Powder: -20°C for 3 years | In solvent: -80°C for 1 year
AZD 4017 is an inhibitor of 11β-Hydroxysteroid Dehydrogenase Type 1(11β-HSD1) (IC50: 7 nM).
パッケージサイズ | 在庫状況 | 単価(税別) | |||
---|---|---|---|---|---|
サンプルについてお問い合わせ | |||||
1 mg | 在庫あり | ¥ 15,500 | |||
5 mg | 在庫あり | ¥ 37,500 | |||
10 mg | 在庫あり | ¥ 66,500 | |||
25 mg | 在庫あり | ¥ 133,000 | |||
50 mg | 在庫あり | ¥ 191,500 | |||
100 mg | 在庫あり | ¥ 264,000 | |||
1 mL * 10 mM (in DMSO) | 在庫あり | ¥ 41,000 |
ターゲット&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]. |
分子量 | 419.58 |
分子式 | C22H33N3O3S |
CAS No. | 1024033-43-9 |
Powder: -20°C for 3 years | In solvent: -80°C for 1 year
DMSO: 125 mg/mL (297.92 mM)
You can also refer to dose conversion for different animals. 詳細
bottom
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.
AZD 4017 1024033-43-9 Metabolism Dehydrogenase AZD4017 inhibit AZD-4017 Inhibitor inhibitor