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AZD 4017

Catalog No. T14388 CAS 1024033-43-9

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

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AZD 4017, CAS 1024033-43-9

Pack Size	Availability	Price/USD
1 mg	In stock	$ 67.00
5 mg	In stock	$ 163.00
10 mg	In stock	$ 289.00
25 mg	In stock	$ 578.00
50 mg	In stock	$ 833.00
100 mg	In stock	$ 1,150.00
1 mL * 10 mM (in DMSO)	In stock	$ 178.00

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Biological Description

Chemical Properties

Storage & Solubility Information

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

Solubility Information

DMSO: 125 mg/mL (297.92 mM)

References and Literature

1. Scott JS, et al. Discovery of a potent, selective, and orally bioavailable acidic 11β-hydroxysteroid dehydrogenase type 1 (11β-HSD1) inhibitor: discovery of 2-[(3S)-1-[5-(cyclohexylcarbamoyl)-6-propylsulfanylpyridin-2-yl]-3-piperidyl]acetic acid (AZD4017). J Med Chem. 2012 Jun 28;55(12):5951-64.

Related compound libraries

This product is contained In the following compound libraries：

Drug Repurposing Compound Library Inhibitor Library Clinical Compound Library Anti-Cancer Metabolism Compound Library Bioactive Compounds Library Max Bioactive Compound Library Metabolism Compound Library ReFRAME Related Library

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Method for preparing DMSO master liquid: mg drug pre-dissolved in μL DMSO (Master liquid concentration mg/mL)，Please contact us first if the concentration exceeds the DMSO solubility of the batch of drug.

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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.

Keywords

AZD 4017 1024033-43-9 Metabolism Dehydrogenase AZD4017 inhibit AZD-4017 Inhibitor inhibitor

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