CAS: 1947-37-1; Tetragastrin

该化合物是一种模仿自然产生的激素催化剂作用的合成浸泡物,主要用于刺激胃胃的胃酸分泌,由对其生物活动至关重要的氨基酸序列组成,在研究和临床环境中经常使用四甲氏剂研究胃肠道的气分功能并评估胃肠道的生理反应,其结构允许它与特定的气分泌受体结合,从而推动气分解,提高消化过程.该物质通常在受控制的剂量下施用,因为其影响会影响胃pH和总体消化健康.此外,四甲丙丙氏剂在诊断程序中,特别是在评估胃酸分泌和胃肌肉功能方面,应用了各种诊断程序,尤其是用于评估胃酸分泌和胃肌肉的功能.与任何微粒激素,其稳定性,溶性,溶性以及生物利用率一样,都是影响其治疗和研究应用效力的重要因素.

结构式图片

上下游产品

L-Tryptophyl-L-Methionyl-L-Aspartyl-L-Phenylalanine 35144-91-3
叔丁氧羰基-色氨酰-蛋氨酰-天冬氨酰-苯丙氨酰胺 N-Tert-Butoxycarbonyl-L-Tryptophyl->L-Methionyl->L-α-Aspartyl->L-Phenylalanine Amide 5235-21-2
H-Trp-Met-Asp-Oh 97586-87-3
N-叔丁氧羰基-L-色氨酸 Boc-Trp-Oh 13139-14-5
N-[(1,1-二甲基乙氧基)羰基]-L-色氨酸 4-硝基苯基酯 Boc-Trp-Onp 15160-31-3

合成工艺路线路线简述

    📜L-Tryptophyl-L-Methionyl-L-Aspartyl-L-Phenylalanine置于bacillus Licheniformis Serine Endoprotease,氨体系中,用 1,4-二氧六环,N,N-二甲基甲酰胺,叔丁醇 用作溶剂,化学反应 16.0H,反应生成四肽胃泌素
    参考文献:氨基酸和多肽的酶促c末端酰胺化
    标题:氨基酸和多肽的酶促c末端酰胺化
    摘要:在本文中,我们描述了两种通用且高产的酶促方法,可将半保护的氨基酸和肽基c末端α-羧酸转化为它们相应的酰胺.在第一种方法中,分别使用脂肪酶南极假丝酵母脂肪酶-B(cal-B),在第二种方法中,分别使用蛋白酶枯草杆菌蛋白酶a.我们发现,通过使用α-羧酸的铵盐代替单独的氨源,酶促酰胺化反应的进行速度大大加快,而没有副反应,并且使产物收率接近定量.
    Doi:10.1016/j.Tetlet.2012.05.039

    海关参考信息

    专利信息


    专利号:US-5817751-A
    优先权日:1994-06-23
    标 题 :Method for synthesis of diketopiperazine and diketomorpholine derivatives
    发明人:SZARDENINGS ANNA KATRIN; CAMPBELL DAVID
    权利人:AFFYMAX TECH NV
    摘要:The present invention relates to the areas of organic and medicinal chemistry. More specifically, the present invention is concerned with combinatorial and solid phase methods for the synthesis of diverse diketopiperazine derivatives, and the use of such methods to create libraries of diverse diketopiperazine derivatives. The present invention has application in the areas of chemical synthesis, the screening for new diketopiperazine derivatives having beneficial medical properties and the use of such screening to provide compositions and methods including diketopiperazine derivatives for treating disease.

    专利号:US-11845970-B2
    优先权日:2016-01-15
    标 题:Endo-S2 mutants as glycosynthases, method of making and use for glycoengineering of glycoproteins
    发明人:WANG LAI-XI; YANG QIANG; LI TIEZHENG; TONG XIN
    权利人:UNIV MARYLAND
    摘要:The present invention provides for recombinant Endo-S2 mutants (named Endo-S2 glycosynthases) that exhibit reduced hydrolysis activity and increased transglycosylation activity for the synthesis of glycoproteins wherein a desired sugar chain is added to a fucosylated or nonfucosylated GlcNAc-IgG acceptor. As such, the present invention allows for the synthesis and remodeling of therapeutic antibodies thereby providing for certain biological activities, such as, prolonged half-life time in vivo, less immunogenicity, enhanced in vivo activity, increased targeting ability, and/or ability to deliver a therapeutic agent.

    专利号:US-2003147958-A1
    优先权日:2002-01-29
    标题 :Biodegradable multi-block copolymers of poly(amino acid)s and poly(ethylene glycol) for the delivery of bioactive agents
    发明人:AHN CHEOL-HEE; CHAE SU YOUNG
    摘要:This patent discloses the synthesis of a multi-block copolymer containing poly(amino acids) (PAA) and a hydrophilic polymer which are degradable under physiological conditions. Control over the degradation rate of the obtained copolymers is achieved by introducing ester, amide or urethane groups as a biodegradable linkage connecting the PAA and the hydrophilic polymer. The biodegradable multi-block copolymers display high transfection efficiency in plasmid delivery with low cytotoxicity.

