CAS: 23110-15-8; (2E,4E,6E,8E)-10-(((3R,4S,5S,6R)-5-Methoxy-4-((2R,3R)-2-Methyl-3-(3-Methylbut-2-En-1-yl)Oxiran-2-yl)-1-Oxaspiro[2.5]Octan-6-yl)Oxy)-10-Oxodeca-2,4,6,8-Tetraenoic Acid

该化合物是一种自然产生的抗生素和抗风素化合物,源自真菌Aspergillus fumigatus,其强效抗血管性能得到显著的承认,通过针对甲型五氯苯乙胺(MetAP-2)2(MetAP-2),抑制内皮细胞扩散.这一机制在研究应用中具有价值,特别是在研究肿瘤生长和微粒子感染方面.Fumagellin表现出低浓度的高生物活动,突出其在受控实验环境中的功效.MetAP-2的稳定性和特性也促进了对治疗潜力的调查,尽管由于毒性问题,其使用仍然主要局限于实验室研究.适当的处理和储存对于保持其完整性至关重要.

结构式图片

欧盟法规

ECHA物质C&L通报REACH预注册

上下游产品

fumagillolfumagillol 26H33O7(1-)*Na(1+)C26H33O7(1-)*Na(1+) ligerin 1-chloromethyl-3-methoxy-2-[2-methyl-3-(3-methylbut-2-enyl)oxiranyl]cyclohexane-1,4-diol

合成工艺路线路线简述

    5-甲氧基-4-[2-甲基-3-(3-甲基丁-2-烯基)环氧乙烷-2-基]-1-氧杂螺[2.5]辛烷-6-醇,(2E,4E,6E,8E)-Deca-2,4,6,8-Tetraenedioyl Dichloride 以75%的收率获得烟曲霉素
    参考文献:(-)-烟曲霉素的合成
    标题:(-)-烟曲霉素的合成
    摘要:血管生成对于实体瘤的生长是必不可少的.1A,B 因此,血管生成抑制剂作为抗肿瘤剂正在积极研究中.最近提出的初步证据表明,血管生成抑制剂也能有效抑制动脉粥样硬化斑块的生长.通过发酵制备的 1C Fumagillin1 (Eq 1) 是这些研究中的主要先导化合物.半合成衍生物如 Tnp-470 2 目前正在临床试验中作为抗肿瘤剂.2,3 烟曲霉素 14 和相关的卵磷脂 35 均已通过全合成制备,并且已经报道了一些初步的结构-活性研究.
    Doi:10.1021/ja990784K

    海关参考信息

    专利信息


    专利号:US-11311505-B2
    优先权日:2017-02-24
    标 题:Synergistic compositions to stimulate the synthesis of human lung and sinus surfactants to decrease coughing, increase FEV-1/FVC ratios, decrease lung fibrosis, by increasing apoptosis of myofibroblasts
    发明人:MARTIN ALAIN
    权利人:MARTIN ALAIN; CELLULAR SCIENCES INC
    摘要:Methods for the treatment of patients with both Chronic Obstructive Pulmonary Disease (COPD) and pulmonary fibrosis, and of patients with idiopathic pulmonary fibrosis without COPD, by stimulating the synthesis of human and animal patient lung and sinus surfactants to increase lung functions, inhibiting fibrosis and reducing coughing and nasal erythema, include the following steps: A) analyzing and diagnosing a patient with a lung ailment selected from the group consisting of i) both COPD and pulmonary fibrosis; and ii) idiopathic pulmonary fibrosis without COPD; and, B) treating the patient to raise the patient's lung functions including FEV1/FVC ratio by contacting mammalian cells with a [therapeutically effective amount of a treatment] composition that includes: a) a pyruvate salt; b) a phosphate; c) a salt of calcium; and d) a salt of magnesium, in an aqueous carrier, containing no more than 2.2 grams of said pyruvate salt per liter.

    专利号:US-10813893-B2
    优先权日:2017-02-24
    标 题:Compositions and methods for the treatment and prevention of chronic hypoxemia and dyspnea
    发明人:MARTIN ALAIN
    权利人:MARTIN ALAIN; CELLULAR SCIENCES INC
    摘要:The present invention has shown that not all salts of pyruvic acid enhance lung functions or enhance the synthesis of lung surfactants and that certain salts of pyruvic acid with the correct concentrations of calcium, phosphate and magnesium, are synergistic in their ability to enhance the synthesis of lung surfactants that will enhance lung alveoli functions, while decreasing coughing and lung tightness, and increasing oxygen saturation values to prevent hypoxemia. This patent demonstrates that the sodium pyruvate formula with calcium, phosphate and magnesium was superior over standard sodium pyruvate formula in saline alone in the removal of mucus, reduction of lung or sinus infections, and in reducing drug side effects and congestion. The use of this formula clearly demonstrated that it can be used to produce better efficacy in patients with hypoxemia, with lung and sinus diseases including, asthma, COPD, cystic fibrosis, interstitial lung disease, allergic rhinitis, sinusitis, Alzheimer's, disease, Parkinson's disease, brain trauma, nicotine addiction, sleep apnea, autism, migraine headaches, sleep disorders, lung and sinus infections, cancer therapy with cancer drugs, nicotine addiction, and medications that cause a decrease in lung surfactants.

