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AZD 4017

Catalog No. T14388Cas No. 1024033-43-9

AZD 4017 is an inhibitor of 11β-Hydroxysteroid Dehydrogenase Type 1(11β-HSD1) (IC50: 7 nM).

AZD 4017

AZD 4017

Purity: 99.39%
Catalog No. T14388Cas No. 1024033-43-9
AZD 4017 is an inhibitor of 11β-Hydroxysteroid Dehydrogenase Type 1(11β-HSD1) (IC50: 7 nM).
Pack SizePriceAvailabilityQuantity
1 mg$67In Stock
5 mg$163In Stock
10 mg$289In Stock
25 mg$578In Stock
50 mg$833In Stock
100 mg$1,150In Stock
1 mL x 10 mM (in DMSO)$178In Stock
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Purity:99.39%
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Product Introduction

Bioactivity
Description
AZD 4017 is an inhibitor of 11β-Hydroxysteroid Dehydrogenase Type 1(11β-HSD1) (IC50: 7 nM).
Targets&IC50
11β-HSD1:7 nM
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[1]. 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.
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[1].
Chemical Properties
Molecular Weight419.58
FormulaC22H33N3O3S
Cas No.1024033-43-9
Storage & Solubility Information
StoragePowder: -20°C for 3 years | In solvent: -80°C for 1 year | Shipping with blue ice.
Solubility Information
DMSO: 125 mg/mL (297.92 mM)
Solution Preparation Table
DMSO
1mg5mg10mg50mg
1 mM2.3833 mL11.9167 mL23.8334 mL119.1668 mL
5 mM0.4767 mL2.3833 mL4.7667 mL23.8334 mL
10 mM0.2383 mL1.1917 mL2.3833 mL11.9167 mL
20 mM0.1192 mL0.5958 mL1.1917 mL5.9583 mL
50 mM0.0477 mL0.2383 mL0.4767 mL2.3833 mL
100 mM0.0238 mL0.1192 mL0.2383 mL1.1917 mL

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