Powder: -20°C for 3 years | In solvent: -80°C for 1 year
AZD 4017 是高效的、选择性的11β-HSD1抑制剂,IC50为 7 nM。
规格 | 价格/CNY | 货期 | 数量 | |
---|---|---|---|---|
1 mg | ¥ 689 | 现货 | ||
5 mg | ¥ 1,620 | 现货 | ||
10 mg | ¥ 2,860 | 现货 | ||
25 mg | ¥ 4,760 | 现货 | ||
50 mg | ¥ 6,780 | 现货 | ||
100 mg | ¥ 9,180 | 现货 | ||
1 mL * 10 mM (in DMSO) | ¥ 1,710 | 现货 |
产品描述 | AZD 4017 is an inhibitor of 11β-Hydroxysteroid Dehydrogenase Type 1(11β-HSD1) (IC50: 7 nM). |
靶点活性 | 11β-HSD1:7 nM |
体外活性 | 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]. AZD 4017 displays excellent selectivity versus the related enzymes 11-βHSD2, 17β-HSD1, 17β-HSD3 (all IC50>30 μM). It 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. |
体内活性 | 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. Which demonstrating the dose dependent inhibition of 11β-HSD1 by AZD 4017 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)
可选溶剂 | 浓度 体积 质量 | 1 mg | 5 mg | 10 mg | 25 mg |
DMSO | 1 mM | 2.3833 mL | 11.9167 mL | 23.8334 mL | 59.5834 mL |
5 mM | 0.4767 mL | 2.3833 mL | 4.7667 mL | 11.9167 mL | |
10 mM | 0.2383 mL | 1.1917 mL | 2.3833 mL | 5.9583 mL | |
20 mM | 0.1192 mL | 0.5958 mL | 1.1917 mL | 2.9792 mL | |
50 mM | 0.0477 mL | 0.2383 mL | 0.4767 mL | 1.1917 mL | |
100 mM | 0.0238 mL | 0.1192 mL | 0.2383 mL | 0.5958 mL |
对于不同动物的给药剂量换算,您也可以参考 更多...
请在以下方框中输入您的动物实验信息后点击计算,可以得到母液配置方法和体内配方的制备方法: 比如您的给药剂量是10 mg/kg,每只动物体重20 g,给药体积100 μL,一共给药动物10 只,您使用的配方为5% DMSO+30% PEG300+5% Tween 80+60% ddH2O。那么您的工作液浓度为2 mg/mL。
母液配置方法:2 mg 药物溶于 50 μL DMSO (母液浓度为 40 mg/mL), 如您需要配置的浓度超过该产品的溶解度,请先与我们联系。
体内配方的制备方法:取 50 μL DMSO 主液,加入 300 μL PEG300, 混匀澄清,再加 50 μL Tween 80,混匀澄清,再加 600 μL ddH2O, 混匀澄清。
您可能有的问题的答案可以在抑制剂处理说明中找到,包括如何准备库存溶液,如何存储产品,以及基于细胞的分析和动物实验需要特别注意的问题。
AZD 4017 1024033-43-9 Metabolism Dehydrogenase AZD4017 inhibit AZD-4017 Inhibitor inhibitor