化合物AZD1981 T6399

Product Introduction
Bioactivity


英文名: AZD1981

描述: AZD1981 是一种有效且特异性的 CRTh2 (DP2) 受体拮抗剂，IC50为 4 nM，用于研究哮喘、绝经后、药代动力学、哮喘患者和药物相互作用等治疗和基础科学的试验。

体外活性: AZD1981, as a potent antagonist in a disease relevant cell system, inhibits DK-PGD2-induced CD11b expression in human eosinophils with IC50 of 10 nM. [1] AZD1981 blocks DP2-mediated shape change in human eosinophils and basophils in blood, as well as DP2-mediated chemotaxis of human Th2 cells and eosinophils. Moreover, AZD1981 also blocks the binding of [3H]PGD2 to mouse, rat, guinea pig, rabbit and dog recombinant DP2. [2]

体内活性: AZD1981 has high oral bioavailability in male sprague dawley rats. [1] In guinea pig hind limb model, AZD1981 (100 nM) completely inhibits DK-PGD2-induced eosinophil mobilization. [2]

存储条件: Powder: -20°C for 3 years | In solvent: -80°C for 1 year

溶解度: Ethanol : < 1 mg/mL (insoluble or slightly soluble)
H2O : < 1 mg/mL (insoluble or slightly soluble)
DMSO : 9 mg/mL (23.1 mM)


关键字: Prostaglandin Receptor | Inhibitor | AZD 1981 | AZD1981 | inhibit | AZD-1981

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相关库: Drug Repurposing Compound Library | Anti-Cancer Drug Library | Membrane Protein-targeted Compound Library | Bioactive Compounds Library Max | Inhibitor Library | Anti-Cancer Clinical Compound Library | GPCR Compound Library | Highly Selective Inhibitor Library | NO PAINS Compound Library | Bioactive Compound Library

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注：该产品未在中华人民共和国食品药品监督管理部门申请医疗器械注册和备案，不可用于临床诊断或治疗等相关用途