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Apocynin

Apocynin (NSC 2146) 是一种选择性NADPH-氧化酶抑制剂，IC50为10 μM。

CAS号

498-02-2

分子式

C9H10O3

主要靶点

Apoptosis|NADPH|Autophagy

仅限科研使用

Cat No : CM00726

Print datasheet

Synonyms

Acetovanillone|香草乙酮|Acetoguaiacone|罗布麻宁|NSC 2146

验证数据展示

  • CAS No.: 498-02-2

    Apocynin
    CAS#: 498-02-2

产品信息

Apocynin (NSC 2146) is a specific NADPH-oxidase inhibitor (IC50: 10 μM).

CAS号 498-02-2
分子式 C9H10O3
主要靶点 Apoptosis|NADPH|Autophagy
主要通路 代谢|凋亡|自噬
分子量 166.17
纯度 99.71%， 此纯度可做参考，具体纯度与批次有关系，可咨询客服
储存条件 Powder: -20°C for 3 years | In solvent: -80°C for 1 year
别名 Acetovanillone|香草乙酮|Acetoguaiacone|罗布麻宁|NSC 2146

靶点活性

NADPH-oxidase:10 μM

体内活性

经代谢转化后,Apocynin可抑制NADPH氧化酶的组装,这也许是因为活性氧(ROS)的产生。Apocynin抑制p47phox的丝氨酸磷酸化,并使其与gp91phox的联系被阻断,从而使NADPH氧化酶的活性钝化。 Apocynin可降低活化的巨噬细胞和嗜中性粒细胞中超氧化物(O(2)(-))的产生。

体外活性

Apocynin降低中性粒细胞浸润,脊髓损伤的程度,PAR和硝基酪氨酸形成,ICAM-1和P选择素表达,IκB-α降解,NF-κB激活,细胞凋亡(TUNEL着色,FAS配体表达,Bax和Bcl-2表达),促炎性细胞因子产生(TNF-α和IL-1β)及MAPK活化(P-38和磷酸化-JNK).对小鼠的LD50为 9 g/kg（p.o.）.Apocynin在各种炎症细胞和动物模型中均有抗炎活性.Apocynin可减弱角叉菜胶处理的小鼠肺中TNF-α和IL-1β的产生,及iNOS的表达. Apocynin在脊髓受伤的小鼠模型中具有有益作用.

溶解度

DMSO:16.6 mg/mL (100 mM),Ethanol:16.6 mg/mL (100 mM)

参考文献

1.Stolk J,et al. Am J Respir Cell Mol Biol, 1994, 11(1), 95-102.
2.Simons JM, et al. Free Radic Biol Med, 1990, 8(3), 251-258.
3.Stefanska J, et al. Mediators Inflamm, 2008, 106507.
4.Impellizzeri D, et al. Biochem Pharmacol, 2011, 81(5), 636-648.
5.Impellizzeri D, et al. Free Radic Res, 2011, 45(2), 221-236.
6.Deng Zheng, Fei Shi, Zheng Zhou, Feng Sun, Menghao Sun, Qian Sun, Lei Chen et al. M1 macrophage mediated increased reactive oxygen species (ROS) influence wound healing via the MAPK signaling in vitro and in vivo [J]. Toxicology and Applied Pharmacology. 2019 Mar 1;366:83-95.

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