GW604714X是丙酮酸支持的线粒体呼吸(mitochondrialrespiration)的有效选择性抑制剂。GW604714X抑制线粒体丙酮酸载体(MPC)的Ki值<0.1μM。GW604714X也能抑制质膜单羧酸转运蛋白MCT1对L-乳酸的转运，但其浓度要比MPC高4个数量级。
货号:ajcx32082
CAS:853953-65-8
分子式:C21H18FN5O5S
分子量：471.46
溶解度:N/A
纯度：98%
存储：Store at -20°C
库存：现货

Background:

GW604714X is a potent and selective inhibitor of mitochondrial respiration supported by pyruvate but not other substrates. GW604714X inhibits the mitochondrial pyruvate carrier (MPC) with a Ki values<0.1 μM. GW604714X also inhibits L-lactate transport by the plasma membrane monocarboxylate transporter MCT1, but at concentrations more than four orders of magnitude greater than the MPC[1].

GW604714X inhibits the mitochondrial pyruvate carrier (MPC) with Ki values<0.1 μM in direct measurement of pyruvate transport into rat liver and yeast mitochondria. Inhibitor titrations of pyruvate-dependent respiration by heart mitochondria gave values for the concentration of inhibitor binding sites and their Ki (nM) of 56.0 nM and 0.057 nM for the GW604714X[1].GW604714X inhibits the transport of 0.5 mM [14C]-l-lactate into rat red blood cells, mediated by the monocarboxylate transporter MCT1. GW604714X at 10 μM reduces the initial rate of uptake to 30% of control values[1].

[1]. K K Yamamoto, et al. Isolation of a cDNA encoding a human serum marker for acute pancreatitis. Identification of pancreas-specific protein as pancreatic procarboxypeptidase B. J Biol Chem. 1992 Feb 5;267(4):2575-81.