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AZD 4017

CAS No. : 1024033-43-9

MCE 站：AZD 4017

产品活性：AZD 4017 是一个有效的、11β-HSD1 的选择性抑制剂，其 IC₅₀ 值为 7 nM。

研究领域：Others

作用靶点：Others

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.

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.

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