD 1981 )
Catalog No. 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.
Purity : 98%
COA
Datasheet
HNMR
HPLC
MSDS
Handing Instructions
Size | Price / USD | Stock | Quantity |
5MG | 37 | In Stock |
|
10MG | 71 | In Stock |
|
25MG | 147 | In Stock |
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50MG | 288 | In Stock |
|
100MG | 434 | In Stock |
|
200MG | Get Quote | In Stock |
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500MG | Get Quote | In Stock |
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1G | Get Quote | In Stock |
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Biological Information
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Product NameAZD1981
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NoteResearch use only, not for human use.
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Brief DescriptionAZD1981 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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DescriptionAZD1981is 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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SynonymsAZD1981; AZD-1981; AZD 1981
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PathwayMetabolic Enzyme/Protease
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TargetDehydrogenase
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RecptorCRTh2 (DP2) receptor
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Research AreaInflammation/Immunology
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Indication——
Chemical Information
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CAS Number802904-66-1
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Formula Weight388.87
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Molecular FormulaC19H17ClN2O3S
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Purity98%
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SolubilityDMSO : ≥ 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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Chemical Name2-(4-acetamido-3-((4-chlorophenyl)thio)-2-methyl-1H-indol-1-yl)acetic acid
Shipping & Storage Information
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Storage(-20℃)
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ShippingWith Ice Pack
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Stability≥ 2 years
Reference
1. Luker T, et al. Bioorg Med Chem Lett. 2011, 21(21), 6288-6292.
molnova catalog
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