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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
Pack Size | Price | Availability | Quantity |
---|---|---|---|
1 mg | $97 | In Stock | |
5 mg | $239 | In Stock | |
10 mg | $383 | In Stock | |
25 mg | $653 | In Stock | |
50 mg | $892 | In Stock | |
100 mg | $1,230 | In Stock |
Description | 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 |
In vitro | 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. |
Alias | 2,4-Thiazolidinedione, 5-[[5-[6-(4-acetyl-1-piperazinyl)-3-nitro-2-pyridinyl]-2-fluorophenyl]methylene]- |
Molecular Weight | 471.46 |
Formula | C21H18FN5O5S |
Cas No. | 853953-65-8 |
Smiles | CC(=O)N1CCN(CC1)c1ccc(c(n1)-c1ccc(F)c(\C=C2/SC(=O)NC2=O)c1)[N+]([O-])=O |
Relative Density. | no data available |
Storage | Powder: -20°C for 3 years | In solvent: -80°C for 1 year | Shipping with blue ice. | |||||||||||||||||||||||||
Solubility Information | DMF: 5 mg/mL (10.61 mM), Sonication is recommended. DMSO: 4 mg/mL (8.48 mM) | |||||||||||||||||||||||||
Solution Preparation Table | ||||||||||||||||||||||||||
DMSO/DMF
DMF
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