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Chemical Structure| 130929-57-6 Chemical Structure| 130929-57-6
Chemical Structure| 130929-57-6

*Storage: Sealed in dry,2-8°C.

Entacapone

CAS No.: 130929-57-6

Entacapone is a specific, potent and peripherally acting catechol-O-methyltransferase (COMT) inhibitor with IC50 of 151 nM for PD treatment.

Synonyms: OR-611

4.5 *For Research Use Only !

Cat. No.: A102154 Purity: 95%

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Product Details of [ Entacapone ]

CAS No. :130929-57-6
Formula : C14H15N3O5
M.W : 305.29
SMILES Code : O=C(N(CC)CC)/C(C#N)=C/C1=CC([N+]([O-])=O)=C(O)C(O)=C1
Synonyms :
OR-611
MDL No. :MFCD00866580
InChI Key :JRURYQJSLYLRLN-BJMVGYQFSA-N
Pubchem ID :5281081

Safety of [ Entacapone ]

GHS Pictogram:
Signal Word:Warning
Hazard Statements:H315-H319-H335-H413
Precautionary Statements:P261-P273-P305+P351+P338

Biological Activity

Target
  • Histone Methyltransferase

    COMT, IC50:151 nM

Clinical Trial:

NCT Number Conditions Phases Recruitment Completion Date Locations
NCT00192855 Schizophrenia COMPLETED 2025-10-06 Rambam medical center, Haifa, ... More >>31096, Israel Less <<
NCT00237263 Parkinson's Disease PHASE2 COMPLETED 2025-07-07 Novartis Pharmaceuticals, East... More >> Hanover, New Jersey, 07936, United States Less <<

Protocol

Bio Calculators
Preparing Stock Solutions 1mg 5mg 10mg

1 mM

5 mM

10 mM

3.28mL

0.66mL

0.33mL

16.38mL

3.28mL

1.64mL

32.76mL

6.55mL

3.28mL

Dissolving Methods
Please choose the appropriate dissolution scheme according to your animal administration guide.For the following dissolution schemes, clear stock solution should be prepared according to in vitro experiments, and then cosolvent should be added in turn:

in order to ensure the reliability of the experimental results, the clarified stock solution can be properly preserved according to the storage conditions; The working fluid for in vivo experiment is recommended to be prepared now and used on the same day;

The percentage shown in front of the following solvent refers to the volume ratio of the solvent in the final solution; If precipitation or precipitation occurs in the preparation process, it can be assisted by heating and/or ultrasound.
Protocol 1
Add each solvent one by one:  10% DMSO    40% PEG300    5% Tween-80    45% Saline
Solubility: ≥ 2.5 mg/mL (8.19 mM); Clear solution
Protocol 2
Add each solvent one by one:  10% DMSO    90% Corn Oil
Solubility: 2.5 mg/mL (8.19 mM); Clear solution; Need warming
The prepared working fluid is recommended to be prepared now and used up as soon as possible in a short period of time. The percentage shown in front of the following solvent refers to the volume ratio of the solvent in the final solution; If precipitation or precipitation occurs in the preparation process, it can be assisted by heating and/or ultrasound.
Protocol 1
Add each solvent one by one:  PBS
Solubility: 1 mg/mL (3.28 mM); Clear solution; Need ultrasonic and warming and heat to 60°C

References

[1]Di Giovanni S, Eleuteri S, et al. Entacapone and tolcapone, two catechol O-methyltransferase inhibitors, block fibril formation of alpha-synuclein and beta-amyloid and protect against amyloid-induced toxicity. J Biol Chem. 2010 May 14;285(20):14941-54.

[2]Piccini P, Brooks DJ, et al. The catechol-O-methyltransferase (COMT) inhibitor entacapone enhances the pharmacokinetic and clinical response to Sinemet CR in Parkinson's disease. J Neurol Neurosurg Psychiatry. 2000 May;68(5):589-94.

[3]Funaki T, Onodera H, Ushiyama N, Tsukamoto Y, Tagami C, Fukazawa H, Kuruma I. The disposition of the tolcapone 3-O-methylated metabolite is affected by the route of administration in rats. J Pharm Pharmacol. 1994 Jul;46(7):571-4. doi: 10.1111/j.2042-7158.1994.tb03859.x. PMID: 7996385.

[4]De Santi C, Giulianotti PC, Pietrabissa A, Mosca F, Pacifici GM. Catechol-O-methyltransferase: variation in enzyme activity and inhibition by entacapone and tolcapone. Eur J Clin Pharmacol. 1998 May;54(3):215-9. doi: 10.1007/s002280050448. PMID: 9681662.

[5]Holm KJ, Spencer CM. Entacapone. A review of its use in Parkinson's disease. Drugs. 1999 Jul;58(1):159-77. doi: 10.2165/00003495-199958010-00017. PMID: 10439935.

[6]Li LS, Liu CZ, Xu JD, Zheng LF, Feng XY, Zhang Y, Zhu JX. Effect of entacapone on colon motility and ion transport in a rat model of Parkinson's disease. World J Gastroenterol. 2015 Mar 28;21(12):3509-18. doi: 10.3748/wjg.v21.i12.3509. PMID: 25834315; PMCID: PMC4375572.

[7]Heikkinen H, Varhe A, Laine T, Puttonen J, Kela M, Kaakkola S, Reinikainen K. Entacapone improves the availability of L-dopa in plasma by decreasing its peripheral metabolism independent of L-dopa/carbidopa dose. Br J Clin Pharmacol. 2002 Oct;54(4):363-71. doi: 10.1046/j.1365-2125.2002.01654.x. PMID: 12392583; PMCID: PMC1874436.

 

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