AZD7545

SKU: orb1223173

Description

AZD7545 is an inhibitor of pyruvate dehydrogenase kinase 2 (PDHK2) (IC50 value of 6.4nM ) for the treatment of type 2 diabetes. AZD7545 activates pyruvate dehydrogenase in vivo and improves blood glucose control in obese (fa/fa) Zucker rats.

Key Properties

• CAS Number: 252017-04-2
• MW: 478.87
• Purity: >98% (HPLC)
• Formula: C₁₉H₁₈ClF₃N₂O₅S
• SMILES: O=C(N(C)C)c1ccc(S(=O)(=O)c2ccc(NC(=O)[C@@](C)(O)C(F)(F)F)c(Cl)c2)cc1
• Target: Hydroxylase
• Solubility: DMSO : ≥ 46 mg/mL; 96.06 mM

Bioactivity

• In Vivo:
  A single dose of AZD7545 (Oral administration; 10 mg/kg once a day (08: 00 h) or Twice a day (08: 00 and 18: 00 h); for 7 days) to Wistar rats increases the proportion of liver PDH in its active, dephosphorylated form in a dose-related manner. A single dose of 10 mg/kg also significantly elevates muscle PDH activity in obese Zucker (fa/fa) rats. Animal model: Obese male (fa/fa) Zucker rats. Dosage: 10 mg/kg. Administration: Oral administration; once a day (08: 00 h) or Twice a day (08: 00 and 18: 00 h); for 7 days. Result: Improved the control of blood glucose levels.
• In Vitro:
  AZD7545 (10 μM; 90 hours for BRAFV600E human melanoma cells and 120 hours for NRAS mut human melanoma cells) specifically suppresses growth of cells harboring BRAF and NRAS mutations as well as in inhibitor-resistant human melanoma. Cell Proliferation Assay Cell line: Human melanoma cells lines of BRAFV600E (A375, IGR37) and NRASmut (SKMel30, IPC298, MelJuso). Concentration: 10 μM. Incubation time: 90 hours (BRAFV600E human melanoma cells) and 120 hours (NRAS mut human melanoma cells). Result: Mediated growth suppression of BRAFV600E mutant and NRAS mut human melanoma cells.

Storage & Handling

• Storage: Storage temperature: -20°C. Stability: ≥ 2 years
• Expiration Date: 12 months from date of receipt.
• Disclaimer: For research use only

Alternative Names

AZD7545 | AZD-7545 | AZD 7545

Quick Database Links

Gene Symbol

Hydroxylase