GW604714X 

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 K_i <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].

GW604714X inhibits the mitochondrial pyruvate carrier (MPC) with K_i value <0.1 μM in direct measurement of pyruvate transport into rat liver and yeast mitochondria^[1].
Inhibitor titrations of pyruvate-dependent respiration by heart mitochondria gave values for the concentration of inhibitor binding sites and their K_i (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].

MCE has not independently confirmed the accuracy of these methods. They are for reference only.

471.46

Solid

C₂₁H₁₈FN₅O₅S

853953-65-8

O=C(NC/1=O)SC1=C/C2=CC(C3=NC(N4CCN(C(C)=O)CC4)=CC=C3[N+]([O-])=O)=CC=C2F

Room temperature in continental US; may vary elsewhere.

• [1]. John C W Hildyard, et al. Identification and characterisation of a new class of highly specific and potent inhibitors of the mitochondrial pyruvate carrier. Biochim Biophys Acta. Apr-May 2005;1707(2-3):221-30.  [Content Brief]

  [2]. Allen K. Bourdon, et al. Alzheimer's and Parkinson's Disease Novel Therapeutic Target: The Mitochondrial Pyruvate Carrier - Ligand Docking to Screen Natural Compounds Related to Classic Inhibitors. DOI:10.4018/IJKDB.2017070104