N′-[1-(4-シアノベンジル)-3-(トリフルオロメチル)-5-メチル-1H-ピラゾール-4-イル]-7-フルオロキノリン-2,4-ジカルボアミド 化学特性,用途語,生産方法
説明
BAY-876 is a potent, highly selective, cell-permeable inhibitor of glucose transporter GLUT1. It had an IC50 value of 2 nM in vitro and inhibited glucose uptake by Hela-MaTu cells with an IC50 value of 3.2 nM. BAY-876 was at least 130-fold selective for GLUT1 relative to GLUT2, GLUT3, GLUT4 and a panel of 18 kinases and 68 proteins.BAY-588 is used as a negative control and is available from Sigma.
使用
BAY-876 is a potent and selective inhibitor of glucose transporter 1 (Glut1) with IC50 values of 2, 10,800, 1,670, and 290 nM for Glut1, Glut2, Glut3, and Glut4, respectively, in CHO cells expressing human recombinant receptors.1 It shows low metabolic clearance and has high permeability in vitro. In vivo, BAY-876 displays low plasma clearance and high oral bioavailability in rats and dogs.
生物活性
Potent and selective GLUT1 inhibitor (IC50 = 2 nM). Displays selectivity for GLUT1 over GLUT2/3/4 (IC50 values are 10.8, 1.67 and 0.29 μM, respectively). Induces cell death in hypoxic conditions in vitro. Inhibits glucose uptake by Hela-MaTu cells. Cell permeable and orally bioavailable.
N′-[1-(4-シアノベンジル)-3-(トリフルオロメチル)-5-メチル-1H-ピラゾール-4-イル]-7-フルオロキノリン-2,4-ジカルボアミド 上流と下流の製品情報
原材料
準備製品