CAS: 140898-91-5; Hexaminolevulinate Hydrochloride

该化合物是一种化学化合物,具有氨基氨基化合物和酯功能组的特点,表明其作为生物活性分子的潜力;该化合物的特征是五甲酸基质,它具有脂肪酸特性,而氨基和基托组则表明它可能参与各种生物化学相互作用;六氧基酯部分会增加其亲脂性,有可能影响其溶解性和生物系统中的渗透性;作为盐酸盐,它可能比其自由基质形式更容易溶解,而自由基本形式可能有利于药物应用;盐酸的存在表明它可能会用于稳定性和溶解性至关重要的配方;总体而言,该化合物可能表现出有趣的药理特性,成为医学化学和药物开发领域进一步研究的候选物.

结构式图片

欧盟法规

ECHA物质C&L通报

合成工艺路线路线简述

    5-氨基乙酰丙酸盐酸盐,正己醇置于氯化亚砜体系中,化学反应生成5-氨基酮戊酸己酯盐酸盐
    参考文献:新的5-氨基乙酰丙酸衍生物作为原卟啉的前药在光动力疗法中的合成与评价
    标题:新的5-氨基乙酰丙酸衍生物作为原卟啉的前药在光动力疗法中的合成与评价
    摘要:原卟啉ix(ppix)在癌症的光动力诊断(pdd)和光动力疗法(pdt)中用作光敏剂,由5-氨基乙酰丙酸(5-Ala)前体在细胞内合成.设计并合成了13种新颖的5-Ala衍生物,具有定制的亲水性和亲脂性.检测的ppix的生成和它们的抗肿瘤活性在体外和体内也进行了研究.结果表明,化合物9B-c,11B-c和13A在小鼠纤维肉瘤s180细胞中孵育5小时后,在593 Nm处显示出特征性的长波吸收峰.在暴露于600 Nm激光照射后,这些化合物可在体外抑制s180细胞中的细胞增殖.这些化合物在体内可明显抑制s180细胞肿瘤在昆明小鼠中的生长.在这些化合物中,13A具有低的暗毒性和高的光毒性,这使其成为pdt的有效和有前途的前药.
    Doi:10.1039/c7Pp00203C

    海关参考信息

    专利信息


    专利号:US-2009062211-A1
    优先权日:2003-03-05
    标 题:Conopeptides and methods of use
    发明人:MARI FRANK; FIELDS GREGG B
    权利人:UNIV FLORIDA ATLANTIC
    摘要:Isolation, synthesis and therapeutic use of conotoxin and conophan compounds and related compositions including a new class of conopeptides including the modified amino acid D-γ-hydro-oxyvalinie (D-Hyv=V*) are described herein. These isolated peptides are the first known example of a naturally occurring polypeptide chain containing D-Hyv. The active peptides, termed γ-Hydroxyconophans are heavily hydroxylated small peptides. These peptides contain a definitive structural motif which is a double modification of the polypeptide chain (γ-D-OH-Hyv-Trp).

    专利号:US-2006019892-A1
    优先权日:2003-03-05
    标 题:Conopeptides and methods of use
    发明人:MARI FRANK
    权利人:UNIV FLORIDA ATLANTIC
    摘要:Isolation, synthesis and therapeutic use of compounds and related compositions based on a new class of conopeptides comprising the modified amino acid γ-hydroxyvaline (Hyv=V*). These isolated peptides are the first known example of a naturally occurring polypeptide chain containing Hyv. The active peptides, termed γ-Hydroxyconophans are heavily hydroxylated small peptides. These peptides contain a definitive structural motif which is a double modification of the polypeptide chain (γ-OH-Hyv-D-Trp).

    专利号:US-12144874-B2
    优先权日:2015-09-09
    标题 :Synthesis and composition of photodynamic therapeutic agents for the targeted treatment of cancer
    发明人:KULARATNE SUMITH A; GAGARE PRAVIN
    权利人:ON TARGET LABORATORIES LLC; ON TARGET LABORATORIES INC
    摘要:The present invention describes new compounds that are useful for image-guided surgery and photodynamic therapy. In particular the compounds may be targeted to the nucleus or the mitochondria after compounds were delivered to diseased tissues such as cancer using a ligand that target receptor that express on the diseased tissue and followed by receptor mediated endocytosis and provide effective activity against cancer cells as well as other disorders. Methods and compositions for use of the same are described.

