| Identification | Back Directory | [Name]
2,4-Thiazolidinedione, 5-[[5-[6-(4-acetyl-1-piperazinyl)-3-nitro-2-pyridinyl]-2-fluorophenyl]methylene]- | [CAS]
853953-65-8 | [Synonyms]
GW604714X
5-[[5-[6-(4-acetyl-1-piperazinyl)-3-nitro-2-pyridinyl]-2-fluorophenyl]methylene]-
5-(5-(6-(4-Acetylpiperazin-1-yl)-3-nitropyridin-2-yl)-2-fluorobenzylidene)thiazolidine-2,4-dione
2,4-Thiazolidinedione, 5-[[5-[6-(4-acetyl-1-piperazinyl)-3-nitro-2-pyridinyl]-2-fluorophenyl]methylene]-
2,4-Thiazolidinedione, 5-[[5-[6-(4-acetyl-1-piperazinyl)-3-nitro-2-pyridinyl]-2-fluorophenyl]methylene]- ISO 9001：2015 REACH | [Molecular Formula]
C21H18FN5O5S | [MDL Number]
MFCD33402205 | [MOL File]
853953-65-8.mol | [Molecular Weight]
471.46 |
| Hazard Information | Back Directory | [Biological Activity]
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]. | [References]
[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. |
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