|1-(4-羟基-3-甲氧基苯基)乙酮|CsnPharm

CAS No.: 498-02-2

香草乙酮 Catalog No. CSN12681

Synonyms: Acetovanillone;Acetoguaiacone;NSC 2146

Apocynin is potent and selective NADPH-oxidase inhibitor with IC50 value of 10 μM.

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纯度 & 质量文件批次:

靶点选择性

生物活性

实验方案

技术信息

生物活性

靶点 NADPH Oxidase

IC50:10μM
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]

动物研究
剂量	Rat: 20 mg/kg - 40 mg/kg^[6] (i.p.), 5 mg/kg^[7] (i.p.); 16 mg/kg^[8] (p.o.) Mice: 0.05 mg/kg - 5 mg/kg^[9] (s.c.) Mongolian gerbil: 100 mg/kg, 200 mg/kg^[10] (p.o.)
给药途径	i.p., p.o., s.c.

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 ... more >> Pennsylvania State University Recruiting University Park, Pennsylvania, United States, 16802 Collapse <<
NCT03680573	Cardiovascular Diseases ... more >> Cardiovascular Risk Factor Vasoconstriction Collapse <<	Phase 1	Completed	-	United States, Texas ... more >> Engineering Research Building Arlington, Texas, United States, 76019 Collapse <<
NCT03680638	Cardiovascular Diseases ... more >> Cardiovascular Risk Factor Vasodilation Collapse <<	Phase 1	Completed	-	United States, Texas ... more >> Engineering Research Building Arlington, Texas, United States, 76019 Collapse <<

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参考文献

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
- 6.0178 mL
- 30.0890 mL
- 60.1779 mL
- 5 mM
- 1.2036 mL
- 6.0178 mL
- 12.0356 mL
- 10 mM
- 0.6018 mL
- 3.0089 mL
- 6.0178 mL

技术信息

CAS号

498-02-2

储存条件

粉末: Sealed in dry,Room Temperature

液体: -20°C:3-6 月 -80°C:12月

分子式

C9H10O3

运输

蓝冰

分子量

166.17

别名

Acetovanillone;Acetoguaiacone;NSC 2146;NSC-209524;香草乙酮

溶解度

DMSO	33.0 mg/mL (198.6 mM)
Water	Insoluble
Ethanol	33.0 mg/mL (198.6 mM)

动物实验配方

2% DMSO+30% PEG 300+water

5 mg/mL

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香草乙酮 Catalog No. CSN12681

靶点选择性

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