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抑制剂描述:

产品名称:BAY-876

产品别名:见爱必信官网

英文别名:BAY-876

靶点:GLUT1

CAS:1799753-84-6

纯度:98%

外观:见爱必信官网

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.

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。

溶解性:DMSO : 92 mg/mL (185.4 mM) ;
Ethanol : 3 mg/mL (6.04 mM)

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.

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.

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