Powder: -20°C for 3 years | In solvent: -80°C for 1 year
GSK2837808A 是一种选择性的乳酸脱氢酶A 抑制剂,对 hLDHA (IC50:2.6 nM) 和 hLDHB (IC50:43 nM)。
规格 | 价格/CNY | 货期 | 数量 | |
---|---|---|---|---|
1 mg | ¥ 558 | 现货 | ||
5 mg | ¥ 1,450 | 现货 | ||
10 mg | ¥ 2,360 | 现货 | ||
25 mg | ¥ 3,680 | 现货 | ||
50 mg | ¥ 5,290 | 现货 | ||
100 mg | ¥ 7,480 | 现货 | ||
500 mg | ¥ 14,900 | 现货 | ||
1 mL * 10 mM (in DMSO) | ¥ 1,880 | 现货 |
产品描述 | GSK2837808A is a potent and selective inhibitor of lactate dehydrogenase A (LDHA) (IC50s: 1.9 and 14 nM for LDHA and LDHB, respectively). |
靶点活性 | LDHB:1.9 nM, LDHA:1.9 nM |
体外活性 | GSK2837808A inhibits lactate production in hypoxia but at higher concentrations than in normoxia (EC50=10 μM). It also reduces ECAR (EC50=10 μM). LDH inhibition by GSK2837808A alters multiple metabolic pathways in Snu398 cells. GSK2837808A rapidly and profoundly inhibits lactate production rates in multiple cancer cell lines including hepatocellular and breast carcinomas. GSK2837808A potency does not correlate with LDHA, LDHB, or the total LDH expression levels. The potency of GSK2837808A across 30 cancer cell lines with different LDHA and LDHB expression levels range from 400 nM to no effect (EC50 reported as 30 μM). |
体内活性 | GSK2837808A (p.o.; 50 mg/kg in rats; 100 mg/kg in mice) treatment, causes blood compound levels at or below the detection limit of 2.5 ng/mL. Clearance following IV infusion of GSK2837808A at 0.25 mg/kg is displayed to be 69 mL/minute/kg in rats and it exceeds the animal liver blood flow. |
分子量 | 649.62 |
分子式 | C31H25F2N5O7S |
CAS No. | 1445879-21-9 |
Powder: -20°C for 3 years | In solvent: -80°C for 1 year
DMSO: 95 mg/mL (146.24 mM)
可选溶剂 | 浓度 体积 质量 | 1 mg | 5 mg | 10 mg | 25 mg |
DMSO | 1 mM | 1.5394 mL | 7.6968 mL | 15.3936 mL | 38.484 mL |
5 mM | 0.3079 mL | 1.5394 mL | 3.0787 mL | 7.6968 mL | |
10 mM | 0.1539 mL | 0.7697 mL | 1.5394 mL | 3.8484 mL | |
20 mM | 0.077 mL | 0.3848 mL | 0.7697 mL | 1.9242 mL | |
50 mM | 0.0308 mL | 0.1539 mL | 0.3079 mL | 0.7697 mL | |
100 mM | 0.0154 mL | 0.077 mL | 0.1539 mL | 0.3848 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。
GSK2837808A 1445879-21-9 Metabolism Dehydrogenase Inhibitor inhibit LDH Lactate Dehydrogenase GSK-2837808A inhibitor