Powder: -20°C for 3 years | In solvent: -80°C for 1 year
GW604714X (2,4-Thiazolidinedione, 5-[[5-[6-(4-acetyl-1-piperazinyl)-3-nitro-2-pyridinyl]-2-fluorophenyl]methylene]-) 是一种高度特异性的线粒体丙酮酸载体抑制剂,Ki<0.1 nM。它是一种线粒体呼吸抑制剂。它也能抑制质膜单羧酸转运体的 L-乳酸转运,但浓度比 MPC 的大 4 个数量级。
规格 | 价格/CNY | 货期 | 数量 | |
---|---|---|---|---|
1 mg | ¥ 1,160 | 现货 | ||
5 mg | ¥ 2,830 | 现货 | ||
10 mg | ¥ 4,190 | 现货 | ||
25 mg | ¥ 6,730 | 现货 | ||
50 mg | ¥ 9,130 | 现货 | ||
100 mg | ¥ 12,300 | 现货 | ||
500 mg | ¥ 24,600 | 现货 |
产品描述 | GW604714X (2,4-Thiazolidinedione, 5-[[5-[6-(4-acetyl-1-piperazinyl)-3-nitro-2-pyridinyl]-2-fluorophenyl]methylene]-) were found to be potent inhibitors of mitochondrial respiration supported by pyruvate |
体外活性 | Direct measurement of pyruvate transport into rat liver and yeast mitochondria confirmed that these agents inhibited the mitochondrial pyruvate carrier (MPC) with K(i) values <0.1 μM. Inhibitor titrations of pyruvate-dependent respiration by heart mitochondria gave values for the concentration of inhibitor binding sites (pmol per mg protein) and their K(i) (nM) of 56.0 and 0.057 nM for the more hydrophobic GW604714X. GW604714X inhibited l-lactate transport by the plasma membrane monocarboxylate transporter MCT1, but at concentrations more than four orders of magnitude greater than the MPC. |
别名 | 2,4-Thiazolidinedione, 5-[[5-[6-(4-acetyl-1-piperazinyl)-3-nitro-2-pyridinyl]-2-fluorophenyl]methylene]- |
分子量 | 471.46 |
分子式 | C21H18FN5O5S |
CAS No. | 853953-65-8 |
Powder: -20°C for 3 years | In solvent: -80°C for 1 year
DMF: 5 mg/mL(10.61 mM), Sonication is recommended.
DMSO: 4 mg/mL (8.48 mM)
可选溶剂 | 浓度 体积 质量 | 1 mg | 5 mg | 10 mg | 25 mg |
DMF / DMSO | 1 mM | 2.1211 mL | 10.6054 mL | 21.2107 mL | 53.0268 mL |
5 mM | 0.4242 mL | 2.1211 mL | 4.2421 mL | 10.6054 mL | |
DMF | 10 mM | 0.2121 mL | 1.0605 mL | 2.1211 mL | 5.3027 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。
GW604714X 853953-65-8 Metabolism Mitochondrial Metabolism Inhibitor mitochondrial respiration Parkinson's Disease MCT1 pyruvate Alzheimer's Disease GW-604714X inhibit MPC 2,4-Thiazolidinedione, 5-[[5-[6-(4-acetyl-1-piperazinyl)-3-nitro-2-pyridinyl]-2-fluorophenyl]methylene]- inhibitor