BAY876 是一种具有口服活性的选择性葡萄糖转运蛋白 1 抑制剂，IC50为 2 nM。它还是一种糖酵解代谢和卵巢癌生长的有效阻滞剂。

BAY-876 is a potent and selective GLUT1 inhibitor.

BAY-876 is a highly-selective GLUT1 inhibitor with selectivity over GLUT2, 3, and 4 of 4700-, 800-, and 135-fold, respectively[1].

BAY-876 displays low clearance also in?vivo in rat and in dog. The volume of distribution in steady state (Vss) is moderate in both species. Terminal half life is intermediate in rat (2.5 h) and long in dog (22 h) due to the very low clearance. The oral bioavailability (F%) is 85% and 79% in rat and dog, respectively. Preliminary in?vivo PK studies of BAY-876 demonstrate that a good oral bioavailability and long terminal half-life is attainable making it an excellent chemical probe to further evaluate the hypothesis of cancer treatment with a very selective GLUT1 inhibitor[1].

1799753-84-6

C24H16F4N6O2

496.426

H2O:<1 mgml
DMSO:92 mg/mL (185.4 mM)
Ethanol:3 mg/mL (6.04 mM)
Powder: -20°C for 3 years
In solvent: -80°C for 2 years