CAS: 107444-51-9; L-Histidyl-L-Alanyl-L-α-Glutamylglycyl-L-Threonyl-L-Phenylalanyl-L-Threonyl-L-Seryl-L-α-Aspartyl-L-Valyl-L-Seryl-L-Seryl-L-Tyrosyl-L-Leucyl-L-α-Glutamylglycyl-L-Glutaminyl-L-Alanyl-L-Alanyl-L-Lysyl-L-α-Glutamyl-L-Phenylalanyl-L-Isoleucyl-L-Alanyl-L-Tryptophyl-L-Leucyl-L-Valyl-L-Lysylglycyl-L-Argininamide

该化合物是一种在葡萄糖代谢和食欲调控方面起着关键作用的浸泡激素,它来自丙烯酸基因,主要由肠道L细胞根据食物摄入量进行隐秘.这种浸泡酸由30氨基酸组成,以其能以依赖葡萄糖的方式刺激胰岛素分泌,从而有助于降低血糖水平.此外,GLP-1碎片7-36氨酸抑制甘油释放,慢化气气清空和促销,使其成为糖尿病治疗和肥胖管理的目标.氨化物表表明,酸的C终点受到恐吓,这对于其生物活动和稳定性十分重要.由于其生理影响,GlP-1及其类物质被用于治疗应用,特别是用于管理2类糖尿病.化学文摘社编号为10744-51-9,在化学数据库中独特地确认了这种具体的浸渍,促进了药学和生物化学化学化学学的研究与发展.

结构式图片

合成工艺路线路线简述

    专利信息


    专利号:US-2012203004-A1
    优先权日:2009-08-13
    标题 :process for the synthesis of alkyl/aralkyl (2s)-2-(tert-butoxycarbonyl)-amino-2-[-8-azabicyclo[3.2.1]oct-3-yl]-exo-acetate and analogs thereof: key intermediates for the preparation of dppiv inhibitors
    发明人:ROY BHAIRAB NATH; KAMBOJ RAJENDER KUMAR; GOERGE SHAJI K; VENUGOPAL SPINVIN C; SHANMUGVADIVELU MUTHU KUMARAN; SINHA NEELIMA
    权利人:ROY BHAIRAB NATH; KAMBOJ RAJENDER KUMAR; GOERGE SHAJI K; VENUGOPAL SPINVIN C; SHANMUGVADIVELU MUTHU KUMARAN; SINHA NEELIMA; LUPIN LTD
    摘要:An improved process for the synthesis of intermediates like Alkyl/Aralkyl (2S)-2-(tert-butoxycarbonyl)-amino-2-[-8-azabicyclo[3.2.1]oct-3-yl]-exo-acetate and analogs thereof which are useful in the synthesis of Dipeptidyl peptidase-IV (DP-PIV) inhibitors.

    专利号:US-2019177392-A1
    优先权日:2014-09-23
    标 题 :Synthesis of glp-1 peptides
    发明人:PENIAS NAVON SHARON; NAVEH SHIRLY; VASILEIOU ZOI; BARLOS KONSTANTINOS
    权利人:NOVETIDE LTD
    摘要:Disclosed are processes for the synthesis of GLP-1 peptides, such as liraglutide and semaglutide, and a process for purifying liraglutide.

    专利号:US-10005720-B2
    优先权日:2013-04-05
    标题:Compounds useful for the treatment of metabolic disorders and synthesis of the same
    发明人:SEXTON JONATHAN Z; BRENMAN JAY E; MUSSO DAVID L
    权利人:NORTH CAROLINA CENTRAL UNIV; UNIV NORTH CAROLINA CHAPEL HILL
    摘要:The present invention provides compounds of Formula (I): wherein variables X, Y, Z and R1 are as described herein. Some of the compounds described herein are glutamate dehydrogenase activators. The invention is also directed to pharmaceutical compositions comprising these compounds, uses of these compounds and compositions in the treatment of metabolic disorders as well as synthesis of the compounds.

