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Entacapone | COMT inhibitor

CAS:
130929-57-6
Catalog Number:
10-2025
Activity:
COMT inhibitor – anti-Parkinsons
Chemical Name:
(2E)-2-Cyano-3-(3,4-dihydroxy-5-nitrophenyl)-N,N-diethyl-2-propenamide
Molecular Weight:
305.29
Molecular Formula:
C14H15N3O5
Solubility:
Soluble in DMSO (up to 30 mg/ml) or in Ethanol (up to 3 mg/ml)
Physical Properties:
Yellow solid
Purity:
98% by HPLC
NMR (Conforms)
Storage Temperature:
-20°C
Stability:
Stable for 1 year from date of purchase as supplied. Solutions in DMSO or ethanol may be stored at -20°C for up to 1 month.
Shipping Code:
RT

Entacapone (130929-57-6) is a potent catechol O-methyltransferase (COMT) inhibitor (IC50 = 14.3, 20.1 and 73.3 nM for rat liver soluble COMT, total COMT and membrane-bound COMT respectively).1 Increases bioavailability of L-DOPA as adjunct therapy for Parkinson’s disease.2 Entacapone inhibits α-synuclein aggregation in vitro and inhibits α-synuclein-induced cell death in PC-12 cells.3 Antioxidant. Inhibits oxidative stress-induced cell death.4

References/Citations:

1) Forsberg et al. (2003), Pharmacokinetics and pharmacodynamics of entacapone and tolcapone after acute and repeated administration: a comparative study in the rat; J. Pharmacol. Exp. Ther., 304 498
2) Merello et al. (1994), Effect of entacapone, a peripherally acting catechol-O-methyltransferase inhibitor, on the motor response to acute treatment with levodopa in patients with Parkinson’s disease; J. Neurol. Neurosurg. Psychiatry, 57 186
3) Giovanni et al. (2010), 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., 285 14941
4) Chen et al. (2016), Entacapone is an Antioxident More Potent than Vitamin C and Vitamin E for Scavenging of Hypochlorous Acid and Peroxynitrite, and the Inhibition of Oxidative Stress-induced Cell Death; Med. Sci. Monit., 22 687

Entacapone | COMT inhibitor is also available in the Cellular Metabolism Library.
CAS:
130929-57-6
Catalog Number:
10-2025
Activity:
COMT inhibitor – anti-Parkinsons
Chemical Name:
(2E)-2-Cyano-3-(3,4-dihydroxy-5-nitrophenyl)-N,N-diethyl-2-propenamide
Molecular Weight:
305.29
Molecular Formula:
C14H15N3O5
Solubility:
Soluble in DMSO (up to 30 mg/ml) or in Ethanol (up to 3 mg/ml)
Physical Properties:
Yellow solid
Purity:
98% by HPLC
NMR (Conforms)
Storage Temperature:
-20°C
Stability:
Stable for 1 year from date of purchase as supplied. Solutions in DMSO or ethanol may be stored at -20°C for up to 1 month.
Shipping Code:
RT

Safety Data Sheet:

N/A

Product Data Sheet:

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