中文名：Nemiralisib (GSK2269557)
英文名：Nemiralisib (GSK2269557)
纯度：Moligand™，≥99%
货号：N413878
Cas号：1254036-71-9
存储温度：-20°C储存
运输条件：超低温运输
产品介绍：
Information
Nemiralisib, also known as GSK-2269557, is a potent and selectivePI3Kδinhibitor(pKi = 9.9).
Targets
PI3Kδ (Cell-free assay) 9.9(pKi)
In vivo
GSK-2269557 has low oral bioavailability (F=2%) and in vivo clearance of 28 mL/min/kg but has a high volume of distribution of 6.3 L/kg. GSK-2269557 induces concentration-dependent increases in QT interval and Tp-e at 0.3 and 1 μM (1 and 0.5 Hz) and an increase in QRS at 1 μM (2 Hz), however, no treatment-related torsades de pointes (TdP) arrhythmias are observed. In a disease relevant brown Norway rat acute OVA model of Th2 driven lung inflammation, GSK-2269557 is shown to protect against eosinophil recruitment with an ED50 of 67 μg/kg and dose-dependently reduces recruitment of all leukocyte subpopulations and IL-13 in the lungs.
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关键字： 奈米拉利西布 (GSK2269557);6-(1H-indol-4-yl)-4-(5-{[4-(1-methylethyl)-1-piperazinyl]methyl}-1,3-oxazol-2-yl)-1H-indazole ; FT-0716060 ; GSK2269557 free base
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