AZD 4017|1024033-43-9|-陌孚医药/Medlife

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AZD 4017

目录号: PL04772 纯度: ≥98%

CAS No. :1024033-43-9

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中文名称	AZD 4017
英文名称	AZD 4017
英文别名	2-[(3S)-1-[5-(cyclohexylcarbamoyl)-6-propylsulfanylpyridin-2-yl]piperidin-3-yl]acetic acid;AZD-4017;SureCN1967349;14M;{(3s)-1-[5-(Cyclohexylcarbamoyl)-6-(Propylsulfanyl)pyridin-2-Yl]piperidin-3-Yl}acetic Acid;2-[(3S)-1-[5-(cyclohexylcarbamoyl)-6-propylsulfanyl-pyridin-2-yl]-3-piperidyl]acetic acid;UNII-3JL137394Y;CHEMBL2153191;2-[(3S)-1-[5-(cyclohexylcarbamoyl)-6-propylsulfanylpyridin-2-yl]-3-piperidyl]acetic acid;2-[(3S)-1-[5-(cyclohexyl-carbamoyl)-6-propylsulfanyl-pyridin-2-yl]-3-piperidyl]acetic acid;AZD 4017;EOS-62043;(S)-2-(1-(5-(Cyclohexylcarbamoyl)-6-(propylthio)pyridin-2-yl)piperidin-3-yl)acetic acid;3-Piperidineacetic acid, 1-[5-[(cyclohexylaMino)carbonyl]-6-(propylthio)-2-pyridinyl]-, (3S)-;(S)-2-(1-(5-(CYCLOHEXYLCARBAMOYL)-6-(PROPYLTHIO)PYRIDIN-2-YL)PIPERIDIN-3-YL) ACETIC ACID (AZD 4017)
Cas No.	1024033-43-9
分子式	C₂₂H₃₃N₃O₃S
分子量	419.58
包装储存	Powder -20°C 3 years；4°C 2 years

产品详情

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 IC 50 of 7 nM.

性状

Solid

IC50 & Target[1][2]

IC50: 7 nM (11β-HSD1).

体外研究(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. has no

体内研究(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×IC 50 in the mouse, demonstrating the dose dependent inhibition of 11β-HSD1 by AZD 4017 in this model. has not independently confirmed the accuracy of these methods. They are for reference only.

运输条件

Room temperature in continental US; may vary elsewhere.

储存方式

Powder -20°C 3 years；4°C 2 years

ClinicalTrial

参考文献

[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.

溶解度数据	In Vitro: DMSO : 125 mg/mL (297.92 mM; Need ultrasonic)配制储备液

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产品使用指南

Data Sheet

1：一般建议：溶解度为Medlife测试数据，可能与文献描述存在差异。这是由于生产工艺和批次不同产生的正常现象。为了使其更好的溶解，请用37℃加热试管并在超声波水浴中震动片刻。不同批次产品溶解度各有差异，仅做参考，具体以实验方案为准。

2：储存条件：粉末-20°C一般情况可以保存3年，溶于溶剂-80°C一般情况可以保存1年。不同产品及不同批次产品可能存在差异，请细致阅读产品信息，并辅助参考相关文献描述。

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