产品说明书

Apocynin

Print
Chemical Structure| 498-02-2 同义名 : 4'-羟基-3'-甲氧基苯乙酮 ;Acetovanillone;Acetoguaiacone;NSC 209524;NSC 2146
CAS号 : 498-02-2
货号 : A113062
分子式 : C9H10O3
纯度 : 98%
分子量 : 166.174
MDL号 : MFCD00008747
存储条件:

粉末 Sealed in dry,Room Temperature

液体 -20°C:3-6个月-80°C:12个月

溶解度 :

DMSO: 105 mg/mL(631.87 mM),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

H2O: 3 mg/mL(18.05 mM),配合低频超声,并水浴加热至45℃助溶

动物实验配方:

2% DMSO+30% PEG 300+water 5 mg/mL

生物活性
描述 Apocynin is a most widely studied pan-NADPH-oxidase inhibitor and a scavenger of hydrogen peroxide, as well as inhibits rho kinases. Apocynin could eliminate hydrogen peroxid in a dose-dependent manner at concentration ranging in 3-100μM. Intraperitoneal injection with Apocynin at dose of 5mg/kg reduced lung injury and blocked NADPH oxidase activation in lung tissues by carrageenan in mice. The administration of Apocynin significantly reduced ICAM-1, P-selectin induced by carrageenan and attenuated neutrophil infiltration into the lung tissue. Also Apocynin attenuated carrageenan-induced TNF-α and IL-1β, iNOS expression, Fas ligand, apoptosis and Bax expression, as well as prevented carrageenan-induced inhibition of Bcl-2 expression and activation of NF-κB pathway and MAPK pathway at 4h post carrageenan injection. Some study showed that Apocynin may work as an antioxidant more than a NADPH oxidase inhibitor for apocynin failed to inhibit superoxide anion generation in HEK293 cells overexpressing NADPH oxidase isoforms (Nox1, Nox2, or Nox4).
作用机制 Apocynin is an oxidase assembly inhibitor which can inhibit association of p47phox with membrane-bound heterodimer.[5]
临床研究
NCT号 适应症或疾病 临床期 招募状态 预计完成时间 地点
NCT03376555 Microvascular Dysfunction Phase 1 Phase 2 Recruiting June 30, 2019 United States, Pennsylvania ... 展开 >> Pennsylvania State University Recruiting University Park, Pennsylvania, United States, 16802 收起 <<
NCT03680573 Cardiovascular Diseases ... 展开 >> Cardiovascular Risk Factor Vasoconstriction 收起 << Phase 1 Completed - United States, Texas ... 展开 >> Engineering Research Building Arlington, Texas, United States, 76019 收起 <<
NCT03680638 Cardiovascular Diseases ... 展开 >> Cardiovascular Risk Factor Vasodilation 收起 << Phase 1 Completed - United States, Texas ... 展开 >> Engineering Research Building Arlington, Texas, United States, 76019 收起 <<
实验方案
1mg 5mg 10mg

1 mM

5 mM

10 mM

6.02mL

1.20mL

0.60mL

30.09mL

6.02mL

3.01mL

60.18mL

12.04mL

6.02mL

参考文献

[1]Altenhöfer S, Radermacher KA, et al. Evolution of NADPH Oxidase Inhibitors: Selectivity and Mechanisms for Target Engagement. Antioxid Redox Signal. 2015 Aug 10;23(5):406-27.

[2]Stolk J, Hiltermann TJ, et al. Characteristics of the inhibition of NADPH oxidase activation in neutrophils by apocynin, a methoxy-substituted catechol. Am J Respir Cell Mol Biol. 1994 Jul;11(1):95-102.

[3]Impellizzeri D, Esposito E, et al. Effect of apocynin, a NADPH oxidase inhibitor, on acute lung inflammation. Biochem Pharmacol. 2011 Mar 1;81(5):636-48.

[4]Heumüller S, Wind S, et al. Apocynin is not an inhibitor of vascular NADPH oxidases but an antioxidant. Hypertension. 2008 Feb;51(2):211-7. Epub 2007 Dec 17.

[5]Drummond GR, Selemidis S, et al. Combating oxidative stress in vascular disease: NADPH oxidases as therapeutic targets. Nat Rev Drug Discov. 2011 Jun;10(6):453-71.