BAY-876

BAY-876CAS号: 1799753-84-6分子式: C24H16F4N6O2分子量: 496.42描述纯度储存/保存方法别名外观可溶性/溶解性靶点In vitro(体外研究)In vivo(体内研究)

产品描述
描述

BAY-876是有效的、选择性的GLUT1抑制剂(IC50=0.002 μM),对GLUT1的选择性比对GLUT2, GLUT3和GLUT4的选择性高100倍。

纯度
98%
储存/保存方法
Store at -20℃ for one year(Powder);Store at 2-4℃ for two weeks;Store at -20℃ for six months after dissolution.
基本信息
别名
BAY876;BAY 87
外观
white to beige powder
可溶性/溶解性
DMSO : 92 mg/mL (185.4 mM) ;
Ethanol : 3 mg/mL (6.04 mM)
生物活性
靶点
GLUT1
In vitro(体外研究)
BAY-876 is a highly-selective GLUT1 inhibitor with selectivity over GLUT2, 3, and 4 of 4700-, 800-, and 135-fold, respectively.
In vivo(体内研究)
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.

分子结构图

BAY-876