AZD7545

Term ID

CHEBI:49490

Synonyms

• (R)-4-(3-chloro-4-(3,3,3-trifluoro-2-hydroxy-2-methylpropanamido)phenylsulfonyl)-N,N-dimethylbenzamide
• 4-(3-chloro-4-{[(2R)-3,3,3-trifluoro-2-hydroxy-2-methylpropanoyl]amino}benzene-1-sulfonyl)-N,N-dimethylbenzamide
• 4-[(3-chloro-4-{[(2R)-3,3,3-trifluoro-2-hydroxy-2-methylpropanoyl]amino}phenyl)sulfonyl]-N,N-dimethylbenzamide
• AZD 7545
• AZD-7545

Definition

A sulfone that is benzene substituted by [4-(dimethylcarbamoyl)phenyl]sulfonyl, chloro and [(2R)-3,3,3-trifluoro-2-hydroxy-2-methylpropanoyl]amino groups at positions 1, 3 and 4, respectively. It is a potent and non-ATP-competitive inhibitor of pyruvate dehydrogenase kinase 2 (PDHK2) with IC₅₀ of 6.4 nM and exhibits glucose-lowering activity. Also inhibits PDHK1 at higher levels (IC₅₀ = 36.8 nM).

References

• cas:252017-04-2
• chemspider:20572552
• drugbank:DB07403
• lincs.smallmolecule:LSM-6250
• pdb-ccd:AZX
• pubmed:14641018
• pubmed:14641019
• pubmed:17602666
• pubmed:17683942
• pubmed:18658136
• pubmed:27757958
• pubmed:28199108
• pubmed:28595656
• pubmed:30028142
• pubmed:30597326
• pubmed:31495556
• pubmed:33125772

Ontology

ChEBI  ( EBI )