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AZD 4017 

Cat. No.: HY-18053
Handling Instructions

AZD 4017 is a potent, selective 11β-Hydroxysteroid Dehydrogenase Type 1 (11β-HSD1) inhibitor, with an IC50 of 7 nM.

For research use only. We do not sell to patients.

AZD 4017 Chemical Structure

AZD 4017 Chemical Structure

CAS No. : 1024033-43-9

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  • Biological Activity

  • Technical Information

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  • References

Description

AZD 4017 is a potent, selective 11β-Hydroxysteroid Dehydrogenase Type 1 (11β-HSD1) inhibitor, with an IC50 of 7 nM.

IC50 & Target

IC50: 7 nM (11β-HSD1)[1].

In Vitro

AZD 4017 displays excellent selectivity versus the related enzymes 11-βHSD2, 17β-HSD1, 17β-HSD3 (all IC50>30 μM) and shows no measurable activity against the glucocorticoid and mineralocorticoid receptors. Despite having high potency for the human form of 11β-HSD1, AZD 4017 shows much reduced activity across species with the exception of cynomolgous monkey (IC50=0.029 μM). Additionally, as it is believed that adipose is a key target organ, inhibition of 11β-HSD1 activity is measured in isolated human adipocytes from nondiabetic volunteers. AZD 4017 is shown to be a potent inhibitor in this key target tissue (IC50=0.002 μM) in good agreement with the enzyme potency, thus providing some confidence that AZD 4017 is not restricted from adipose tissue by the fact that it was acidic[1].

In Vivo

Since AZD 4017 has lower potency against the mouse enzyme, only a limited number of preclinical pharmacodynamic measurements are performed. Increasing the dose further led to a maximal effect of approximately 70% inhibition at 1500 mg/kg, equivalent to 10×IC50 in the mouse, demonstrating the dose dependent inhibition of 11β-HSD1 by AZD 4017 in this model[1].

Clinical Trial
Solvent & Solubility
In Vitro: 

10 mM in DMSO

Preparing
Stock Solutions
Concentration Solvent Mass 1 mg 5 mg 10 mg
1 mM 2.3833 mL 11.9167 mL 23.8334 mL
5 mM 0.4767 mL 2.3833 mL 4.7667 mL
10 mM 0.2383 mL 1.1917 mL 2.3833 mL
*Please refer to the solubility information to select the appropriate solvent.
References
Molecular Weight

419.58

Formula

C₂₂H₃₃N₃O₃S

CAS No.

1024033-43-9

SMILES

O=C(O)C[[email protected]]1CN(C2=NC(SCCC)=C(C(NC3CCCCC3)=O)C=C2)CCC1

Storage

Please store the product under the recommended conditions in the Certificate of Analysis.

Shipping

Room temperature in continental US; may vary elsewhere

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Product Name:
AZD 4017
Cat. No.:
HY-18053
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AZD 4017

Cat. No.: HY-18053