LAS191859
A CRTH2/DP2 antagonist
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包装价格促销价数量
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500ug￥2662.002130.00- +
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1mg￥4762.003810.00- +
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- 货号: ajci72312
- CAS: 1420071-13-1
- 别名:
- 分子式: C24H24F3N3O3
- 分子量: 459.5
- 纯度: ＞98%
- 溶解度: DMF: 20 mg/ml,DMSO: 20 mg/ml,DMSO:PBS (pH 7.2) (1:2): 0.33 mg/ml,Ethanol: 2.5 mg/ml
- 储存: Store at -20°C
- 库存: 现货
Background
LAS191859 is a potent antagonist of CRTH2/DP2 with IC50 values of 9.58, 14, 15.5, and 7.6 nM for recombinant human, rat, mouse, and guinea pig CRTH2/DP2 receptors, respectively. It is selective for CRTH2/DP2 over a panel of 65 enzymes, ion channels, and transporters with <25% inhibition for all targets when tested at a concentration of 10 μM. LAS191859 reduces shape change of eosinophils (IC50s = 2 and 8.2 nM in isolated eosinophils and whole blood, respectively) and eosinophil chemotaxis (IC50 = 1.3 nM) induced by prostaglandin D2 binding to CRTH2/DP2. Oral administration of LAS191859 reduces PGD2-induced systemic eosinophilia in guinea pigs (ID50 = 131 μg/kg).
