中文名：leniolisib (CDZ 173)
英文名：leniolisib (CDZ 173)
纯度：Moligand™，≥99%
货号：L414153
Cas号：1354690-24-6
存储温度：-20°C储存
运输条件：超低温运输
产品介绍：
Information
Leniolisib (CDZ 173) is a potentPI3Kδselective inhibitor withbiochemical IC50 valuesof 0.244, 0.424, 2.23 and 0.011 μM for PI3Kα, PI3Kβ, PI3Kγ and PI3Kδ, respectively.
Targets
PI3Kδ (Cell-free assay); PI3Kα (Cell-free assay); PI3Kβ (Cell-free assay); DNA-PK ; DNA-PK (Cell-free assay) 31052,0.011 μM; 0.244 μM; 0.424
In vitro
CDZ173 inhibits a large spectrum of immune cell functions, as demonstrated in B and T cells, neutrophils, monocytes, basophils, plasmocytoid dendritic cells, and mast cells. CDZ173 showed no activity up to the highest test concentration when tested against CYP isoform assays (3A3, 2D9, 2D6, 2C9), a panel of ion channels (including hERG) and a protease panel. In a panel of 50 safety related targets (GPCRs, ion channels, transporters), CDZ173 only showed measurable activity for hPDE4D (IC50 = 4.7 μM) and 5HT2B (IC50 = 7.7 μM).
In vivo
CDZ173 inhibits B cell activation in rats and monkeys in a concentration- and time-dependent manner. After prophylactic or therapeutic dosing, CDZ173 potently inhibited antigen-specific antibody production and reduced disease symptoms in a rat collagen-induced arthritis model. CDZ173 is absorbed very quickly across species as can be seen by an early Tmax of the oral profiles. Whereas clearance is low to moderate in rats and monkeys, it was found that clearance in dogs is very low resulting in a very high exposure in blood. Plasma protein binding in dogs is very high (>99%) and the distribution of the compound is restricted into tissue (Vss = 0.3 L/kg).
查看阿拉丁官网此产品相关对应页面：https://www.aladdin-e.com/zh_cn/L414153.html
关键字： 莱尼奥利西布 (CDZ 173);Q27282602 ; US8653092, 67 ; Example 67 [WO2012004299]
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