CAS: 508-75-8; (3S,5S,8R,9S,10S,13R,14S,17R)-5,14-Dihydroxy-13-Methyl-17-(5-Oxo-2,5-Dihydrofuran-3-yl)-3-(((2R,3R,4R,5R,6S)-3,4,5-Trihydroxy-6-Methyltetrahydro-2H-Pyran-2-yl)Oxy)Hexadecahydro-10H-Cyclopenta[a]Phenanthrene-10-Carbaldehyde

该化合物是一种有毒的心心球,产自被称为谷里百合的植物Convalaria majalis,通常称为谷里百合,其特点是能够抑制Na+/K+ATPase酶,该酶在维持细胞膜间隔膜间电化学梯度方面起着关键作用.这种抑制导致细胞内钠浓度增加,随后导致细胞内钙浓度增加,从而可以增加心肌萎缩性.氯甲老二氏表现出一种典型的心脏螺旋侧结构,以糖性类固醇核为主.其药理效应可导致毒性症状,包括恶心,呕吐和潜在威胁生命的心律不齐.由于其强大的生物活动,已经研究过其潜在的治疗用途,尽管其治疗窗口狭窄,必须谨慎.处理这一化合物需要适当的安全措施,因为其毒性性质,并且被归类为危险物质.

结构式图片

欧盟法规

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CAS号5158-64-5 2,3,4-三-O-乙酰基-6... | CAS号66-28-4 毒毛旋花子苷元 | CAS号69980-52-5 2,3,4-tri-O-ace...

合成工艺路线路线简述

    📜Alkaline Earth Salt Of/the/ Methylsulfuric Acid置于enzyme-Substance From Strophanthus Kombe体系中,化学反应生成 铃兰毒甙
    参考文献:Schmutz; Reichstein,Pharmaceutica Acta Helvetiae,1947,Vol. 22,P. 359,364,369
    标题:Schmutz; Reichstein,Pharmaceutica Acta Helvetiae,1947,Vol. 22,P. 359,364,369

    海关参考信息

    专利信息


    专利号:US-10925977-B2
    优先权日:2006-10-05
    标 题 :Efficient synthesis of chelators for nuclear imaging and radiotherapy: compositions and applications
    发明人:YANG DAVID J; YU DONGFANG; THOMPSON ANDREW S
    权利人:YANG DAVID J; YU DONGFANG; THOMPSON ANDREW S; CEIL POINT LLC; UNIV TEXAS
    摘要:Novel methods of synthesis of chelator-targeting ligand conjugates, compositions comprising such conjugates, and therapeutic and diagnostic applications of such conjugates are disclosed. The compositions include chelator-targeting ligand conjugates optionally chelated to one or more metal ions. Methods of synthesizing these compositions in high purity are also presented. Also disclosed are methods of imaging, treating and diagnosing disease in a subject using these novel compositions, such as methods of imaging a tumor within a subject and methods of diagnosing myocardial ischemia.

    专利号:WO-0112817-A1
    优先权日:1999-08-12
    标题:Evolution and use of enzymes for combinathorial and medicinal chemistry
    发明人:KREBBER CLAUS; DAVIS S CHRISTOPHER; DELCARDAYRE STEPHEN; SELIFONOV SERGEY A; HOWARD RUSSELL
    权利人:MAXYGEN INC; LIU LU; KREBBER CLAUS; DAVIS S CHRISTOPHER; DELCARDAYRE STEPHEN; SELIFONOV SERGEY A; HOWARD RUSSELL
    摘要:This invention provides libraries of recombinant derivatizing enzymes that are useful for biocatalytic synthesis of derivatives oforganic molecules, including lead compounds for pharmaceutical use. The recombinant derivatizing enzymes catalyze reactions such as modification or replacement of functional groups on the organicmolecules, or addition of chemical moieties onto preexisting functional groups. The use of recombinant enzyme libraries enables one to obtain enzymes that catalyze the formation of organic molecule derivatives that could not otherwise be made using only naturally occurring enzymes.

    专利号:US-10814013-B2
    优先权日:2006-10-05
    标 题 :Efficient synthesis of chelators for nuclear imaging and radiotherapy: compositions and applications

    专利号:AU-2007308022-A2
    优先权日:2006-10-05
    标题 :Efficient synthesis of chelators for nuclear imaging and radiotherapy: compositions and applications

    专利号:AU-2007308022-A1
    优先权日:2006-10-05
    标 题 :Efficient synthesis of chelators for nuclear imaging and radiotherapy: compositions and applications

    专利号:US-2008107598-A1
    优先权日:2006-10-05
    标 题:Efficient Synthesis of Chelators for Nuclear Imaging and Radiotherapy: Compositions and Applications

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    📌 第三方产品分析报告

    ✅ COA系统入驻 | 共享模式

    主要参考文献


    1: Fink SL, Robey TE, Tarabar AF, Hodsdon ME. Rapid detection of convallatoxin using five digoxin immunoassays. Clin Toxicol (Phila). 2014 Aug;52(7):659-63. doi: 10.3109/15563650.2014.932366. Epub 2014 Jul 1.
    2: Gozalpour E, Greupink R, Bilos A, Verweij V, van den Heuvel JJ, Masereeuw R, Russel FG, Koenderink JB. Convallatoxin: a new P-glycoprotein substrate. Eur J Pharmacol. 2014 Dec 5;744:18-27. doi: 10.1016/j.ejphar.2014.09.031. Epub 2014 Sep 28. doi: 10.1309/AJCPCOXF0O5XXTKD. doi: 10.1371/journal.pone.0091094. eCollection 2014.
    5: Everett JM, Kojima YA, Davis B, Wahed A, Dasgupta A. The iDigoxin Assay is More Sensitive than LOCI Digoxin Assay for Rapid Detection of Convallatoxin, the Active Cardiac Glycoside of Lily of The Valley. Ann Clin Lab Sci. 2015 Spring;45(3):323-6. Print 2016 Dec 1.

    合成参考文献


    摘要:Farmakologiya i Toksikologiya, 44(342), 1981 []
    摘要:Arzneimittel-Forschung. Drug Research., 11(848), 1961 []
    摘要:Full text:
    摘要:Belova LF; Mater Vses Konf Issled Lek Rast Perspekt Ikh Ispol'z Proizvod Lek Prep: 12 (1972)
    摘要:Full text: https://www.ncbi.nlm.nih.gov/pmc/articles/PMC4180104
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