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AZD 4017

Name: AZD 4017
Brand: TargetMol
SKU: T14388
Price: 67 USD
Availability: InStock
Rating: 5 (10 reviews)

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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

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Purity: 99.61%

Catalog No. T14388Cas No. 1024033-43-9

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

Pack Size	Price	USA Warehouse	Global Warehouse
1 mg	$67	In Stock	In Stock
5 mg	$163	In Stock	In Stock
10 mg	$289	In Stock	In Stock
25 mg	$578	In Stock	In Stock
50 mg	$833	In Stock	In Stock
100 mg	$1,150	In Stock	In Stock
1 mL x 10 mM (in DMSO)	$178	In Stock	In Stock

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In Stock Estimated shipping dateUSA Warehouse[1-2 days] Global Warehouse[5-7 days]

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Purity:99.61%

Appearance:Solid

Color:White

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COA LCMS

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 Weight	419.58
Formula	C₂₂H₃₃N₃O₃S
Cas No.	1024033-43-9
Smiles	CCCSc1nc(ccc1C(=O)NC1CCCCC1)N1CCC[C@@H](CC(O)=O)C1
Relative Density.	1.22 g/cm3 (Predicted)

Storage & Solubility Information

Storage

Powder: -20°C for 3 years | In solvent: -80°C for 1 year | Shipping with blue ice/Shipping at ambient temperature.

Solubility Information

DMSO: 150 mg/mL (357.5 mM), Sonication is recommended.

In Vivo Formulation

10% DMSO+40% PEG300+5% Tween 80+45% Saline: 4 mg/mL (9.53 mM), Sonication is recommended.

Please add the solvents sequentially, clarifying the solution as much as possible before adding the next one. Dissolve by heating and/or sonication if necessary. Working solution is recommended to be prepared and used immediately. The formulation provided above is for reference purposes only. In vivo formulations may vary and should be modified based on specific experimental conditions.

Solution Preparation Table

DMSO

	1mg	5mg	10mg	50mg
1 mM	2.3833 mL	11.9167 mL	23.8334 mL	119.1668 mL
5 mM	0.4767 mL	2.3833 mL	4.7667 mL	23.8334 mL
10 mM	0.2383 mL	1.1917 mL	2.3833 mL	11.9167 mL
20 mM	0.1192 mL	0.5958 mL	1.1917 mL	5.9583 mL
50 mM	0.0477 mL	0.2383 mL	0.4767 mL	2.3833 mL
100 mM	0.0238 mL	0.1192 mL	0.2383 mL	1.1917 mL

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In Vivo Formulation Calculator (Clear solution)

Please enter your animal experiment information in the following box and click Calculate to obtain the stock solution preparation method and in vivo formula preparation method:

For example, if the intended dosage is 10 mg/kg for animals weighing 20 g , with a dosing volume of 100 μL per animal, TargetMol | Animal experiments

and a total of 10 animals are to be administered, using a formulation of TargetMol | reagent

10% DMSO+ 40% PEG300+ 5% Tween 80+ 45% Saline/PBS/ddH₂O , the resulting working solution concentration would be 2 mg/mL.

Stock Solution Preparation:

Dissolve 2 mg of the compound in 100 μL DMSO TargetMol | reagent to obtain a stock solution at a concentration of 20 mg/mL . If the required concentration exceeds the compound's known solubility, please contact us for technical support before proceeding.

Preparation of the In Vivo Formulation:

1) Add 100 μL of the DMSO TargetMol | reagent stock solution to 400 μL PEG300 and mix thoroughly until the solution becomes clear.

2) Add 50 μL Tween 80 and mix well until fully clarified.

3) Add 450 μL Saline,PBS or ddH₂O TargetMol | reagent and mix thoroughly until a homogeneous solution is obtained.

This example is provided solely to demonstrate the use of the In Vivo Formulation Calculator and does not constitute a recommended formulation for any specific compound. Please select an appropriate dissolution and formulation strategy based on your experimental model and route of administration.

All co-solvents required for this protocol, includingDMSO, PEG300/PEG400, Tween 80, SBE-β-CD, and Corn oil, are available for purchase on the TargetMol website.

Dose Conversion

You can also refer to dose conversion for different animals. More Dose Conversion

Tech Support

Please see Inhibitor Handling Instructions for more frequently ask questions. Topics include: how to prepare stock solutions, how to store products, and cautions on cell-based assays & animal experiments, etc