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Nitecapone Sale

(Synonyms: 硝替卡朋,OR-462) 目录号 : GC14223

A selective S-COMT inhibitor

Nitecapone Chemical Structure

Cas No.:116313-94-1

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5mg
¥1,016.00
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10mg
¥1,935.00
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25mg
¥4,060.00
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Sample solution is provided at 25 µL, 10mM.

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产品描述

Nitecapone is S-COMT inhibitor [1].

Catechol-O-methyltransferase (COMT) plays an essential role in normal brain function and has been implicated in human disorders, such as Parkinson's disease. The COMT has been involved in the degradation of catecholamines including dopamine, epinephrine, and norepinephrine. [1].

In vitro: Nitecapone is a highly effective inhibitor of rat S-COMT with IC50 values of about 300 nM in the liver and 20 nM in the brain tissues. The Ki value in the rat liver was 23 nM. In pure recombinant COMT enzyme forms, the Ki value of nitecapone was around 1 nM [1]. Nitecapone was selective for COMT, inhibiting dopamine-β-hydroxylase, tyrosine hydroxylase, DOPA decarboxylase, and monoamine oxidase-A/B with IC50 values in the micromolar range [1].

In vivo: In rats, oral administration of nitecapone (3-30 mg/kg) in combination with levodopa and carbidopa effectively reduced 3-OMD formation and elevated serum and brain l-dopa, dopamine, DOPAC, and HVA levels. Nitecapone prevented ischemia-reperfusion injury in experimental heart surgery in rats. Nitecapone increased bicarbonate secretion from rat and human duodenum after both i.v. and intraluminal administration. High concentrations of nitecapone increased synthesis and secretion of gastric sulfomucin [1].

Reference:
[1] Mnnist P T, Kaakkola S.  Catechol-O-methyltransferase (COMT): biochemistry, molecular biology, pharmacology, and clinical efficacy of the new selective COMT inhibitors[J]. Pharmacological reviews, 1999, 51(4): 593-628.

Chemical Properties

Cas No. 116313-94-1 SDF
别名 硝替卡朋,OR-462
化学名 3-[(3,4-dihydroxy-5-nitrophenyl)methylene]-2,4-pentanedione
Canonical SMILES OC1=C([N+]([O-])=O)C=C(/C=C(C(C)=O)/C(C)=O)C=C1O
分子式 C12H11NO6 分子量 265.2
溶解度 ≥ 60.4 mg/mL in DMSO, ≥ 3.64 mg/mL in EtOH with ultrasonic 储存条件 Store at -20°C
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储备液的保存方式和期限:-80°C 储存时,请在 6 个月内使用,-20°C 储存时,请在 1 个月内使用。
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1 mg 5 mg 10 mg
1 mM 3.7707 mL 18.8537 mL 37.7074 mL
5 mM 0.7541 mL 3.7707 mL 7.5415 mL
10 mM 0.3771 mL 1.8854 mL 3.7707 mL
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