UK-5099

Short Summary : MCTs and MPC inhibitor

Category : Membrane Transporter/Ion Channel|MCT2

Purity : 0.98

CAS Number : 56396-35-1

Formula : C18H12N2O2

Molecular Weight : 288.3

SMILE : C1=CC=C(C=C1)N2C=C(C3=CC=CC=C32)C=C(C#N)C(=O)O

Solubility : Soluble in DMSO > 10 mM

Storage : Store at -20°C

Description : UK-5099 is a potent inhibitor of the mitochondrial pyruvate carrier [1]. 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 ?M. Also, UK-5099 decreased the overall efflux rate in a concentration-dependant way [1]. In mitochondria isolated from S. Guttatum, UK-5099 (20 ?M) inhibited pyruvate-dependent 02 consumption [2]. In rat heart mitochondria, UK-5099 inhibited pyruvate oxidation with a non-linear inhibition kinetics [2]. In glucagon-treated rats, UK-5099 inhibited pyruvate carboxylation and total pyruvate metabolism with a linear relationship [3]. In rat liver and heart mitochondria, UK-5099 inhibited pyruvate-dependent 02 consumption with IC50 value of 50 nM [4].References:[1]. Wiemer EA, Michels PA, Opperdoes FR. The inhibition of pyruvate transport across the plasma membrane of the bloodstream form of Trypanosoma brucei and its metabolic implications. Biochem J, 1995, 312 ( Pt 2): 479-484.[2]. Halestrap AP. The mitochondrial pyruvate carrier. Kinetics and specificity for substrates and inhibitors. Biochem J, 1975, 148(1): 85-96.[3]. Halestrap AP, Armston AE. A re-evaluation of the role of mitochondrial pyruvate transport in the hormonal control of rat liver mitochondrial pyruvate metabolism. Biochem J, 1984, 223(3): 677-685.[4]. Proudlove MO, Beechey RB, Moore AL. Pyruvate transport by thermogenic-tissue mitochondria. Biochem J, 1987, 247(2): 441-447.

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