CAS: 56-59-7; Felypressin

该化合物是天然peptide激素血管抑制素的一种合成类比,主要用于医疗和牙科应用,用于血管抑制性.它通过对V1受体的约束,导致肌肉平稳收缩和减少当地血液流动.这特别有效,因为它是当地...

结构式图片

合成工艺路线路线简述

    H-Cys-Phe-Phe-Gln-Asn-Cys(Acm)-Pro-Lys-Gly-Nh2置于碘,异抗坏血酸体系中,用 溶剂黄146 作为反应溶剂,化学反应生成 苯赖加压素
    参考文献:Counterion Exchange Process For Peptides
    标题:Counterion Exchange Process For Peptides
    摘要:这项发明涵盖了一种纯化肽的过程,包括将肽加载到rp-HPLC柱上;用药用可接受的对离子盐的水溶液冲洗柱;并用含有有机溶剂和药用可接受的对离子的酸的溶剂混合物从柱中洗脱肽,其中水溶液的ph至少约为6.

    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-2005164912-A1
    优先权日:2003-12-31
    标 题:Methods for recovering cleaved peptide from a support after solid phase synthesis
    发明人:BIGELOW ROGER D; CAIN ROBERT O
    摘要:Methods for the solid phase synthesis of peptides and peptide intermediates, in particular methods involving recovering peptides from resin supports at excellent yield. In this invention, an alternating at least partially repeating cycle of shrinking and swelling treatments are used. Each shrinking or swelling part of a cycle may involve one or more washes. The process provides excellent recovery of peptide in a very efficient manner in terms of the number of individual washes and the total volume of wash reagents used.

    专利号:US-2005165215-A1
    优先权日:2003-12-31
    标 题 :Peptide synthesis and deprotection using a cosolvent
    发明人:BIGELOW ROGER D; SCHWINDT MARK A; WITHERS GREGORY P
    摘要:The invention provides methods for synthesizing peptides, which include taking an organic solvent having non-resin bound protected peptide and performing a deprotection reaction on the non-resin bound protected peptide. In these methods it is not required that the peptide is dried immediately before providing to the deprotection reaction. Also provided are methods of synthesizing peptides, wherein a protected peptide is formed in a solution phase reaction, dissolved into an organic solvent, and then introduced into a deprotection reaction. Also provided are methods of synthesizing peptides, wherein a non-resin bound protected peptide is concentrated in an organic solvent prior to being subject to a deprotection reaction.

    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.
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    合成参考文献


    参考文献:10.2165/00002018-200427060-00004
    摘要:Fisher MM, Doig GS. Prevention of anaphylactic reactions to anaesthetic drugs. Drug Saf. 2004;27(6):393–410. doi: 10.2165/00002018-200427060-00004.
    参考文献:10.1038/s41432-019-0021-x
    摘要:Spivakovsky S. Injectable local anaesthetic agents for dental anaesthesia. Evid Based Dent. 2019 Jun;20(2):42–3. doi: 10.1038/s41432-019-0021-x.
    摘要:Editorial: Vasoconstrictors in local anesthetic. Aust Dent J. 1973 Jun;18(3):191–2.
    摘要:Aochi O, Takeshita S, Kawaguchi C, Goto Y, Yasunaka H. [Fundamental and clinical studies on PLV2 (Octapressin)]. Masui. 1966 May;15(5):436–43.
    摘要:Saito T, Matsuzaki T, Wakisaka K, Okazaki K, Hirano T. [Problems and precautions in the application of octapressin]. Masui. 1966 Oct;15(11):1089–94.
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