A reversible COMT inhibitor (IC50s = 10

Entacapone – 50 mg

Brand:
Cayman
CAS:
130929-57-6
Storage:
-20
UN-No:
Non-Hazardous - /

Entacapone is a reversible catechol O-methyltransferase (COMT) inhibitor (IC50s = 10, 10, 20, and 160 nM for rat duodenum, brain, erythrocyte, and liver COMT, respectively).{42398} It is selective for COMT over monoamine oxidase A (MAO-A) and MAO-B and phenolsulphotransferase M (PST-M) and PST-P (IC50s = >50 µM). Entacapone (10 mg/kg), in combination with L-DOPA (Item No. 13248) and carbidopa (Item No. 23783), reduces 3-O-methyldopa (3-OMD) levels in the rat striatum and hypothalamus to 52 and 27%, respectively, of the levels in control animals receiving only L-DOPA and carbidopa.{22703} In a 6-OHDA rat model of Parkinson’s disease, entacapone (10 mg/kg), in combination with L-DOPA and benserazide (Item No. 20298), increases contralateral turning behavior and striatal extracellular dopamine levels.{42399} Entacapone also inhibits contraction of colon longitudinal muscle explants from a 6-OHDA rat model of Parkinson’s disease (EC50 = 200 µM).{42400} Formulations containing entacapone have been used in the treatment of Parkinson’s disease.  

 

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Description

A reversible COMT inhibitor (IC50s = 10, 10, 20, and 160 nM for rat duodenum, brain, erythrocyte, and liver COMT, respectively); selective for COMT over MAO-A, MAO-B, PST-M, and PST-P (IC50s = >50 µM); in combination with L-DOPA and carbidopa, reduces 3-OMD levels in the rat striatum and hypothalamus to 52 and 27%, respectively, of the levels in control animals receiving only L-DOPA and carbidopa; in combination with L-DOPA and benserazide, increases contralateral turning behavior and striatal extracellular dopamine levels in a 6-OHDA rat model of Parkinson’s disease; inhibits contraction of colon longitudinal muscle explants from a 6-OHDA rat model of Parkinson’s disease (EC50 = 200 µM)

Formal name: 2-cyano-3-(3,4-dihydroxy-5-nitrophenyl)-N,N-diethyl-2E-propenamide

Synonyms:  OR-611

Molecular weight: 305.3

CAS: 130929-57-6

Purity: ≥98%

Formulation: A crystalline solid

Application||Product Type|Biochemicals|Small Molecule Inhibitors|Methyltransferases||Research Area|Neuroscience|Neurodegenerative Disorders|Parkinson’s Disease

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