Nitecapone (Synonyms: OR-462) |
| Catalog No.GC14223 |
Nitecapone(OR-462)은 위장 보호 및 항산화 특성을 가진 경구 활성 및 속효성 카테콜-O-메틸트랜스퍼라제(COMT) 억제제입니다.
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Cas No.: 116313-94-1
Sample solution is provided at 25 µL, 10mM.
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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 | |
| Synonyms | OR-462 | ||
| Chemical Name | 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 | ||
| Formula | C12H11NO6 | M.Wt | 265.2 |
| Solubility | ≥ 60.4 mg/mL in DMSO, ≥ 3.64 mg/mL in EtOH with ultrasonic | Storage | Store at -20°C |
| General tips | Please select the appropriate solvent to prepare the stock solution according to the
solubility of the product in different solvents; once the solution is prepared, please store it in
separate packages to avoid product failure caused by repeated freezing and thawing.Storage method
and period of the stock solution: When stored at -80°C, please use it within 6 months; when stored
at -20°C, please use it within 1 month. To increase solubility, heat the tube to 37°C and then oscillate in an ultrasonic bath for some time. |
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| Shipping Condition | Evaluation sample solution: shipped with blue ice. All other sizes available: with RT, or with Blue Ice upon request. | ||
| Prepare stock solution | |||
|
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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Method for preparing in vivo formulation: Take μL DMSO master liquid, next add μL Corn oil, mix and clarify.
Note: 1. Please make sure the liquid is clear before adding the next solvent.
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Quality Control & SDS
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- Purity: >99.00%
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Average Rating: 5 (Based on Reviews and 26 reference(s) in Google Scholar.)
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