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AZD1981
本产品不向个人销售，仅用作科学研究，不用于任何人体实验及非科研性质的动物实验。
AZD1981图片
CAS NO:802904-66-1
包装与价格：
包装价格(元)
10mM (in 1mL DMSO)电议
5mg电议
25mg电议

产品介绍
AZD1981 是一种有效的选择性 CRTh2 拮抗剂；以高效力 (pIC50 = 8.4) 从人重组 DP2 中置换放射性标记的 PGD2。
Cas No.802904-66-1
化学名2-[4-acetamido-3-(4-chlorophenyl)sulfanyl-2-methylindol-1-yl]acetic acid
Canonical SMILESCC1=C(C2=C(N1CC(=O)O)C=CC=C2NC(=O)C)SC3=CC=C(C=C3)Cl
分子式C19H17ClN2O3S
分子量388.87
溶解度≥ 19.8mg/mL in DMSO
储存条件Store at -20°C
General tipsFor obtaining a higher solubility , please warm the tube at 37 ℃ and shake it in the ultrasonic bath for a while.
Shipping ConditionEvaluation sample solution : ship with blue ice
All other available size: ship with RT , or blue ice upon request
产品描述

AZD1981 is a selective, orally bioavailable and potent antagonist of the chemoattractant receptor-homologous expressed on Th2 lymphocytes receptor (CRTh2 or DP2) with an IC50 value of 4 nM [1].

AZD1981 has shown to inhibit eosinophil migration with a pIC50 value of 7.6±0.1. AZD1981 could block chemotaxis of DP2+ T-cell lines with a pIC50 value of 7.5±0.1. AZD1981 has been demonstrated to inhibit PGD2 binding to mouse, rat, rabbit, dog, guinea pig and human DP2. AZD1981 could inhibit shape change induced by DP2 in dog and guinea pig granulocytes as well as in human eosinophils and basophils in blood [2].

References:
[1] Luker T1, Bonnert R, Brough S, Cook AR, Dickinson MR, Dougall I, Logan C, Mohammed RT, Paine S, Sanganee HJ, Sargent C, Schmidt JA,Teague S, Thom S. Substituted indole-1-acetic acids as potent and selective CRTh2 antagonists-discovery of AZD1981. Bioorg Med Chem Lett. 2011 Nov 1;21(21):6288-92.
[2] Schmidt JA1, Bell FM, Akam E, Marshall C, Dainty IA, Heinemann A, Dougall IG, Bonnert RV, Sargent CA. Biochemical and pharmacological characterization of AZD1981, an orally available selective DP2 antagonist in clinical development for asthma. Br J Pharmacol. 2013 Apr;168(7):1626-38.