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    Entacapone (OR611)
    Entacapone (OR611)

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    This product is for research use only, not for human use. We do not sell to patients.
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    InvivoChem Cat #: V0402
    CAS #: 130929-57-6 Purity ≥98%

    Description: Entacapone (OR-611) is an approved anti-PD/Parkinson's Disease medication acting as a specific and peripherally active catechol-O-methyltransferase (COMT) inhibitor (IC50 = 151 nM). It is used in combination with levodopa and carbidopa for treating Parkinson's disease (PD).

    References: Eur J Clin Pharmacol. 1998 May;54(3):215-9; J Biol Chem. 2010 May 14;285(20):14941-54. 

    Related CAS: 1047659-02-8 (Entacapone sodium salt); 160391-70-8 (Entacapone acid; AG 1290; AG-1290; AG1290)

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    Molecular Weight (MW)305.29
    FormulaC14H15N3O5
    CAS No.130929-57-6
    Storage-20℃ for 3 years in powder form
    -80℃ for 2 years in solvent
    Solubility (In vitro)DMSO: 61 mg/mL (199.8 mM)
    Water:<1 mg/mL 
    Ethanol: 2 mg/mL (6.5 mM)
    Other info
    Chemical Name: (E)-2-cyano-3-(3,4-dihydroxy-5-nitrophenyl)-N,N-diethylacrylamide
    InChi Key: JRURYQJSLYLRLN-BJMVGYQFSA-N
    InChi Code: InChI=1S/C14H15N3O5/c1-3-16(4-2)14(20)10(8-15)5-9-6-11(17(21)22)13(19)12(18)7-9/h5-7,18-19H,3-4H2,1-2H3/b10-5+
    SMILES Code: O=C(N(CC)CC)/C(C#N)=C/C1=CC([N+]([O-])=O)=C(O)C(O)=C1 
    SynonymsOR 611; OR611; OR-611; Comtan; Entacapone; HSDB-8251; HSDB8251; HSDB 8251; 


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    In Vitro

    In vitro activity: 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. 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.


    Kinase Assay: Entacapone is a second-generation catechol-O-methyltransferase (COMT) inhibitor that potently inhibits rat liver total COMT with the half maximal inhibition concentration IC50 and inhibition constant Ki values of 20.1 nM and 10.7 nM respectively. The IC50 values of entacapone against rate liver soluble COMT (S-COMT) and rat liver membrane-bound COMT (MB-COMT) are 14.3 nM and 73.3 nM respectively 


    Cell Assay: 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. 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.

    In VivoLevodopa/carbidopa/entacapone has been shown to improve the pharmacokinetic profile of levodopa and provide superior symptomatic control compared with conventional levodopa/dopa decarboxylase inhibitor therapy. We report four case histories describing clinical experience of using levodopa/carbidopa/entacapone 200/50/200 mg, one of the latest doses of this formulation, in a range of patients with Parkinson's disease. These cases illustrate that levodopa/carbidopa/entacapone 200/50/200 mg provides improvements in symptomatic control.
    Animal model
    Formulation & Dosage
    References

    Eur J Clin Pharmacol. 1998 May;54(3):215-9; J Biol Chem. 2010 May 14;285(20):14941-54. 


    These protocols are for reference only. InvivoChem does not independently validate these methods.

    Entacapone
    Compounds have an inhibitory effect on the α-syn seeding polymerization. J Biol Chem. 2010 May 14; 285(20): 14941–14954.



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