GW604714X 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。
产品描述
GW604714X 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.
Cas No.
853953-65-8
分子式
C21H18FN5O5S
分子量
471.46
别名
2,4-Thiazolidinedione, 5-[[5-[6-(4-acetyl-1-piperazinyl)-3-nitro-2-pyridinyl]-2-fluorophenyl]methylene]-
储存和溶解度
DMF:5mg/ml(10.61mM),Need ultrasonic
Powder: -20°C for 3 years
In solvent: -80°C for 2 years