AZD-4017-DataSheet-MedChemExpress

发布于:2021-09-23 16:05:25

Product Data?Sheet
AZD 4017
Cat. No.: CAS No.: Molecular Formula: Molecular Weight: Target: Pathway: Storage: HY-18053 1024033-43-9 C??H??N?O?S 419.58 Others Others Please store the product under the recommended conditions in the COA.

Inhibitors ? Agonists ? Screening Libraries

Solvent & Solubility
In Vitro 10 mM in DMSO Mass 1 mg 5 mg 10 mg

Solvent Concentration Preparing Stock Solutions 5 mM 10 mM 1 mM

2.3833 mL 0.4767 mL 0.2383 mL

11.9167 mL 2.3833 mL 1.1917 mL

23.8334 mL 4.7667 mL 2.3833 mL

Please refer to the solubility information to select the appropriate solvent.

BIOLOGICAL ACTIVITY
Description AZD 4017 is a potent, selective 11β-Hydroxysteroid Dehydrogenase Type 1 (11β-HSD1) inhibitor, with an IC50 of 7 nM. IC?? & Target In Vitro IC50: 7 nM (11β-HSD1)[1]. 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

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4017 in this model[1].

REFERENCES
[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.

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