UK-5099_56396-35-1_DataSheet_MedChemExpress

Product Name:

UK-5099CAS No.:

56396-35-1Cat. No.:

HY-15475

Product Data Sheet

MWt:

288.30Formula:

C18H12N2O2Purity :>98%

Solubility:

DMSO >20 mg/mL

Mechanisms:

Biological Activity:

UK-5099(PF1005023)is a potent inhibitor of plasma membrane monocarboxylate transporters

Pathways:Membrane Tranporter/Ion Channel; Target:MCT UK 5099(PF1005023) is a potent inhibitor of plasma membrane monocarboxylate transporters (MCTs) and the mitochondrial pyruvate carrier (MPC); inhibits pyruvate-dependent O2 consumption

with an IC50 of 50 nM.

IC50 value: 50 nM

Target: MCT The trypanosomal pyruvate carrier was found to be rather insensitive to inhibition by alpha-cyano-4-hydroxycinnamate (Ki = 17 mM) but could be completely blocked by UK5099 (Ki = 49 microM).Inhibition of pyruvate transport resulted in the retention, and concomitant accumulation, of pyruvate within the trypanosomes, causing acidification of the cytosol and osmotic destabilization of the cells.References:

[1]. Nakamichi N, Kambe Y, Oikawa H,et al. Protection by exogenous pyruvate through a

mechanism related to monocarboxylate transporters against cell death induced by hydrogen peroxide in cultured rat cortical neurons.J Neurochem.2005Apr;93(1):https://www.wendangku.net/doc/829909425.html,-5099 is more powerful inhibitor than alpha-cyano-4-hydroxycinnamate showing 50% inhibition of pyruvate-dependent O2 consumption by rat heart mitochondria at concentrations of 200, 200 and 50nM respectively....

peroxide in cultured rat cortical neurons. J Neurochem. 2005 Apr; 93(1):8493.[2]. 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 Dec 1;312 ( Pt 2):479-84.[3]. Simchowitz L, Textor JA, Cragoe EJ Jr. Cell volume regulation in human neutrophils: 2-

(aminomethyl)phenols as Cl- channel inhibitors. Am J Physiol. 1993 Jul;265(1 Pt 1):C143-55.[4]. A P Halestrap. The mitochondrial pyruvate carrier. Kinetics and specificity for substrates and

inhibitors. Biochem J. 1975 April; 148(1): 85-96....

Caution: Not fully tested. For research purposes only

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