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AKR1C1-IN-1

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Chemical Structure| 4906-68-7 同义名 : 3-bromo-5-phenyl Salicylic Acid;NSC 109116
CAS号 : 4906-68-7
货号 : A550789
分子式 : C13H9BrO3
纯度 : 99%+
分子量 : 293.113
MDL号 : MFCD18378258
存储条件：

粉末 Inert atmosphere,Room Temperature

液体 -20°C:3-6个月-80°C:12个月
溶解度 :

DMSO: 105 mg/mL(358.22 mM)，配合低频超声助溶，注意：DMSO长时间开封后，会吸水并导致溶解能力下降，请避免使用长期开封的DMSO
动物实验配方：
生物活性
描述 Human 20R-hydroxysteroid dehydrogenase (AKR1C1) plays an important role in progesterone metabolism and is essential for brain function. AKR1C1-IN-1 is a potent and selective AKR1C1 inhibitor with a Ki value of 4 ± 4nM. The Ki values of AKR1C1-IN-1 for AKR1C1-2, -3, and -4 are 87 ± 12nM, 4.2 ± 0.15μM, and 18.2 ± 2.5μM, respectively. AKR1C1-IN-1 potently inhibited the metabolism of progesterone with an IC50 value of 460nM.[1]
作用机制 AKR1C1-IN-1 is a potent AKR1C1 inhibitor. It targets a selectivity pocket in the active site of AKR1C1.[1]
实验方案
1mg 5mg 10mg

1 mM

5 mM

10 mM

3.41mL

0.68mL

0.34mL

17.06mL

3.41mL

1.71mL

34.12mL

6.82mL

3.41mL
参考文献

[1]El-Kabbani O, Scammells PJ, Gosling J, Dhagat U, Endo S, Matsunaga T, Soda M, Hara A. Structure-guided design, synthesis, and evaluation of salicylic acid-based inhibitors targeting a selectivity pocket in the active site of human 20alpha-hydroxysteroid dehydrogenase (AKR1C1). J Med Chem. 2009 May 28;52(10):3259-64. doi: 10.1021/jm9001633