1. Metabolic Enzyme/Protease
    Neuronal Signaling
  2. COMT
  3. Entacapone

Entacapone 

Cat. No.: HY-14280 Purity: 99.97%
Handling Instructions

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

For research use only. We do not sell to patients.

Entacapone Chemical Structure

Entacapone Chemical Structure

CAS No. : 130929-57-6

Size Price Stock Quantity
Free Sample (0.5-1 mg)   Apply now  
10 mM * 1 mL in DMSO USD 66 In-stock
Estimated Time of Arrival: December 31
10 mg USD 60 In-stock
Estimated Time of Arrival: December 31
50 mg USD 120 In-stock
Estimated Time of Arrival: December 31
100 mg USD 180 In-stock
Estimated Time of Arrival: December 31
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Customer Review

Based on 1 publication(s) in Google Scholar

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Description

Entacapone is a specific, potent, peripherally acting catechol-O-methyltransferase (COMT) inhibitor with IC50 of 151 nM for PD treatment. IC50 Value: 151 nM Target: COMT 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. 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 vivo: Levodopa/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. Clinical trial: The combination product carbidopa/levodopa/entacapone (CLE) was approved in 2003 for the treatment of PD patients.

Clinical Trial
Molecular Weight

305.29

Formula

C₁₄H₁₅N₃O₅

CAS No.

130929-57-6

SMILES

O=C(N(CC)CC)/C(C#N)=C/C1=CC([N+]([O-])=O)=C(O)C(O)=C1

Shipping

Room temperature in continental US; may vary elsewhere.

Storage
Powder -20°C 3 years
  4°C 2 years
In solvent -80°C 6 months
  -20°C 1 month
Solvent & Solubility
In Vitro: 

DMSO : 33.33 mg/mL (109.17 mM; Need ultrasonic)

H2O : 2 mg/mL (6.55 mM; ultrasonic and adjust pH to 10 with NaOH)

Preparing
Stock Solutions
Concentration Solvent Mass 1 mg 5 mg 10 mg
1 mM 3.2756 mL 16.3779 mL 32.7557 mL
5 mM 0.6551 mL 3.2756 mL 6.5511 mL
10 mM 0.3276 mL 1.6378 mL 3.2756 mL
*Please refer to the solubility information to select the appropriate solvent.
In Vivo:
  • 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

  • 2.

    Add each solvent one by one:  10% DMSO    90% (20% SBE-β-CD in saline)

    Solubility: ≥ 2.5 mg/mL (8.19 mM); Clear solution

  • 3.

    Add each solvent one by one:  10% DMSO    90% corn oil

    Solubility: 2.5 mg/mL (8.19 mM); Clear solution; Need warming

*All of the co-solvents are provided by MCE.
References

Purity: 99.97%

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Keywords:

EntacaponeCOMTCatechol-O-methyltransferaseInhibitorinhibitorinhibit

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Entacapone
Cat. No.:
HY-14280
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