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Entacapone COMT inhibitor

Catalog No.A4168
Size Price Stock Qty
10mM (in 1mL DMSO)
$50.00
In stock
10mg
$50.00
In stock
100mg
$150.00
In stock

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Sample solution is provided at 25 µL, 10mM.

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Chemical structure

Entacapone

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Chemical Properties

Cas No. 130929-57-6 SDF Download SDF
Chemical Name (E)-2-cyano-3-(3,4-dihydroxy-5-nitrophenyl)-N,N-diethylprop-2-enamide
Canonical SMILES CCN(CC)C(=O)C(=CC1=CC(=C(C(=C1)O)O)[N+](=O)[O-])C#N
Formula C14H15N3O5 M.Wt 305.29
Solubility >13.1mg/mL in DMSO Storage Store at -20°C
General tips For obtaining a higher solubility , please warm the tube at 37 ℃ and shake it in the ultrasonic bath for a while.Stock solution can be stored below -20℃ for several months.
Shipping Condition Evaluation sample solution : ship with blue ice
All other available size: ship with RT , or blue ice upon request

Background

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 [1].

Entacapone has succbe used as an adjunct to standard levodopa-dopa decarboxylase inhibitor therapy in patients with Parkinson’s disease (PD), for its abilities to increase the bioavailability of levodopa by inhibiting the generation of 3-O-methyldopa and to prolong the duration and clinical benefit of levodopa [1].

Reference

References:
[1] Forsberg M, Lehtonen M, Heikkinen M, Savolainen J, Järvinen T, Männistö PT. Pharmacokinetics and pharmacodynamics of entacapone and tolcapone after acute and repeated administration: a comparative study in the rat. J Pharmacol Exp Ther. 2003 Feb;304(2):498-506.