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Entacapone

    
99%

Entacapone

源葉(MedMol)
S82780 一鍵復(fù)制產(chǎn)品信息
130929-57-6
C14H15N3O5
305.29
恩他卡朋;(E)-2-氰基-3-(3,4二羥基-5-硝基苯)-N,N二乙基丙烯酰胺
貨號(hào) 規(guī)格 價(jià)格 上海 北京 武漢 南京 購(gòu)買(mǎi)數(shù)量
S82780-5mg 99% ¥208.00 1 - - -
S82780-10mg 99% ¥360.00 6 - - -
S82780-25mg 99% ¥680.00 1 - - -
S82780-50mg 99% ¥1120.00 7 - - -
S82780-100mg 99% ¥1680.00 3 - - -
產(chǎn)品介紹 參考文獻(xiàn)(3篇) 質(zhì)檢證書(shū)(COA) 摩爾濃度計(jì)算器 相關(guān)產(chǎn)品

產(chǎn)品介紹

Entacapone (OR-611) 抑制兒茶酚-O-甲基轉(zhuǎn)移酶(COMT)活性,IC50為151 nM。Entacapone 是一種 FTO demethylation 的抑制劑,IC50為3.5 μM,可用于代謝紊亂的研究

產(chǎn)品描述: Entacapone (OR-611) 抑制兒茶酚-O-甲基轉(zhuǎn)移酶(COMT)活性,IC50為151 nM。Entacapone 是一種 FTO demethylation 的抑制劑,IC50為3.5 μM,可用于代謝紊亂的研究
靶點(diǎn): COMT:151 nM;Transferase
體外研究: Entacapone在不同組織中抑制catechol-O-methyltransferase(COMT)的IC50值大體相似,包括肝臟,十二指腸, 腎臟和肺, 但是entacapone在這些組織中抑制效果比tolcapone更好。 Entacapone (< 100 μM)可以有效抑制α-syn和β-amyloid (Aβ) 齊聚反應(yīng)和原纖維生成同時(shí)可以保護(hù)PC12細(xì)胞免受這兩種蛋白聚集誘導(dǎo)的細(xì)胞外毒性
體內(nèi)研究: Entacapone administration reduced body weight and lowered fasting blood glucose concentrations in diet-induced obese mice.
細(xì)胞實(shí)驗(yàn): Cell lines: PC12 cells Concentrations: 5 μM Incubation Time: 72 h Method: Cells were treated with various concentrations of drug for 72 h.
動(dòng)物實(shí)驗(yàn): Animal Models: Male C57BL/6 mice Dosages: 600 mg/kg Administration: p.o.
參考文獻(xiàn): 1. De Santi C, et al. Catechol-O-methyltransferase: variation in enzyme activity and inhibition by entacapone and tolcapone. Eur J Clin Pharmacol, 1998, 54(3), 215-219. 2. Di Giovanni S, et al. Entacapone and tolcapone, two catechol O-methyltransferase inhibitors, block fibril formation of alpha-synuclein and beta-amyloid and protect against amyloid-induced toxicity. J Biol Chem, 2010, 285(20), 14941-14954. 3. Jenner P, et al. Avoidance of dyskinesia: preclinical evidence for continuous dopaminergic stimulation. Neurology, 2004, 62(1 Suppl 1), S47-55. 4. Hamaue N, et al. Entacapone, a catechol-O-methyltransferase inhibitor, improves the motor activity and dopamine content of basal ganglia in a rat model of Parkinson's disease induced by Japanese encephalitis virus. Brain Res, 2010, 1309, 110-115. 5. Peng S, et al. Identification of entacapone as a chemical inhibitor of FTO mediating metabolic regulation through FOXO1. Sci Transl Med. 2019 Apr 17;11(488):eaa
溶解性: Soluble  in  DMSO、Ethanol
保存條件: 2-8℃
配置溶液濃度參考:
1mg 5mg 10mg
1 mM 3.276 ml 16.378 ml 32.756 ml
5 mM 0.655 ml 3.276 ml 6.551 ml
10 mM 0.328 ml 1.638 ml 3.276 ml
50 mM 0.066 ml 0.328 ml 0.655 ml
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質(zhì)檢證書(shū)(COA)

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摩爾濃度計(jì)算器

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