ChemicalBook--->CAS DataBase List--->853953-65-8

853953-65-8

853953-65-8 Structure

853953-65-8 Structure
IdentificationBack 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
Chemical PropertiesBack Directory
[storage temp. ]

Store at -20°C
[form ]

Solid
[color ]

Light yellow to green yellow
Hazard InformationBack Directory
[Uses]

GW604714X is a potent inhibitor of mitochondrial respiration supported by pyruvate but not other substrates. GW604714X is a highly specific mitochondrial pyruvate carrier (MPC) inhibitor with a Ki <0.1 nM. GW604714X also inhibits?L-lactate transport by the?plasma membrane?monocarboxylate transporter?(MCT1), but at concentrations more than 4 orders of magnitude greater than the MPC[1].
[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.
Spectrum DetailBack Directory
[Spectrum Detail]

2,4-Thiazolidinedione, 5-[[5-[6-(4-acetyl-1-piperazinyl)-3-nitro-2-pyridinyl]-2-fluorophenyl]methylene]-(853953-65-8)1HNMR
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