Product Overview
UK-5099 is a potent inhibitor of the mitochondrial pyruvate carrier. The mitochondrial pyruvate carrier (MPC) facilitates pyruvate transport across the mitochondrial inner membrane and plays a critical role in carbohydrate, lipid and amino acid metabolism. UK-5099 (1 mM) completely blocked pyruvate uptake with Ki value of 49 μM. Also, UK-5099 decreased the overall efflux rate in a concentration-dependant way. In mitochondria isolated from S. Guttatum, UK-5099 (20 μM) inhibited pyruvate-dependent 02 consumption. In rat heart mitochondria, UK-5099 inhibited pyruvate oxidation with a non-linear inhibition kinetics. In glucagon-treated rats, UK-5099 inhibited pyruvate carboxylation and total pyruvate metabolism with a linear relationship. In rat liver and heart mitochondria, UK-5099 inhibited pyruvate-dependent 02 consumption with IC50 value of 50 nM.
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