| Description | Apocynin (NSC 2146) is a specific NADPH-oxidase inhibitor (IC50: 10 μM). |
| In vitro | 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. |
| In vivo | 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。 |
| Target activity | NADPH oxidase:10 μM |
| Synonyms | 香草乙酮, Acetovanillone, Acetoguaiacone, NSC 2146, 罗布麻宁 |
| molecular weight | 166.17 |
| Molecular formula | C9H10O3 |
| CAS | 498-02-2 |
| Storage | Powder: -20°C for 3 years | In solvent: -80°C for 1 year |
| Solubility | DMSO: 45 mg/mL (270.81 mM) Ethanol: 16.6 mg/mL (100 mM) |
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