    专利号:US-11628186-B2
    优先权日:2017-02-24
    标题 :Method and composition for the reduction of viral replication, duration and spread of the COVID-19 and the flu
    发明人:MARTIN ALAIN
    权利人:MARTIN ALAIN; CELLULAR SCIENCES INC
    摘要:A method for stimulating the synthesis of nasal nitric oxide and nasal and lung surfactants to inhibit the docking and adhesion of viruses to cellular receptors, including ACE2, to reduce viral replication, duration, spread and severity of infections, and also to inhibit lung fibrosis, increase the synthesis of serotonin to reduce coughing and mouth breathing, reduce the cytokine storm produced by LI-6 caused by viruses such as COVID-19 and flu in patients susceptible to these infections, including patients with hypoxemia, asthma, chronic obstructive pulmonary disease, cystic fibrosis, diabetics, interstitial lung disease, pulmonary fibrosis, allergic rhinitis, sinusitis, smokers, sleep apnea and lung cancer, which includes: contacting mammalian cells with a therapeutically effective amount of a composition, said composition including the following constituents: sodium pyruvate; a phosphate; a salt of calcium; and a salt of magnesium.

    专利号:WO-2021040673-A1
    优先权日:2019-08-26
    标 题:Methods for the treatment of chronic hypoxemia and inhibiting lung fibrosis in patients with pulmonary fibrosis with and without copd
    发明人:MARTIN ALAIN
    权利人:MARTIN ALAIN
    摘要:The present invention involves methods for the treatment of chronic hypoxemia, COPD and lung fibrosis in patients with both COPD and pulmonary fibrosis, and in patients with idiopathic pulmonary fibrosis without COPD, by stimulating the synthesis of human and animal patient lung and sinus surfactants to increase lung functions, prevent hypoxemia while reducing the sinus and lung infections, reducing some drug side effects, inhibiting fibrosis and reducing coughing and nasal erythema. These methods include the following steps: A) analyzing and diagnosing a patient with a lung ailment elected from the group consisting of i) both COPD and pulmonary fibrosis; and ii) idiopathic pulmonary fibrosis without COPD; and, B.) treating the patient to raise the patient's lung functions including FEV1/ FVC ratio by contacting mammalian cells with a therapeutically effective amount of a treatment composition that includes a therapeutically effective amount of each constituent of the composition.

    专利号:US-9382288-B2
    优先权日:2010-10-06
    标题 :Derivatives of steroid benzylamines, having an antiparasitic antibacterial, antimycotic and/or antiviral action
    发明人:BECKER KATJA; KRIEG REIMAR; SCHÖNECKER BRUNO
    权利人:BECKER KATJA; KRIEG REIMAR; SCHÖNECKER BRUNO; UNIV GIESSEN JUSTUS LIEBIG
    摘要:The present invention relates to compounds derived from steroids of the general formula (I) n nwherein L represents a linker and R # represents a steroid residue, the use of compounds of the general formula (I) in medicine and for the prophylaxis and/or the treatment of infectious diseases. Furthermore described are pharmaceutical compositions containing at least one compound of the general formula (I). A further aspect of the invention relates to the synthesis of said compounds of the general formula (I).

    专利号:US-10772971-B2
    优先权日:2017-06-22
    标 题:Methods of producing drug-carrying polymer scaffolds and protein-polymer-drug conjugates
    发明人:GURIJALA VENU REDDY; BOLLU SATYANARAYAN REDDY; LEBLANC JACQUES; LOWINGER TIMOTHY B; MCGILLICUDDY DENNIS; YIN MAO; YURKOVETSKIY ALEKSANDR V
    权利人:MERSANA THERAPEUTICS INC; MERSANA THERPEUTICS INC
    摘要:The disclosure provides methods of synthesis of polymeric scaffolds, e.g., those useful for conjugating with a protein based recognition-molecule (PBRM) to form PBRM-polymer-drug conjugates, and PBRM-polymer-drug conjugates thereof. The methods according to the disclosure allow for large-scale preparation of polymeric scaffolds having a high purity. In some embodiments, the methods according to the disclosure also allow for the preparation of scaffolds and conjugates thereof in better yield than previously used methods for preparing same. Also disclosed are methods of purifying polymeric scaffolds.
    台州市科瑞生物技术有限公司
    ⚠️ 未注册 · 未认证企业
    ⚠️ 该商家尚未完成注册及企业认证,请用户仔细辨别,谨慎交易。
    数据来源于公开网络搜索,平台未作核实,请自行辨别。
    🏢敬请 企业认领
    🏬开设公司展台
    📢获取免费会员权益
    🎖️点亮专属注册企业标签
    📇展现公司完整信息 样本查看立即注册认领 →
    网址: http://www.pharm-intermediates.com
    企业联系电话:0576-88813233👤
    📞台州市科瑞生物技术有限公司 ⚠️参考联系方式
    联系人:金崇光
    电话:0576-88813233
    手机:13396860566
    传真:0576-88813233
    邮箱:sales@pharm-intermediates.com
    通信地址: 台州市开发大道东段288号
    邮编: 318000
    🆔 联系时候可告知是从"百琢研"平台获取的信息.
    ⚠️ 声明: 该企业未认证、未认领,请自行辨别信息的真实性和可靠性。咨询或交易时请注意风险评估与信息核实,百琢研不参与任何交易。企业认领注册入口→

