|5-溴-4-羟基-[1,1'-联苯]-3-羧酸|CsnPharm

CAS No.: 4906-68-7

AKR1C1-IN-1 Catalog No. CSN23670

Synonyms: 3-bromo-5-phenyl Salicylic Acid;NSC 109116

3-bromo-5-phenyl Salicylic Acid is a cell-permeable salicylic acid compound that acts as a highly potent, active-site directed and substrate competitive AKR1C1 inhibitor (Ki = 4 nM) with moderate to excellent selectivity over AKR1C2, AKR1C3 and AKR1C4 (Ki = 0.087, 4.2 and 18.2 µM, respectively).

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400-920-2911

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技术信息

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 K_i value of 4 ± 4nM. The K_i 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]
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

实验方案

计算器摩尔计算器总药量计算器工作液计算器
储存液制备
- 1 mg
- 5 mg
- 10 mg
- 1 mM
- 3.4117 mL
- 17.0583 mL
- 34.1166 mL
- 5 mM
- 0.6823 mL
- 3.4117 mL
- 6.8233 mL
- 10 mM
- 0.3412 mL
- 1.7058 mL
- 3.4117 mL

技术信息

CAS号	4906-68-7	储存条件	粉末 Inert atmosphere,Room Temperature 液体 -20°C:3-6 月 -80°C:12月
分子式	C13H9BrO3	运输	蓝冰
分子量	293.11	别名	3-bromo-5-phenyl Salicylic Acid;NSC 109116

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