Ezetimibe ketone(Synonyms: EZM-K)

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Ezetimibe ketone (Synonyms: EZM-K)

Ezetimibe ketone (EZM-K) 是 Ezetimibe 的 I 期代谢产物。Ezetimibe 是一种 NPC1L1 抑制剂,是有效的 Nrf2 激活剂,Ezetimibe 还是有效的胆固醇吸收抑制剂。

Ezetimibe ketone(Synonyms: EZM-K)

Ezetimibe ketone Chemical Structure

CAS No. : 191330-56-0

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生物活性

Ezetimibe ketone (EZM-K) is a phase-I metabolite of Ezetimibe. Ezetimibe is a Niemann-Pick C1-like1 (NPC1L1) inhibitor, and is a potent Nrf2 activator. Ezetimibe is a potent cholesterol absorption inhibitor[1][2][3].

IC50 & Target

NPC1L1, Nrf2[1]

分子量

407.41

Formula

C24H19F2NO3

CAS 号

191330-56-0

运输条件

Room temperature in continental US; may vary elsewhere.

储存方式

Please store the product under the recommended conditions in the Certificate of Analysis.

参考文献
  • [1]. Yijun Zhu, et al. Efficient and scalable process for the synthesis of antihypercholesterolemic drug ezetimibe. Synthetic Communications. 2016, 46:20, 1687-1693.

    [2]. Lee DH, et al. Ezetimibe, an NPC1L1 inhibitor, is a potent Nrf2 activator that protects mice from diet-induced nonalcoholic steatohepatitis. Free Radic Biol Med. 2016 Sep 12;99:520-532.

    [3]. Chang E, et al. Ezetimibe improves hepatic steatosis in relation to autophagy in obese and diabetic rats. World J Gastroenterol. 2015 Jul 7;21(25):7754-63.

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