CAS: 258818-34-7; 2-((S)-1-((2S,5S,8S,11S)-17-Amino-2-(3-Amino-3-Oxopropyl)-8-Isobutyl-5,11-Diisopropyl-4,7,10,13,16-Pentaoxo-3,6,9,12,15-Pentaazaheptadecan-1-Oyl)Pyrrolidine-2-Carboxamido)Acetic Acid

该化合物是一种调制肠道紧闭关口的蛋白质,主要被调查其在肠道障碍功能失调(如病)条件下的潜在治疗作用.通过有选择地针对zonulin 信号, lazaotide 帮助恢复紧凑关口的完整性, 减少细胞渗透性, 并防止免疫性的转移. 它的行动机制为管理与阻塞有关的自动免疫和炎症反应提供了有针对性的方法. Larazotide 在临床试验中展示了有利的安全特征, 并尽可能减少系统吸收, 使其成为局部肠胃治疗的有希望的候选对象. 研究继续探索其在其他屏障相关疾病中的更广泛应用.

结构式图片

MSDS等安全信息

    合成工艺路线路线简述

      Larazotide Acetate,,,以 水 用作溶剂,化学反应 14.0H,反应生成甘氨酰甘氨酰-L-缬氨酰-L-亮氨酰-L-缬氨酰-L-谷氨酰胺酰-L-脯氨酰甘氨酸
      参考文献:Larazotide Acetate Compositions
      标题:Larazotide Acetate Compositions
      摘要:该发明提供了肽gly-Gly-Val-Leu-Val-Gln-Pro-Gly(seq Id No 1)的晶体形式以及该肽的盐,其中可能进一步具有关联的水分子.这些肽盐和水合肽盐以及包含这些材料的组合物具有有利的药物特性.

      海关参考信息

      专利信息


      专利号:US-12351573-B2
      优先权日:2019-05-09
      标 题:Compounds for use in synthesis of peptidomimetics
      发明人:AL-ABED YOUSEF; CHENG KAI FAN
      权利人:FEINSTEIN INSTITUTES FOR MEDICAL RESEARCH
      摘要:Synthesis of O-benzotriazole and O-imidazole synthons are described. Uses of synthons in synthesis of azapeptides and other peptidomimetics, azapeptides and other peptidomimetics synthesized from the synthons and uses of azapeptides and other peptidomimetics are also described.

      专利号:US-2023159450-A1
      优先权日:2020-05-08
      标 题 :Dimers for use in synthesis of peptidomimetics
      发明人:AL-ABED YOUSEF; ALTITI AHMAD
      权利人:FEINSTEIN INSTITUTES FOR MEDICAL RESEARCH
      摘要:Dimers for use in synthesis of peptidomimetics are described. Uses of dimers as synthons in synthesis of azapeptides and other peptidomimetics, azapeptides and other peptidomimetics synthesized from the dimers and uses of azapeptides and other peptidomimetics are also described.

      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.

      专利号:US-11440881-B2
      优先权日:2019-05-09
      标题 :Thiosemicarbazates and uses thereof
      发明人:AL-ABED YOUSEF; ALTITI AHMAD
      权利人:FEINSTEIN INSTITUTES FOR MEDICAL RESEARCH
      摘要:Thioesters, thiocarbamates, thiocarbazates, semithiocarbazates, peptides, aza-amino acid conjugates, and azapeptides; and a chemoselective and site-specific functionalization protocol of protected thiocarbazates and semithiocarbazates are described. The protocol features the use of Mitsunobu reaction to alkylate specifically the nitrogen atom close to the acylthiol moiety with alcohols to produce protected mono-substituted thiocarbazates that can be stored for months, activated under mild conditions at low temperature using halonium reagents and integrated orthogonally to make substituted semicarbazides that can be used, e.g., as synthons in synthesis of aza-amino acid conjugates, azapeptides and other peptidomimetics. Methods for preparing and using ureases, carbazides, semicarbazides, beta-peptides, azapeptides, and other peptidomimetics and azapeptide conjugates, and uses of ureases, carbazides, semicarbazides, beta-peptides, azapeptides in drug discovery, diagnosis, inhibition, prevention and treatment of diseases are also described.

      专利号:US-2022372022-A1
      优先权日:2019-05-09
      标 题:Compounds for use in synthesis of peptidomimetics

      专利号:US-10919882-B2
      优先权日:2019-05-09
      标题:Compounds for use in synthesis of peptidomimetics
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      ✅ COA系统入驻 | 共享模式

      主要参考文献


      1: Yonker LM, Swank Z, Gilboa T, Senussi Y, Kenyon V, Papadakis L, Boribong BP, Carroll RW, Walt DR, Fasano A. Zonulin Antagonist, Larazotide (AT1001), As an Adjuvant Treatment for Multisystem Inflammatory Syndrome in Children: A Case Series. Crit Care Explor. 2022 Feb 18;10(2):e0641. doi: 10.1097/CCE.0000000000000641.
      2: Caliskan AR, Gul M, Yılmaz I, Otlu B, Uremis N, Uremis MM, Kilicaslan I, Gul S, Tikici D, Saglam O, Yalcin M, Demirel U, Harputluoglu M. Effects of larazotide acetate, a tight junction regulator, on the liver and intestinal damage in acute liver failure in rats. Hum Exp Toxicol. 2021 Dec;40(12_suppl):S693-S701. doi: 10.1177/09603271211058882. Epub 2021 Nov 18. 22(17):9427. doi: 10.3390/ijms22179427.
      4: Hoilat GJ, Altowairqi AK, Ayas MF, Alhaddab NT, Alnujaidi RA, Alharbi HA, Alyahyawi N, Kamal A, Alhabeeb H, Albazee E, Almustanyir S, Abu-Zaid A. Larazotide acetate for treatment of celiac disease: A systematic review and meta-analysis of randomized controlled trials. Clin Res Hepatol Gastroenterol. 2022 Jan;46(1):101782. doi: 10.1016/j.clinre.2021.101782. Epub 2021 Jul 31. 16(4):e0250165. doi: 10.1371/journal.pone.0250165.

      合成参考文献


      参考文献:10.1007/s10620-017-4489-y
      摘要:Discepolo V, Guandalini S. Celiac Disease Treatment: Is It the Chicken or the Egg Yolk Digestive Diseases and Sciences. 2017 Feb 13;62(5):1113–5. doi: 10.1007/s10620-017-4489-y.
      摘要:S55 | ZINC15PHARMA | Pharmaceuticals from ZINC15 | DOI:10.5281/zenodo.3247749
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