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Beschreibung

A cell-permeable, bioavailable trifluomethylpropanamide compound that acts as a potent, selective, reversible, non-ATP-competitive inhibitor of pyruvate dehydrogenase kinases (IC50 = 36.8 & 6.4 nM for PDhK1 & PDhK2, respectively). Inhibits PDhK3 at much higher concentrations (IC50 = 600 nM) and robustly stimulates PDhK4 activity (>10 nM). Also shown to increase pyruvate dehydrogenase (PDh) activity in liver and muscle, and potentiates pyruvate oxidation (EC50 = 105 nM in rat hepatocytes). Occupies lipoyl domain-binding site of PDhK2 (Kd = 19.2 nM) and disrupts the association of PDhK2 and inner lipoyl-bearing domain 2 of dihydrolipoyl acetyltransferase. Improves 24-h glucose profile and eliminates postparandial elevation in blood glucose in Zucker (fa/Fa) rats (10 mg/kg, b.i.d, p.o.,7 days). Please note that the molecular weight for this compound is batch-specific due to variable water content. Please refer to the vial label or the certificate of analysis for the batch-specific molecular weight. The molecular weight provided represents the baseline molecular weight without water., Pyruvate Dehydrogenase Kinase Inhibitor, AZD7545, CAS 252017-04-2, is a potent, selective, reversible inhibitor of PDHK2 (IC₅,₀, = 6.4 nM). Inhibits PDHK1 at higher levels (IC₅,₀, = 36.8 nM)., A cell-permeable, bioavailable trifluomethylpropanamide compound that acts as a potent, selective, reversible, non-ATP-competitive inhibitor of pyruvate dehydrogenase kinases (IC50 = 36.8 & 6.4 nM for PDhK1 & PDhK2, respectively). Inhibits PDhK3 at much higher concentrations (IC50 = 600 nM) and robustly stimulates PDhK4 activity (>10 nM). Also shown to increase pyruvate dehydrogenase (PDh) activity in liver and muscle, and potentiates pyruvate oxidation (EC50 = 105 nM in rat hepatocytes). Occupies lipoyl domain-binding site of PDhK2 (Kd = 19.2 nM) and disrupts the association of PDhK2 and inner lipoyl-bearing domain 2 of dihydrolipoyl acetyltransferase. Improves 24-h glucose profile and eliminates postparandial elevation in blood glucose in Zucker (fa/Fa) rats (10 mg/kg, b.i.d, p.o.,7 days).