Powder: -20°C for 3 years | In solvent: -80°C for 1 year
BAY-876 是口服有效的,选择性的葡萄糖转运蛋白 1 (GLUT1) 抑制剂(IC50= 2 nM)。BAY-876 对 GLUT1 选择性比 GLUT2,GLUT3 和 GLUT4 高(<130 倍)。BAY-876 对糖酵解代谢和卵巢癌生长也有有效的抑制作用。
规格 | 价格/CNY | 货期 | 数量 | |
---|---|---|---|---|
1 mg | ¥ 518 | 现货 | ||
2 mg | ¥ 759 | 现货 | ||
5 mg | ¥ 1,170 | 现货 | ||
10 mg | ¥ 1,820 | 现货 | ||
25 mg | ¥ 2,970 | 现货 | ||
50 mg | ¥ 4,620 | 现货 | ||
100 mg | ¥ 6,590 | 现货 | ||
500 mg | ¥ 13,300 | 现货 | ||
1 mL * 10 mM (in DMSO) | ¥ 1,170 | 现货 |
产品描述 | BAY-876 is an orally active and selective inhibitor of glucose transporter 1 (GLUT1, IC50= 2 nM). BAY-876 exhibits >130-fold more selective for GLUT1 than GLUT2, GLUT3, and GLUT4. BAY-876 also inhibits glycolytic metabolism and ovarian cancer growth. |
靶点活性 | GLUT1:0.002 μM |
体外活性 | BAY-876 is a highly-selective GLUT1 inhibitor with selectivity over GLUT2, 3, and 4 of 4700-, 800-, and 135-fold, respectively[1]. |
体内活性 | 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]. |
分子量 | 496.42 |
分子式 | C24H16F4N6O2 |
CAS No. | 1799753-84-6 |
Powder: -20°C for 3 years | In solvent: -80°C for 1 year
H2O: < 1 mg/mL (insoluble or slightly soluble)
Ethanol: 3 mg/mL (6.04 mM)
DMSO: 92 mg/mL (185.4 mM)
可选溶剂 | 浓度 体积 质量 | 1 mg | 5 mg | 10 mg | 25 mg |
Ethanol / DMSO | 1 mM | 2.0144 mL | 10.0721 mL | 20.1442 mL | 50.3606 mL |
5 mM | 0.4029 mL | 2.0144 mL | 4.0288 mL | 10.0721 mL | |
DMSO | 10 mM | 0.2014 mL | 1.0072 mL | 2.0144 mL | 5.0361 mL |
20 mM | 0.1007 mL | 0.5036 mL | 1.0072 mL | 2.518 mL | |
50 mM | 0.0403 mL | 0.2014 mL | 0.4029 mL | 1.0072 mL | |
100 mM | 0.0201 mL | 0.1007 mL | 0.2014 mL | 0.5036 mL |
对于不同动物的给药剂量换算,您也可以参考 更多...
请在以下方框中输入您的动物实验信息后点击计算,可以得到母液配置方法和体内配方的制备方法: 比如您的给药剂量是10 mg/kg,每只动物体重20 g,给药体积100 μL,一共给药动物10 只,您使用的配方为5% DMSO+30% PEG300+5% Tween 80+60% ddH2O。那么您的工作液浓度为2 mg/mL。
母液配置方法:2 mg 药物溶于 50 μL DMSO (母液浓度为 40 mg/mL), 如您需要配置的浓度超过该产品的溶解度,请先与我们联系。
体内配方的制备方法:取 50 μL DMSO 主液,加入 300 μL PEG300, 混匀澄清,再加 50 μL Tween 80,混匀澄清,再加 600 μL ddH2O, 混匀澄清。
您可能有的问题的答案可以在抑制剂处理说明中找到,包括如何准备库存溶液,如何存储产品,以及基于细胞的分析和动物实验需要特别注意的问题。
BAY-876 1799753-84-6 Metabolism transporter Inhibitor metabolism ovarian glycolytic cancer Glucose transporter BAY 876 glucose inhibit BAY876 orally GLUT inhibitor