AZD 4017|cas:1024033-43-9|西域试剂

AZD 4017,98.89%

产品编号：Bellancom-18053| CAS NO：1024033-43-9| 分子式：C₂₂H₃₃N₃O₃S| 分子量：419.58

本网站销售的所有产品仅用于工业应用或者科学研究等非医疗目的,不可用于人类或动物的临床诊断或者治疗,非药用,非食用，

货号	价格	库存与货期
Bellancom-18053	￥2000.00	杭州北京（现货）
Bellancom-18053	￥3500.00	杭州北京（现货）
Bellancom-18053	￥7000.00	杭州北京（现货）
Bellancom-18053	￥11200.00	杭州北京（现货）

增值税发票√顺丰快递√订货电话：18601927057

AZD 4017

产品介绍

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

生物活性

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

体外研究

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.

西域 has not independently confirmed the accuracy of these methods. They are for reference only.

体内研究

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.

西域 has not independently confirmed the accuracy of these methods. They are for reference only.

体内研究

西域 has not independently confirmed the accuracy of these methods. They are for reference only.

性状

Solid

溶解性数据

In Vitro:

DMSO : 125 mg/mL (297.92 mM; Need ultrasonic)

配制储备液

浓度溶剂体积质量	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

请根据产品在不同溶剂中的溶解度选择合适的溶剂配制储备液；一旦配成溶液，请分装保存，避免反复冻融造成的产品失效。
储备液的保存方式和期限：-80°C, 6 months; -20°C, 1 month。-80°C 储存时，请在 6 个月内使用，-20°C 储存时，请在 1 个月内使用。

In Vivo:

请根据您的实验动物和给药方式选择适当的溶解方案。以下溶解方案都请先按照 In Vitro 方式配制澄清的储备液，再依次添加助溶剂：

——为保证实验结果的可靠性，澄清的储备液可以根据储存条件，适当保存；体内实验的工作液，建议您现用现配，当天使用；以下溶剂前显示的百
分比是指该溶剂在您配制终溶液中的体积占比；如在配制过程中出现沉淀、析出现象，可以通过加热和/或超声的方式助溶

1.

请依序添加每种溶剂： 10% DMSO 40% PEG300 5% Tween-80 45% saline
Solubility: ≥ 2.08 mg/mL (4.96 mM); Clear solution

此方案可获得 ≥ 2.08 mg/mL (4.96 mM，饱和度未知) 的澄清溶液。
以 1 mL 工作液为例，取 100 μL 20.8 mg/mL 的澄清 DMSO 储备液加到 400 μL PEG300 中，混合均匀；向上述体系中加入50 μL Tween-80，混合均匀；然后继续加入 450 μL生理盐水定容至 1 mL。
将 0.9 g 氯化钠，完全溶解于 100 mL ddH₂O 中，得到澄清透明的生理盐水溶液
2.

请依序添加每种溶剂： 10% DMSO 90% corn oil
Solubility: ≥ 2.08 mg/mL (4.96 mM); Clear solution

此方案可获得 ≥ 2.08 mg/mL (4.96 mM，饱和度未知) 的澄清溶液，此方案不适用于实验周期在半个月以上的实验。
以 1 mL 工作液为例，取 100 μL 20.8 mg/mL 的澄清 DMSO 储备液加到 900 μL玉米油中，混合均匀。