    专利号:US-9475837-B2
    优先权日:2011-12-23
    标题 :Process for the synthesis of therapeutic peptides
    发明人:HURLEY FIONN; WEGNER KATARZYNA; FOLEY PATRICK
    权利人:IPSEN MFG IRELAND LTD
    摘要:The present invention relates to a process for the large-scale synthesis of therapeutic peptides using a Sieber Amide resin, which comprises solid-phase Fmoc-chemistry.

    专利号:US-11518794-B2
    优先权日:2016-08-19
    标 题:Synthesis method for liraglutide with low racemate impurity
    发明人:FU YUQING; MA HONGJI; LI XINYU; ZHANG LIXIANG; ZHI QIN; WU LIFEN; LIU ZICHENG
    权利人:SHENZHEN JYMED TECH CO LTD
    摘要:A synthesis method for low-racemization impurity liraglutide comprises the following steps: performing synthesis to obtain a propeptide, coupling 2 to 5 peptides comprising Thr-Phe on the propeptide by using a solid-phase synthesis method; further, performing solid-phase synthesis to obtain a liraglutide resin; the liraglutide resin is cracked after modification, or the liraglutide resin is directly cracked, purified and frozen dry, so as to obtain the liraglutide. The provided liraglutide synthesis method effectively restrains or reduces the generation of racemization impurity D-Thr 5 highly similar to a product property, which facilitates the purification of the coarse liraglutide, and the high yield of the liraglutide is ensured, thereby greatly reducing production costs; during the synthesis of the liraglutide, the syntheses between dipeptide fragments, tripeptide fragments, the tetrapeptide fragments and pentapeptide fragments and the Gly-resin or the syntheses between the combination of the dipeptide fragments, the tripeptide fragments, the tetrapeptide fragments and pentapeptide fragments and the Gly resin can be carried out at the same time, and accordingly the synthesis time is shortened to some extent.

    专利号:US-2020354404-A1
    优先权日:2019-05-09
    标 题 :Peptidomimetic agents, synthesis and uses thereof
    发明人:AL-ABED YOUSEF
    权利人:FEINSTEIN INSTITUTES FOR MEDICAL RESEARCH
    摘要:Compounds for use in synthesis of peptidomimetic agents; synthesis of peptidomimetic agents; peptidomimetic diagnostic and therapeutic agents; and uses of the compounds and peptidomimetic agents in drug discovery, diagnosis, prevention and treatment of diseases are described.
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    合成参考文献


    参考文献:10.1038/ajh.2009.271
    摘要:Dandona P, Chaudhuri A, Dhindsa S. A Novel Antihypertensive Effect of Exenatide, a GLP-1 Agonist. American Journal of Hypertension. 2010 Mar 01;23(3):228. doi: 10.1038/ajh.2009.271.
    参考文献:10.1111/j.1365-2982.2010.01476.x
    摘要:Amato A, Cinci L, Rotondo A, Serio R, Faussone-Pellegrini MS, Vannucchi MG, Mulè F. Peripheral motor action of glucagon-like peptide-1 through enteric neuronal receptors. Neurogastroenterol Motil. 2010 Jun;22(6):664–e203. doi: 10.1111/j.1365-2982.2010.01476.x.
    参考文献:10.1016/s0140-6736(10)60225-5
    摘要:Hallberg P, Schwan S, Melhus H. Liraglutide for weight loss in obese people. Lancet. 2010 Feb 13;375(9714):551; author reply 552–3. doi: 10.1016/s0140-6736(10)60225-5.
    参考文献:10.1016/s0140-6736(10)60226-7
    摘要:Thum T, Anker SD. Liraglutide for weight loss in obese people. Lancet. 2010 Feb 13;375(9714):551–2; author reply 552. doi: 10.1016/s0140-6736(10)60226-7.
    参考文献:10.1097/mpa.0b013e318214832d
    摘要:Kim YS, Oh SH, Park KS, No H, Oh BJ, Kim SK, Jung HS, Kim JH, Lee MS, Lee MK, Kim KW. Improved outcome of islet transplantation in partially pancreatectomized diabetic mice by inhibition of dipeptidyl peptidase-4 with sitagliptin. Pancreas. 2011 Aug;40(6):855–60. doi: 10.1097/mpa.0b013e318214832d.
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