Apocynin Chemical Structure

Apocynin Chemical Structure
Molecular Weight: 166.17

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Product Information

Product Description

Biological Activity

Description Apocynin is a selective NADPH-oxidase inhibitor with IC50 of 10 μM.
Targets NADPH-oxidase [1]
IC50 10 μM
In vitro Apocynin is a naturally occurring methoxy-substituted catechol used as an inhibitor of NADPH-oxidase. Apocynin prevents serine phosphorylation of p47phox and blocks its association with gp91phox, thus blunting NADPH oxidase activation. [2] Apocynin can decrease the production of superoxide (O(2)(-)) from activated neutrophils and macrophages. Apocynin, after metabolic conversion, inhibits the assembly of NADPH-oxidase that is responsible for reactive oxygen species (ROS) production. [3]
In vivo Apocynin has anti-inflammatory activity in a variety of cell and animal models of inflammation. Apocynin attenuates the TNF-α and IL-1β production and iNOS expression in the lung of carrageenan-treated mice. [4] Apocynin exerts beneficial effects in a mice model of spinal cord injury. Apocynin reduces (1) the degree of spinal cord damage, (2) neutrophils infiltration, (3) ICAM-1 and P-selectin expression, (4) PAR and nitrotyrosine formation, (5) IκB-α degradation, (6) NF-κB activation, (7) pro-inflammatory cytokines production (TNF-α and IL-1β), (8) apoptosis (TUNEL staining, FAS ligand expression, Bax and Bcl-2 expression) and (9) MAPK activation (P-38 and phospho-JNK). [5] LD50: Mice 9g/kg (i.g.). [3]

Conversion of different model animals based on BSA (Value based on data from FDA Draft Guidelines)

SpeciesMouseRatRabbitGuinea pigHamsterDog
Weight (kg)
Body Surface Area (m2)0.0070.0250.
Km factor36128520
Animal A (mg/kg) = Animal B (mg/kg) multiplied by  Animal B Km
Animal A Km

For example, to modify the dose of resveratrol used for a mouse (22.4 mg/kg) to a dose based on the BSA for a rat, multiply 22.4 mg/kg by the Km factor for a mouse and then divide by the Km factor for a rat. This calculation results in a rat equivalent dose for resveratrol of 11.2 mg/kg.

Rat dose (mg/kg) = mouse dose (22.4 mg/kg) ×  mouse Km(3)  = 11.2 mg/kg
rat Km(6)


[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.

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Clinical Trial Information( data from http://clinicaltrials.gov, updated on 2016-07-30)

NCT Number Recruitment Conditions Sponsor
Start Date Phases
NCT01402297 Completed Chronic Obstructive Pulmonary Disease Medical Universtity of Lodz|Ministry of Science and Highe  ...more Medical Universtity of Lodz|Ministry of Science and Higher Education, Poland October 2010 Phase 1
NCT00992667 Completed Bronchial Asthma Medical Universtity of Lodz|Ministry of Science and Highe  ...more Medical Universtity of Lodz|Ministry of Science and Higher Education, Poland June 2008 Phase 1

Chemical Information

Download Apocynin SDF
Molecular Weight (MW) 166.17


CAS No. 498-02-2
Storage 3 years -20℃powder
2 years -80℃in solvent
Synonyms Acetovanillone
Solubility (25°C) * In vitro DMSO 33 mg/mL (198.59 mM)
Ethanol 33 mg/mL (198.59 mM)
Water <1 mg/mL
In vivo 2% DMSO+30% PEG 300+ddH2O 5mg/mL
* <1 mg/ml means slightly soluble or insoluble.
* Please note that Selleck tests the solubility of all compounds in-house, and the actual solubility may differ slightly from published values. This is normal and is due to slight batch-to-batch variations.
Chemical Name Ethanone, 1-(4-hydroxy-3-methoxyphenyl)-

Tech Support

Answers to questions you may have can be found in the inhibitor handling instructions. Topics include how to prepare stock solutions, how to store inhibitors, and issues that need special attention for cell-based assays and animal experiments.

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