    专利号:US-11459380-B2
    优先权日:2017-06-29
    标 题 :Transglycosylation of endo-S and endo-S mutants for antibody glycosylation remodeling
    发明人:WANG LAI-XI; TONG XIN; LI TIEZHENG
    权利人:UNIV MARYLAND
    摘要:The present invention provides for a one-pot enzymatic approach which does not require removal of the enzyme and purification of the intermediate after deglycosylation step, and the Endo-S treatment is able to do both deglycosylation and transglycosylation. The one-pot strategy of the present invention enables chemoenzymatic synthesis of an azido-tagged N-glycoform of monocloncal antibodies which could be further modified through orthogonal chemical ligation for various applications.

    专利号:WO-9600391-A1
    优先权日:1994-06-23
    标题:Methods for the synthesis of diketopiperazines
    发明人:CAMPBELL DAVID; GALLOP MARK A; GORDON ERIC M; LOOK GARY C; PATEL DINESH; SZARDENINGS ANNA KATRIN
    权利人:AFFYMAX TECH NV; CAMPBELL DAVID; GALLOP MARK A; GORDON ERIC M; LOOK GARY C; PATEL DINESH; SZARDENINGS ANNA KATRIN
    摘要:Libraries of diverse diketopiperazines bound to a support and methods for synthesizing diketopiperazines on a solid support are described. These libraries have utility in the area of drug design as they can be screened against biological substances to identify compounds which have desirable biological activity.

    专利号:US-11702652-B2
    优先权日:2005-12-01
    标题:Enzymatic encoding methods for efficient synthesis of large libraries

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    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: Tenma T, Yodoya E, Tashima S, Fujita T, Murakami M, Yamamoto A, Muranishi S. Development of new lipophilic derivatives of tetragastrin: physicochemical characteristics and intestinal absorption of acyl-tetragastrin derivatives in rats. Pharm Res. 1993 Oct;10(10):1488-92.
    10: Tatsuta M, Iishi H, Baba M, Taniguchi H. Effect of ornithine decarboxylase inhibitor on tetragastrin treatment of gastric carcinogenesis induced by N-methyl-N'-nitro-N-nitrosoguanidine in Wistar rats. Int J Cancer. 1990 Feb 15;45(2):308-11. pii: pyu053. doi: 10.1093/ijnp/pyu053.
    12: Desai SJ, Borkar CD, Nakhate KT, Subhedar NK, Kokare DM. Neuropeptide Y attenuates anxiety- and depression-like effects of cholecystokinin-4 in mice. Neuroscience. 2014 Sep 26;277:818-30. doi: 10.1016/j.neuroscience.2014.07.062. Epub 2014 Aug 7. Russian. doi: 10.1371/journal.pone.0110502. eCollection 2014.

    合成参考文献


    摘要:Drugs in Japan, -(816), 1995
    参考文献:10.1016/0006-3223(96)00008-x
    摘要:Eriksson M, Eklundh T, Sjöberg S, Angelin B, Nordin C. Cholesterol lowering and cerebrospinal fluid neurotransmitters: increased levels of the anxiogenic cholecystokinin-tetrapeptide during simvastatin administration to healthy male volunteers. Biol Psychiatry. 1996 Aug 15;40(4):302–4. doi: 10.1016/0006-3223(96)00008-x.
    参考文献:10.1007/bf01273363
    摘要:Löfberg C, Harro J, Gottfries CG, Oreland L. Cholecystokinin peptides and receptor binding in Alzheimer's disease. J Neural Transm (Vienna). 1996;103(7):851–60. doi: 10.1007/bf01273363.
    参考文献:10.1016/0924-977x(96)00018-1
    摘要:van Megen HJ, Westenberg HG, Den Boer JA, Kahn RS. The panic-inducing properties of the cholecystokinin tetrapeptide CCK4 in patients with panic disorder. Eur Neuropsychopharmacol. 1996 Aug;6(3):187–94. doi: 10.1016/0924-977x(96)00018-1.
    参考文献:10.1016/0006-3223(95)00479-3
    摘要:Koszycki D, Zacharko RM, Le Melledo JM, Young SN, Bradwejn J. Effect of acute tryptophan depletion on behavioral, cardiovascular, and hormonal sensitivity to cholecystokinin-tetrapeptide challenge in healthy volunteers. Biol Psychiatry. 1996 Oct 01;40(7):648–55. doi: 10.1016/0006-3223(95)00479-3.
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