Home Epigenetics Histone Methyltransferase inhibitor - COMT inhibitor Entacapone For research use only.

Entacapone

Synonyms: OR-611

Entacapone (OR-611) inhibits catechol-O-methyltransferase(COMT) with IC50 of 151 nM. Entacapone can be used for the research of Parkinson's disease. Entacapone serves as a inhibitor of FTO demethylation with an IC50 of 3.5 μM, can be used for the research of metabolic disorders.

Entacapone Chemical Structure

Entacapone Chemical Structure

CAS: 130929-57-6

Selleck's Entacapone has been cited by 2 publications

Purity & Quality Control

Batch: S314701 DMSO] 61 mg/mL] false] Ethanol] 2 mg/mL] false] Water] Insoluble] false Purity: 99.98%
99.98

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Biological Activity

Description Entacapone (OR-611) inhibits catechol-O-methyltransferase(COMT) with IC50 of 151 nM. Entacapone can be used for the research of Parkinson's disease. Entacapone serves as a inhibitor of FTO demethylation with an IC50 of 3.5 μM, can be used for the research of metabolic disorders.
Targets
COMT [1]
151 nM
In vitro
In vitro

Entacapone inhibits catechol-O-methyltransferase(COMT) with similar IC50 in different tissues including live, duodenum, kidney and lung, but entacapone is more active than tolcapone in those tissues. [1]

Entacapone (< 100 μM) is a potent inhibitor of α-syn and β-amyloid (Aβ) oligomerization and fibrillogenesis, and also protects against extracellular toxicity induced by the aggregation of both proteins in PC12 cells. [2]
Cell Research Cell lines PC12 cells
Concentrations 5 μM
Incubation Time 72 h
Method

Cells were treated with various concentrations of drug for 72 h.
In Vivo
In vivo

Entacapone administration reduced body weight and lowered fasting blood glucose concentrations in diet-induced obese mice.
Animal Research Animal Models Male C57BL/6 mice
Dosages 600 mg/kg
Administration p.o.
NCT Number Recruitment Conditions Sponsor/Collaborators Start Date Phases
NCT02058966 Completed Methamphetamine Dependence Oregon Health and Science University|Portland VA Medical Center June 2014 Early Phase 1
NCT00547911 Terminated Parkinson Disease|Multiple System Atrophy|Autonomic Nervous System Diseases National Institute of Neurological Disorders and Stroke (NINDS)|National Institutes of Health Clinical Center (CC) October 2007 Phase 1|Phase 2
NCT00415922 Completed Healthy Novartis July 2006 Phase 1
NCT00415831 Completed Healthy Novartis June 2006 Phase 1
NCT00415844 Completed Healthy Novartis June 2006 Phase 1

Chemical lnformation & Solubility

Molecular Weight 305.29 Formula

C14H15N3O5
CAS No. 130929-57-6 SDF Download Entacapone SDF
Smiles CCN(CC)C(=O)C(=CC1=CC(=C(C(=C1)O)O)[N+](=O)[O-])C#N
Storage (From the date of receipt)

In vitro
Batch:

DMSO : 61 mg/mL ( (199.81 mM)； Moisture-absorbing DMSO reduces solubility. Please use fresh DMSO.)

Ethanol : 2 mg/mL

Water : Insoluble


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In vivo
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Method for preparing DMSO master liquid: mg drug pre-dissolved in μL DMSO ( Master liquid concentration mg/mL, Please contact us first if the concentration exceeds the DMSO solubility of the batch of drug. )

Method for preparing in vivo formulation: Take μL DMSO master liquid, next addμL PEG300, mix and clarify, next addμL Tween 80, mix and clarify, next add μL ddH2O, mix and clarify.

Method for preparing in vivo formulation: Take μL DMSO master liquid, next add μL Corn oil, mix and clarify.

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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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