An inhibitor of PDKs

AZD 7545 – 25 mg

Brand:
Cayman
CAS:
252017-04-2
Storage:
-20
UN-No:
De Minimis - 3077 / 9

AZD 7545 is an inhibitor of pyruvate dehydrogenase (PDH) kinases (PDKs), resulting in an increase in PDH activity with an EC50 value of 5.2 nM for PDK2.{31364,31365} It less potently inhibits PDK1 and PDK3 (IC50s = 87 and 600 nM, respectively).{31363} AZD 7545 stimulates pyruvate oxidation in rat hepatocytes (EC50 = 105 nM) and significantly elevates muscle PDH activity in obese Zucker rats.{31364} It elevates postprandial glucose levels and improves the 24 hour glucose profile in obese, insulin-resistant rats, compared with lean counterparts.{31364}  

 

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Description

An inhibitor of PDKs, resulting in an increase in PDH activity (EC50 = 5.2 nM for PDK2); less potently inhibits PDK1 and PDK3 (IC50s = 87 and 600 nM, respectively)

Formal name: 4-[[3-chloro-4-[[(2R)-3,3,3-trifluoro-2-hydroxy-2-methyl-1-oxopropyl]amino]phenyl]sulfonyl]-N,N-dimethyl-benzamide

Synonyms: 

Molecular weight: 478.9

CAS: 252017-04-2

Purity: ≥98%

Formulation: A crystalline solid

Product Type|Biochemicals|Kinase Inhibitors||Product Type|Biochemicals|Small Molecule Inhibitors|Kinases||Research Area|Cell Biology|Mitochondrial Biology||Research Area|Endocrinology & Metabolism|Metabolic Diseases|Diabetes||Research Area|Endocrinology & Metabolism|Metabolic Diseases|Obesity

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