AZD1981CAS号: 802904-66-1分子式: C19H17ClN2O3S分子量: 388.87描述纯度储存/保存方法别名外观可溶性/溶解性靶点In vitro(体外研究)In vivo(体内研究)
产品描述 | |
描述 |
AZD1981 is a potent, selective CRTh2 (DP2) receptor antagonist with IC50 of 4 nM, showing >1000-fold selectivity over more than 340 other enzymes and receptors, including DP1
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纯度 |
>98%
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储存/保存方法 |
Store at -20℃ for one year(Powder);Store at 2-4℃ for two weeks;Store at -20℃ for six months after dissolution.
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基本信息 | |
别名 |
AZD-1981; AZD 1981
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外观 |
Powder
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可溶性/溶解性 |
DMSO Solubility: 11 mg/mL (28.28 mM)
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生物活性 | |
靶点 |
CRTh2 (DP2) receptor
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In vitro(体外研究) |
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. 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 PGD2 to mouse, rat, guinea pig, rabbit and dog recombinant DP2.
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In vivo(体内研究) |
AZD1981 has high oral bioavailability in male sprague dawley rats. In guinea pig hind limb model, AZD1981 (100 nM) completely inhibits DK-PGD2-induced eosinophil mobilization.
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分子结构图