An S-COMT inhibitor (IC50 = 300 nM in rat liver); is selective for S-COMT over tyrosine hydroxylase

Nitecapone – 10 mg

Brand:
Cayman
CAS:
116313-94-1
Storage:
-20
UN-No:
Non-Hazardous - /

Nitecapone is a reversible inhibitor of S-catechol-O-methyltransferase (S-COMT; IC50 = 300 nM in rat liver).{22704} It is selective for S-COMT over tyrosine hydroxylase, dopamine-β-hydroxylase, DOPA decarboxylase, monoamine oxidase A (MAO-A), and MAO-B (IC50s = >1 µM for all). In vivo, nitecapone inhibits liver, duodenal, and brain S-COMT (ID50s = 5, 5, and 25 mg/kg, respectively). Nitecapone (3–30 mg/kg) reduces 3-O-methyl-DOPA (3-OMD) formation and increases serum and brain L-DOPA, dopamine, and DOPAC levels when administered in combination with L-DOPA (Item No. 13248) and carbidopa (Item No. 23783). Nitecapone (30 mg/kg) reduces mechanical and cold allodynia in a rat model of spinal nerve ligation-induced neuropathy.{30152}  

 

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Description

An S-COMT inhibitor (IC50 = 300 nM in rat liver); is selective for S-COMT over tyrosine hydroxylase, dopamine-β-hydroxylase, DOPA decarboxylase, MAO-A, and MAO-B (IC50s = >1 µM for all); inhibits liver, duodenal, and brain S-COMT (ID50s = 5, 5, and 25 mg/kg, respectively); reduces 3-OMD formation and increases serum and brain L-DOPA, dopamine, and DOPAC levels when administered in combination with L-DOPA and carbidopa from 3-30 mg/kg; reduces mechanical and cold allodynia in a rat model of spinal nerve ligation-induced neuropathy at 30 mg/kg

Formal name: 3-[(3,4-dihydroxy-5-nitrophenyl)methylene]-2,4-pentanedione

Synonyms:  OR-462

Molecular weight: 265.2

CAS: 116313-94-1

Purity: ≥98%

Formulation: A crystalline solid

Application||Product Type|Biochemicals|Small Molecule Inhibitors|Methyltransferases||Research Area|Neuroscience|Pain Research

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