AZD7545

SKU: orb1305472

Description

AZD7545 is a selective and potent inhibitor of pyruvate dehydrogenase kinase (PDHK). It is a valuable research tool for studying metabolic regulation, particularly in diabetes and oncology research, and has been utilized in both cellular and animal models to investigate glucose metabolism and insulin resistance.

Research Area

Metabolism Research

Key Properties

• CAS Number: 252017-04-2
• MW: 478.87
• Purity: 99.13% (May vary between batches)
• Formula: C₁₉H₁₈ClF₃N₂O₅S
• SMILES: CN(C)C(=O)c1ccc(cc1)S(=O)(=O)c1ccc(NC(=O)[C@@](C)(O)C(F)(F)F)c(Cl)c1
• Target: Dehydrogenase
• Solubility: DMSO:88 mg/mL (183.77 mM);10% DMSO+40% PEG300+5% Tween 80+45% Saline:3.3 mg/mL (6.89 mM);H2O:< 1 mg/mL (insoluble or slightly soluble);Ethanol:88 mg/mL (183.77 mM)

Bioactivity

• Target IC50:
  PDHK1:36.8 nM|PDHK2:6.4 nM
• In Vivo:
  AZD7545 inhibits pyruvate dehydrogenase kinase (PDHK) activity by disrupting the interaction between the inner lipoic acid domain of PDHK2 and the dihydrolipoamide acetyltransferase component of the pyruvate dehydrogenase complex (PDC). It increases the activity of pyruvate dehydrogenase (PDH) in primary rat hepatocytes with an EC50 of 105 nM. In the presence of recombinant human PDHK2, AZD7545 also enhances PDH activity, achieving an EC50 of 5.2 nM.
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• In Vitro:
  In obese, insulin-resistant Zucker rats, AZD7545 eliminated postprandial hyperglycemia. AZD7545 increased the percentage of active PDH in the liver and skeletal muscle of Wistar rats.
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Storage & Handling

• Storage: -20°C
• Expiration Date: 12 months from date of receipt.
• Disclaimer: For research use only

Alternative Names

AZD 7545, AZD-7545, AZD7545, inhibit, Inhibitor, Pyruvate dehydrogenase kinase, PDHK, PDHK1, PDH, PDH kinase, PDHK2

Compound Identifiers

PubChem CID

16741245