937812-80-1

• 常用中文名：奥米沙班
• 常用英文名：gamma-Secretase Modulators
• CAS号：937812-80-1
• 分子式：C₂₆H₂₄F₃N₃O₃
• 分子量：483.48200
• 相关类别： 信号通路 神经信号通路 β淀粉样蛋白
• 发布时间：2018-06-20 19:09:29
• 更新时间：2026-06-30 21:13:04
• gamma-Secretase Modulators (Amyloid-β production inhibitor)是淀粉状蛋白β生成抑制剂,可作用于阿尔茨海默病。

名称

• 中文名: 奥米沙班
• 英文名: (4R,7E,9aS)-7-[[3-methoxy-4-(4-methylimidazol-1-yl)phenyl]methylidene]-4-(3,4,5-trifluorophenyl)-1,3,4,8,9,9a-hexahydropyrido[2,1-c][1,4]oxazin-6-one
• 中文别名: FXA可逆型抑制剂(OTAMIXABAN); (E)-(4R,9AS)-7-[3-甲氧基-4-(4-甲基-1H-咪唑-1-基)苯亚甲基]-4-(3,4,5-三氟苯基六氢吡啶并[2,1-C][1,4]嗪-6-酮; 六氢-7-[[3-甲氧基-4-(4-甲基-1H-咪唑-1-基)苯基]亚甲基]-4-(3,4,5-三氟苯基)-(4r,7e,9as)-吡啶并[2,1-c][1,4]噁嗪-6(1h)-酮; (E)-(4R,9AS)-7-[3-甲氧基-4-(4-甲基-1H-咪唑-1-基)苯亚甲基]-4-(3,4,5-三氟苯基六氢吡啶并[2,1-C][1,4]噁嗪-6-酮
• 英文别名: gaMMa-Secretase Modulators; (E)-(4R,9aS)-7-[3-Methoxy-4-(4-methyl-1H-imidazol-1-yl)benzylidene]-4-(3,4,5-trifluorophenyl)hexahydropyrido[2,1-c][1,4]oxazin-6-one; SynonyMs: HYR-141; hexahydro-7-[[3-methoxy-4-(4-methyl-1H-imidazol-1-yl)phenyl]methylene]-4-(3,4,5-trifluorophenyl)-(4R,7E,9aS)-Pyrido[2,1-c][1,4]oxazin-6(1H)-one; gammaSecretase Modulators,gamma Secretase Modulators; Pyrido[2,1-c][1,4]oxazin-6(1H)-one, hexahydro-7-[[3-Methoxy-4-(4-Methyl-1H-iMidazol-1-yl)phenyl]Methylene]-4-(3,4,5-trifluorophenyl)-, (4R,7E,9aS); γ-Secretase Modulators; Otamixaban; Amyloid-β production inhibitor; (E)-(4R)-2-benzenesulfonyl-4,6-dimethyl-non-6-en-3-one; HYR-141; (E)-(4R,9AS)-7-[3-methoxy-4-(4-methyl-1H-imidazol-1-yl)benzylidene]-4-(3,4,5-trifluorophenyl)h; 6-Nonen-3-one,4,6-dimethyl-2-(phenylsulfonyl)-,(4R,6E); (E)-(4R,9aS)-7-[3-methoxy-4-(4-methyl-1H-imidazol-1-yl)benzylidene]-4-(3,4,5-trifluorophenyl)hexahydropyrido[2,1-c][1,4]oxazin-6-one

物化性质

• 密度: 1.37g/cm3
• 分子式: C₂₆H₂₄F₃N₃O₃
• 分子量: 483.48200
• 精确质量: 483.17700
• PSA: 56.59000
• LogP: 4.69040
• 储存条件: 2-8℃

生物活性

• 描述: gamma-Secretase Modulators (Amyloid-β production inhibitor)是淀粉状蛋白β生成抑制剂,可作用于阿尔茨海默病。
• 相关类别:
  信号通路 >> 神经信号通路 >> β淀粉样蛋白
  研究领域 >> 神经疾病
• 参考文献:

  [1]. Watahiki H, Yagishita S, Futai E, Ishiura S.CTF1-51, a truncated carboxyl-terminal fragment of amyloid precursor protein, suppresses the effects of Aβ42-lowering γ-secretase modulators.Neurosci Lett. 2012 Sep 27;526(2):96-9. Epub 2012 Aug 23.

  [2]. Wanngren J, Ottervald J, Parpal S, Portelius E, Str?mberg K, Borgeg?rd T, Klintenberg R, Juréus A, Blomqvist J, Blennow K, Zetterberg H, Lundkvist J, Rosqvist S, Karlstr?m H.Second generation γ-secretase modulators exhibit different modulation of Notch β

  [3]. Wagner SL, Tanzi RE, Mobley WC, Galasko D.Potential Use of γ-Secretase Modulators in the Treatment of Alzheimer Disease.Arch Neurol. 2012 Jul 16:1-4.

  [4]. Bulic B, Ness J, Hahn S, Rennhack A, Jumpertz T, Weggen S.Chemical Biology, Molecular Mechanism and Clinical Perspective of γ-Secretase Modulators in Alzheimer's Disease.Curr Neuropharmacol. 2011 Dec;9(4):598-622.

  [5]. Kretner, Benedikt; Fukumori, Akio; Gutsmiedl, Amelie; Page, Richard M.; Luebbers, Thomas; Galley, Guido; Baumann, Karlheinz; Haass, Christian; Steiner, Harald. Attenuated A.beta.42 Responses to Low Potency .gamma.-Secretase Modulators Can Be Overcome for

合成路线

870837-18-6 937816-18-7 ~% 937812-80-1

文献：Eisai RandD Management Co., Ltd. Patent: US2009/48213 A1, 2009 ; Location in patent: Page/Page column 61 ;

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