BI-135585

SKU: orb1701054

Description

BI-135585 is a potent and selective oral inhibitor of human 11β-HSD1, an enzyme implicated in metabolic disorders. It is a valuable research tool for investigating type 2 diabetes mechanisms, enabling both in vitro enzymatic assays and in vivo studies of glucocorticoid metabolism.

Research Area

Metabolism Research

Key Properties

• CAS Number: 1114561-85-1
• MW: 460.57
• Purity: 99.70% (May vary between batches)
• Formula: C₂₈H₃₂N₂O₄
• SMILES: C(C(C)(C)O)[C@]1(OC(=O)N([C@@H](C)C2=CC=C(C=C2)C3=CC(=O)N(C)C=C3)CC1)C4=CC=CC=C4
• Target: Dehydrogenase

Bioactivity

• Target IC50:
  the enzyme activity in perirenal adipose tissue (cynomolgus monkey):10 nM|conversion of corticosterone to cortisol:11 nM|11β-HSD1:1 nM|the enzyme activity in abdominal subcutaneous adipose tissue (cynomolgus monkey):100 nM
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• In Vivo:
  BI-135585 (compound 11j; 1-3 mg/kg; orally) inhibited the enzyme activity in perirenal adipose tissue of cynomolgus monkeys by 67% and 90%, respectively.
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• In Vitro:
  BI-135585 interacts with the substrate binding pocket of the 11β-HSD1 active site. In human preadipocytes, its inhibition of 11β-HSD1 activity was evaluated and found to have an average IC50 of 1 nM. In isolated human adipose tissue, BI-135585 blocked the conversion of corticosterone to cortisol at an average IC50 of 11 nM. A study of abdominal subcutaneous and perirenal adipose tissue from a male cynomolgus monkey showed that BI-135585 (20 hours of action) exhibited dose-dependent inhibition of the enzyme activity in perirenal adipose tissue with an IC50 of approximately 10 nM, while in abdominal subcutaneous adipose tissue the IC50 was approximately 100 nM.
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Storage & Handling

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

Alternative Names

BI135585, BI-135585, BI 135585

Compound Identifiers

PubChem CID

44476893