CAS: 56974-61-9; Ethyl 4-((6-Guanidinohexanoyl)Oxy)Benzoate Methanesulfonate

该化合物是合成蛋白酶抑制剂,具有抗凝胶和抗炎特性.它通过选择性抑制血清蛋白质,如强血素,试金素和颗粒素发挥作用,有助于急性胰腺炎等疾病的管理和传播血管内部凝聚(DIC),该化合物毒性低,而且快速清除,尽量减少系统性副作用.它的水溶性允许静脉注射管理,确保高效的生物利用率.加贝氏体中聚醚还被用于研究蛋白质中间途径.该化合物的特性和有利的药用动能特征使它在临床和实验应用中成为有价值的工具.

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CAS号120-47-8 尼泊金乙酯 | CAS号6659-35-4 6-胍基己酸 | CAS号120-47-8 尼泊金乙酯 | CAS号80693-42-1 6-(hydrazinylme...

合成工艺路线路线简述

    甲烷磺酸,Gabexate Carbonate 以 丙酮 作为反应溶剂,以77.8 %的收率获得产物甲磺酸加贝酯
    参考文献:Cn115141124
    标题:Cn115141124

    海关参考信息

    专利信息


    专利号:US-11977084-B2
    优先权日:2015-02-11
    标题 :Nervous system-specific transmembrane proteasome complex that modulates neuronal signaling through extracellular signaling via brain activity peptides
    发明人:MARGOLIS SETH S; RAMACHANDRAN KAPIL V
    权利人:UNIV JOHNS HOPKINS
    摘要:The inventors surprisingly found that neural stimulation caused the synthesis and degradation of proteins into peptides which were then secreted into the cell media within minutes of stimulation by a novel neural-specific and membrane bound proteasome (neuronal membrane proteasome or NMP) that is transmembrane in nature. These secreted, activity-induced, proteasomal peptides (SNAPPs) range in size from about 500 Daltons to about 3000 Daltons. Surprisingly none of the peptides appear to be those previously known to have any neuronal function. Moreover, these SNAPPs have stimulatory activity and are heretofore a new class of signaling molecules. Moreover, the NMP appears to play a highly significant role in aspects of neuronal signaling known to be critical for neuronal function. The inventors have gone on to develop all tools to study this novel mechanisms including protocols and practice for generation and purification of SNAPPs as well as a new and specific inhibitor of the NMP allowing for selective control of this process in the nervous system. The present invention provides methods of making and using these SNAPPs for both laboratory and clinical purposes, the screening for molecules which modulate NMP function in vivo and in vitro, and methods for diagnosis of NMP related diseases.

    专利号:WO-2018160662-A1
    优先权日:2017-02-28
    标题 :A novel nervous system-specific transmembrane proteasome complex that modulates neuronal signaling through extracellular signaling via brain activity peptides
    发明人:MARGOLIS SETH; RAMACHANDRAN KAPIL V
    权利人:UNIV JOHNS HOPKINS
    摘要:The inventors surprisingly found that neural stimulation caused the synthesis and degradation of proteins into peptides which were then secreted into the cell media within minutes of stimulation by a novel neural membrane bound proteasome (NMP). These secreted, activity-induced, proteasomal peptides (SNAPPs) range in size from about 500 Daltons to about 3000 Daltons. Surprisingly none of the peptides appear to be those previously known to have any neuronal function. Moreover, these SNAPPs have stimulatory activity and are heretofore a new class of signaling molecules. The present invention provides methods of modulating NMP function, including in cases of NMP associated disease or disorder of neuronal cells, by stimulating or inhibiting NMP function. The present invention also provides methods for stimulation or enhancing cognitive function using SNAPPs, and methods for treating of NMP related diseases using SNAPPs.

    专利号:US-2020071367-A1
    优先权日:2017-02-28
    标 题 :A novel nervous system-specific transmembrane proteasome complex that modulates neuronal signaling through extracellular signaling via brain activity peptides
    发明人:MARGOLIS SETH; RAMACHANDRAN KAPIL V
    权利人:UNIV JOHNS HOPKINS
    摘要:The inventors surprisingly found that neural stimulation caused the synthesis and degradation of proteins into peptides which were then secreted into the cell media within minutes of stimulation by a novel neural membrane bound proteasome (NMP). These secreted, activity-induced, proteasomal peptides (SNAPPs) range in size from about 500 Daltons to about 3000 Daltons. Surprisingly none of the peptides appear to be those previously known to have any neuronal function. Moreover, these SNAPPs have stimulatory activity and are heretofore a new class of signaling molecules. The present invention provides methods of modulating NMP function, including in cases of NMP associated disease or disorder of neuronal cells, by stimulating or inhibiting NMP function. The present invention also provides methods for stimulation or enhancing cognitive function using SNAPPs, and methods for treating of NMP related diseases using SNAPPs.
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    主要参考文献


    1: Gao HJ, Song Q, Lv FQ, Wang S, Wang YR, Luo YK, Mei XG, Tang J. A novel thermosensitive in-situ gel of gabexate mesilate for treatment of traumatic pancreatitis: An experimental study. J Huazhong Univ Sci Technolog Med Sci. 2015 Oct;35(5):707-11. doi: 10.1007/s11596-015-1494-2. Epub 2015 Oct 22. doi: 10.1007/s00068-014-0478-4. Epub 2014 Nov 20. doi: 10.1097/MBC.0000000000000214. doi: 10.1002/bmc.3373. Epub 2014 Oct 30. doi: 10.1016/j.jiac.2014.04.010. Epub 2014 May 21. doi: 10.1016/j.transproceed.2013.10.037. doi: 10.1007/s00431-013-2068-6. Epub 2013 Jun 29. doi: 10.3109/0886022X.2013.780620. Epub 2013 Apr 8. doi: 10.1097/MPA.0b013e31826495a0. doi: 10.1371/journal.pone.0041347. Epub 2012 Jul 24.
    13: Noguchi H, Naziruddin B, Jackson A, Shimoda M, Fujita Y, Chujo D, Takita M, Peng H, Sugimoto K, Itoh T, Kobayashi N, Ueda M, Okitsu T, Iwanaga Y, Nagata H, Liu X, Kamiya H, Onaca N, Levy MF, Matsumoto S. Comparison of ulinastatin, gabexate mesilate, and nafamostat mesilate in preservation solution for islet isolation. Cell Transplant. 2012;21(2-3):509-16. doi: 10.3727/096368911X605420. doi: 10.5009/gnl.2012.6.2.256. Epub 2012 Apr 17.
    15: Kwon YH, Kim JY, Lee SJ, Jang SY, Park HW, Yang HM, Jung MK, Jeon SW, Cho CM, Tak WY, Kweon YO, Kim SK. [Could nafamostat or gabexate prevent the post endoscopic retrograde cholangiopancreatography pancreatitis?]. Korean J Gastroenterol. 2012 Mar;59(3):232-8. Korean. doi: 10.1016/j.ajem.2011.06.003. Epub 2011 Dec 26. doi: 10.1016/j.transproceed.2011.10.035. Japanese. doi: 10.1016/j.transproceed.2010.10.007.

    合成参考文献


    摘要:Nippon Yakurigaku Zasshi. Japanese Journal of Pharmacology., 71(71), 1975 []
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