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首页-小分子抑制剂&激动剂-Metabolic Enzyme/Protease-11β-HSD-AZD 4017
AZD 4017

Chemical Structure : AZD 4017

CAS No.: 1024033-43-9

AZD 4017 (AZD4017, AZD-4017)

货号: PC-61987Not For Human Use, Lab Use Only.

AZD4017 (AZD-4017) is a potent, selective, and orally bioavailable human 11β-HSD1 with IC50 of 7 nM, shows no significant activity against 11β-HSD1 and 17β-HSD1, 17β-HSD3 (IC50>30 uM).

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纯度 & COA & 质检文件 纯度: >98% (HPLC) Select Batch:

生物&药学活性

AZD4017 (AZD-4017) is a potent, selective, and orally bioavailable human 11β-HSD1 with IC50 of 7 nM, shows no significant activity against 11β-HSD1 and 17β-HSD1, 17β-HSD3 (IC50>30 uM).
AZD4017 is inactive (<25% inhibition at 10 μM) against Cytochrome P450 enzymes (CYP1A2, CYP2C9, CYP2C19, CYP2D6, and CYP3A4), and lower potency against the mouse, rat and dog 11β-HSD1 (IC50=750-4000 nM).
AZD4017 demonstrates the dose dependent inhibition of 11β-HSD1 in vivo.

物理化学性质&存储条件

分子量 419.58
分子式 C22H33N3O3S
外观性状 Solid
CAS No.
储存条件
固体粉末
-20 °C 12 个月; 4°C 6 个月
配置液
-80 °C 6 个月; -20°C 6 个月
Shipping
Solubility

10 mM in DMSO

Chemical Name/SMILES

2-[(3S)-1-[5-(cyclohexylcarbamoyl)-6-propylsulfanylpyridin-2-yl]-3-piperidyl]acetic acid

参考文献

1. Scott JS, et al. J Med Chem. 2012 Jun 28;55(12):5951-64.

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