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Description: AZD7545 is a novel, potent, selective small-molecule inhibitor of PDHK (pyruvate dehydrogenase kinase 2) with IC50 of 36.8 nM and 6.4 nM for PDHK1 and PDHK2, respectively. Besides that, AZD7545 increases PDH activity with EC50 value of 5.2nM when using recombinant human PDHK2. In vivo studies show that administration of AZD7545 significantly activates PDH activity in liver and partially activates PDH activity in skeletal muscle and heart. In Zucker (fa/fa) rats, AZD7545 at dose of 10 mg/kg increases muscle PDH from 61% to 97% active and liver PDH from 33.5% to 72.8%.
References: Biochem Soc Trans. 2003 Dec; 31(Pt 6):1165-7; Biochemistry. 2007 Jul 24; 46(29):8592-602.
Exact Mass: 478.0577
Chemical Name: 4-[3-chloro-4-[[(2R)-3, 3, 3-trifluoro-2-hydroxy-2-methylpropanoyl]amino]phenyl]sulfonyl-N, N-dimethylbenzamideSMILES Code: O=C(N(C)C)C1=CC=C(S(=O)(C2=CC=C(NC([C](C)(O)C(F)(F)F)=O)C(Cl)=C2)=O)C=C1
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