Shopping Cart
- Remove All
- Your shopping cart is currently empty
AZD 4017 is an inhibitor of 11β-Hydroxysteroid Dehydrogenase Type 1(11β-HSD1) (IC50: 7 nM).
Pack Size | Price | Availability | Quantity |
---|---|---|---|
1 mg | $67 | In Stock | |
5 mg | $163 | In Stock | |
10 mg | $289 | In Stock | |
25 mg | $578 | In Stock | |
50 mg | $833 | In Stock | |
100 mg | $1,150 | In Stock | |
1 mL x 10 mM (in DMSO) | $178 | In Stock |
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]. |
Molecular Weight | 419.58 |
Formula | C22H33N3O3S |
Cas No. | 1024033-43-9 |
Storage | Powder: -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
|
Copyright © 2015-2024 TargetMol Chemicals Inc. All Rights Reserved.