    地址:台州市开发大道东段288号
    ⚠️ 未注册 · 未认证企业
    注册入口 备注: 📌 数据来源说明:本展台内容基于各搜索引擎等公开数据整理,仅作展示用途。请用户自行辨别
    ✉️ 若企业需抹除展台内容或有异议, 请通过页面底部联系方式告知我们,我们会尽快处理。
    上海泽吉生物科技有限公司
    ⚠️ 未注册 · 未认证企业
    ⚠️ 该商家尚未完成注册及企业认证,请用户仔细辨别,谨慎交易。
    数据来源于公开网络搜索,平台未作核实,请自行辨别。
    🏢敬请 企业认领
    🏬开设公司展台
    📢获取免费会员权益
    🎖️点亮专属注册企业标签
    📇展现公司完整信息 样本查看立即注册认领 →
    网址: http://www.3klh.com
    电话: 0086 (21) 5448-0173👤
    📞上海泽吉生物科技有限公司 ⚠️参考联系方式

    销售电话:0086 (21) 5448-0173
    邮箱:klh@vip.163.com
    🆔 联系时候可告知是从"百琢研"平台获取的信息.
    ⚠️ 声明: 该企业未认证、未认领,请自行辨别信息的真实性和可靠性。咨询或交易时请注意风险评估与信息核实,百琢研不参与任何交易。企业认领注册入口→

    ⚠️ 未注册 · 未认证企业
    注册入口 备注: 📌 数据来源说明:本展台内容基于各搜索引擎等公开数据整理,仅作展示用途。请用户自行辨别 ✉️ 若企业需抹除展台内容或有异议, 请通过页面底部联系方式告知我们,我们会尽快处理。
    第 1 / 1 页
    现货

    供应商参考报价(招募中)

    品牌试剂参考报价(招募中)

    📌 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: Kanno T, Uehara T, Osawa M, Fukumoto H, Mine S, Ueda K, Hasegawa H, Katano H. Fumagillin, a potent angiogenesis inhibitor, induces Kaposi sarcoma-associated herpesvirus replication in primary effusion lymphoma cells. Biochem Biophys Res Commun. 2015 Aug 7;463(4):1267-72. doi: 10.1016/j.bbrc.2015.06.100. Epub 2015 Jun 18. doi: 10.1016/j.foodchem.2015.01.111. Epub 2015 Jan 31. doi: 10.7150/thno.10014. eCollection 2015.
    4: Zhou HF, Yan H, Hu Y, Springer LE, Yang X, Wickline SA, Pan D, Lanza GM, Pham CT. Fumagillin prodrug nanotherapy suppresses macrophage inflammatory response via endothelial nitric oxide. ACS Nano. 2014 Jul 22;8(7):7305-17. doi: 10.1021/nn502372n. Epub 2014 Jun 24.
    5: Blanchet E, Vansteelandt M, Le Bot R, Egorov M, Guitton Y, Pouchus YF, Grovel O. Synthesis and antiproliferative activity of ligerin and new fumagillin analogs against osteosarcoma. Eur J Med Chem. 2014 May 22;79:244-50. doi: 10.1016/j.ejmech.2014.04.012. Epub 2014 Apr 5. doi: 10.1021/jf4055374. Epub 2014 Mar 21. Review. doi: 10.1021/ja500881e. Epub 2014 Mar 11.

    合成参考文献


    摘要:Antibiotics and Chemotherapy, 1(54), 1951
    摘要:A3058: Stanimirovic Z, Stevanovic J, Bajic V, Radovic I: Evaluation of genotoxic effects of fumagillin by cytogenetic tests in vivo. Mutat Res. 2007 Mar 30;628(1):1-10. Epub 2007 Jan 14.
    摘要:Peterson, M.H., Goldstein, A.W. and Denison, F.W. Jr.; U.S. Patent 2,803,586; August 20, 1957; assigned to Abbott Laboratories.
    参考文献:10.1023/a:1007541713398
    摘要:Black AF, Hudon V, Damour O, Germain L, Auger FA. A novel approach for studying angiogenesis: a human skin equivalent with a capillary-like network. Cell Biol Toxicol. 1999 Apr;15(2):81–90. doi: 10.1023/a:1007541713398.
    参考文献:10.1023/a:1006591805332
    摘要:Yatsunami J, Tsuruta N, Fukuno Y, Kawashima M, Taniguchi S, Hayashi S. Inhibitory effects of roxithromycin on tumor angiogenesis, growth and metastasis of mouse B16 melanoma cells. Clin Exp Metastasis. 1999 Mar;17(2):119–24. doi: 10.1023/a:1006591805332.
    📝 需求与反馈
    尽可能描述清楚需求与问题信息
    ×

    通知