Nitecapone
(Synonyms: 硝替卡朋,OR-462) 目录号 : GC14223A selective S-COMT inhibitor
Cas No.:116313-94-1
Sample solution is provided at 25 µL, 10mM.
Quality Control & SDS
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- Purity: >99.00%
- COA (Certificate Of Analysis)
- SDS (Safety Data Sheet)
- Datasheet
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.
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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Shipping Condition | 评估样品解决方案:配备蓝冰进行发货。所有其他可用尺寸:配备RT,或根据请求配备蓝冰。 |
制备储备液 | |||
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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2.
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