AZD 4017

SKU: orb1308605

Description

AZD4017 is a potent and selective inhibitor of 11β-HSD1 with an IC50 of 7 nM. This compound is a valuable research tool for investigating the enzyme's role in metabolic diseases, including diabetes and obesity, in both cellular and animal models.

Research Area

Metabolism Research

Key Properties

• CAS Number: 1024033-43-9
• MW: 419.58
• Purity: 99.61% (May vary between batches)
• Formula: C₂₂H₃₃N₃O₃S
• SMILES: CCCSc1nc(ccc1C(=O)NC1CCCCC1)N1CCC[C@@H](CC(O)=O)C1
• Target: Dehydrogenase
• Solubility: 10% DMSO+40% PEG300+5% Tween 80+45% Saline:4 mg/mL (9.53 mM);DMSO:125 mg/mL (297.92 mM)

Bioactivity

• Target IC50:
  11β-HSD1:7 nM
• In Vivo:
  AZD 4017 exhibits dose-dependent inhibition of 11β-HSD1, with its effect being limited by lower potency against the mouse enzyme, restricting the scope of preclinical pharmacodynamic measurements. Increasing doses achieved a peak inhibition of roughly 70% at 1500 mg/kg, corresponding to 10×IC50 in mice, demonstrating the compound's efficacy in this model.
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• In Vitro:
  AZD 4017 exhibits significant inhibition of a crucial target tissue (IC50=0.002 μM), aligning well with its enzyme potency, suggesting its effectiveness in adipose tissue is not compromised by its acidic nature. It demonstrates remarkable selectivity against related enzymes 11-βHSD2, 17β-HSD1, and 17β-HSD3 (all IC50>30 μM), while showing negligible activity towards glucocorticoid and mineralocorticoid receptors. Although AZD 4017 is highly potent against the human variant of 11β-HSD1, its efficacy significantly diminishes across species, excluding cynomolgous monkey (IC50=0.029 μM). Considering adipose tissue as a critical organ, the compound's ability to inhibit 11β-HSD1 activity has been confirmed in isolated human adipocytes from nondiabetic volunteers.
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Storage & Handling

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

Alternative Names

11β-HSD1, AZD 4017, AZD4017, AZD-4017, inhibit, Inhibitor

Compound Identifiers

PubChem CID

24946280