    专利号:US-10676487-B2
    优先权日:2015-09-09
    标 题 :Synthesis and composition of photodynamic therapeutic agents for the targeted treatment of cancer
    发明人:KULARATNE SUMITH A; GAGARE PRAVIN; MYERS CARRIE H
    权利人:ON TARGET LABORATORIES LLC
    摘要:The present invention describes new compounds that are useful for image-guided surgery and photodynamic therapy. In particular the compounds may be targeted to the nucleus or the mitochondria after compounds were delivered to diseased tissues such as cancer using a ligand that target receptor that express on the diseased tissue and followed by receptor mediated endocytosis and provide effective activity against cancer cells as well as other disorders. Methods and compositions for use of the same are described.

    专利号:WO-2025121735-A1
    优先权日:2023-12-05
    标 题 :Pharmaceutical composition comprising upconversion nanoparticles for preventing or treating cancer
    发明人:KIM KI SU; CHOI HYE EUN; ANARA MOLKENOVA; LEE SU BIN
    权利人:NAT UNIV PUSAN IND UNIV COOP FOUND
    摘要:The present invention relates to a nano-platform comprising core-shell structured upconversion nanoparticles, a composition comprising same, and a treatment method, the nano-platform comprising: a core formed of NaYF4:Yb, Tm through single-step synthesis; and a shell, which encompasses the core and is formed of NaYF4:Nd.

    专利号:EP-3347010-A1
    优先权日:2015-09-09
    标题:Synthesis and composition of photodynamic therapeutic agents for the targeted treatment of cancer
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    主要参考文献


    1: Togsverd-Bo K, Lerche CM, Philipsen PA, Hædersdal M, Wulf HC. Artificial daylight photodynamic therapy with "non-inflammatory" doses of hexyl aminolevulinate only marginally delays SCC development in UV-exposed hairless mice. Photochem Photobiol Sci. 2013 Sep 24. [Epub ahead of print] doi: 10.1016/j.eururo.2013.07.007. Epub 2013 Jul 19. doi: 10.1111/j.1600-0625.2012.01442.x. Epub 2012 Feb 10. doi: 10.1039/c0pp00369g. Epub 2011 Mar 30. doi: 10.1586/era.09.73. Review. doi: 10.1016/j.pdpdt.2008.07.001. Epub 2008 Aug 28. doi: 10.1039/b804921a. Epub 2008 Jul 23. Review.

    合成参考文献


    参考文献:10.1007/s11307-017-1050-5
    摘要:Tipirneni KE, Rosenthal EL, Moore LS, Haskins AD, Udayakumar N, Jani AH, Carroll WR, Morlandt AB, Bogyo M, Rao J, Warram JM. Fluorescence Imaging for Cancer Screening and Surveillance. Molecular Imaging and Biology. 2017 Feb 02;19(5):645–55. doi: 10.1007/s11307-017-1050-5.
    参考文献:10.1007/s13671-016-0154-5
    摘要:Thunshelle C, Yin R, Chen Q, Hamblin MR. Current Advances in 5-Aminolevulinic Acid Mediated Photodynamic Therapy. Current Dermatology Reports. 2016 Jul 13;5(3):179–90. doi: 10.1007/s13671-016-0154-5.
    参考文献:10.1023/a:1015784926550
    摘要:Hirschberg H, Sun CH, Tromberg BJ, Madsen SJ. ALA- and ALA-ester-mediated photodynamic therapy of human glioma spheroids. J Neurooncol. 2002 Mar;57(1):1–7. doi: 10.1023/a:1015784926550.
    参考文献:10.1007/s00120-008-1778-2
    摘要:Jichlinski P, Lovisa B, Erling C, Aymon D, van den Berg H, Wagnieres G. [Fluorescence cystoscopy. Perspective in clinical practice and research]. Urologe A. 2008 Aug;47(8):975–7. doi: 10.1007/s00120-008-1778-2.
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