AZD7545 (C09-0735-476)

InformationAZD7545 AZD7545 is a potent PDHK inhibitor with IC50 of 36.8 nM and 6.4 nM for PDHK1 and PDHK2 , respectively. It failed to inhibit PDHK4 at higher concentrations(>10 nM), AZD7545 stimulates PDHK4 activity.TargetsPDHK2 ; PDHK1 6.4 nM; 36.8 nMIn vitroIn the presence of recombinant human PDHK2, AZD7545 increases PDH activity with EC50 of 5.2 nM. In primary rat hepatocytes, AZD7545 increases PDH activity with EC50 of 105 nM. AZD7545 inhibits PDHK activity by disrupting the interactions between PDHK2 and the inner lipoyl-bearing domains (L2) of the dihydrolipoyl transacetylase component (E2) of PDC.In vivoIn Wistar rats, AZD7545 increases the percentage of active PDH in the liver and skeletal muscle. In obese, insulin-resistant, Zucker rats, AZD7545 eliminates the postprandial elevation in blood glucose. Specifications and Purity: 98%. Molecular Formula: C19H18ClF3N2O5S. Molecular Weight: 478.87. PubChem CID: 16741245. Isomeric SMILES: C[C@@](C(=O)NC1=C(C=C(C=C1)S(=O)(=O)C2=CC=C(C=C2)C(=O)N(C)C)Cl)(C(F)(F)F)O. Related Document: https://ald-pub-files.oss-cn-shanghai.aliyuncs.com/aladdinsci/pdp/sds/1/A413767-SCI_bcee27f3cbedc898f4f80219809232f7.pdf