CAS: 581-05-5; α-Melanocyte Stimulating Hormone

该化合物是一种浸泡激素,在调控各种生理过程,包括色素,食欲和能量软化作用方面发挥着关键作用,它源自于亲蛋白蛋白质前体,由13种氨基酸构成. -MSH的主要功能是刺激梅氏素的产生,即对皮肤和头发色素产生影响的青蒿素在青蒿素中的生产.此外, -MSH还参与调节炎症反应和调控胃食欲,影响体重和新陈代谢.该物质的特点在于它能够与梅诺索丁摄取器(特别是MMC1R)捆绑在一起,而MMC1R是该物质对色素的影响媒介. -MSH还参与中央...

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N-(fluoren-9-ylmethoxycarbonyl)glycine Fm°C-Val-OH Fm°C-Pro-OH N-Fm°C L-Phe

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    📜Fmoc-L-苯丙氨酸,Fmoc-O-叔丁基-L-丝氨酸,Fmoc-甘氨酸,Fmoc-L-缬氨酸,Fmoc-O-叔丁基-L-酪氨酸,N-Fmoc-N'-三苯甲基-L-组氨酸,Fmoc-L-脯氨酸,Fmoc-L-蛋氨酸,Fmoc-赖氨酸,Fmoc-Pbf-L-精氨酸,Fmoc-L-谷氨酸,Fmoc-L-色氨酸(Boc)-Oh置于6-Chloro-3-((Dimethylamino)(Dimethyliminio)Methyl)-1H-Benzo[d][1,2,3]Triazol-3-Ium-1-Olatehexafluorophosphate(V),N,N-二异丙基乙胺,哌啶体系中,用 N,N-二甲基甲酰胺 作为反应溶剂,化学反应 0.83H,反应生成 Alpha-促黑激素
    参考文献:具有典型氨基酸的mc1R选择性γ-Msh类似物的设计导致效价和色素沉着
    标题:具有典型氨基酸的mc1R选择性γ-Msh类似物的设计导致效价和色素沉着
    摘要:黑色素瘤是皮肤癌的致命形式.受黑色素皮质激素1受体(mc1R)调节的皮肤色素沉着是对黑色素瘤的有效保护.但是,内源性mc1R激动剂对mc1R缺乏选择性,因此会产生副作用.在先前的mc1R配体开发中使用非规范氨基酸引起了安全隐患.在这里,我们报告的第一个有效和选择性的hmc1R激动剂只有规范的氨基酸的发展.使用γ-Msh为模板,我们开发了一种肽,[亮氨酸3,亮氨酸7,苯丙氨酸8]-γ-Msh-Nh 2(化合物5),其是用于hmc1R 16倍选择性(ec 50= 4.5 Nm)与其他黑皮质素受体相比.构象研究揭示了该线性肽的受约束构象.分子对接表明黑皮质素1受体的疏水结合袋.体内色素沉着研究显示,效力高且持续时间短.[亮氨酸3,亮氨酸7,苯丙氨酸8]-γ-Msh-Nh 2是理想的用于诱导短期的皮肤色素沉着,而不太阳黑素瘤预防.
    DOI:10.1021/acs.Jmedchem.7B01295

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    专利信息


    专利号:US-4913852-A
    优先权日:1986-06-24
    标题 :Compounds obtained from the associative synthesis of sulfur-containing or sulfur-free amino acids with pregnane derivatives
    发明人:MILIONI CATHERINE; EFTHYIMIOPOULOS CONSTANTIN; KOCH BERNARD; JUNG LOUIS; JUNG JEAN
    权利人:MILIONI CATHERINE; EFTHYIMIOPOULOS CONSTANTIN; KOCH BERNARD; JUNG LOUIS; JUNG JEAN
    摘要:Compounds obtained from the associative synthesis of sulfur-containing or sulfur-free amino acids with derivatives of Δ-4-pregnene-3,20-dione or with derivatives of Δ-1,4-pregnadiene-3,20-dione of the general formulas (I), (II) and (III), having glucocorticoidal and anti-inflammatory properties have been prepared and tested. Pharmaceutical compositions, medicaments containing them as well as their applications are claimed, particularly in the cutaneous and ophthalmic fields. ##STR1##

    专利号:US-9096647-B2
    优先权日:2008-09-16
    标题 :Simplified one-pot synthesis of [18F]SFB for radiolabeling
    发明人:OLMA SEBASTIAN; SHEN CLIFTON KWANG-FU
    权利人:UNIV CALIFORNIA
    摘要:A non-aqueous single pot synthesis of [ 18 F]SFB is set forth. The [ 18 F]SFB produced with this method is then used, for example, to label a peptide or an engineered antibody fragment (diabody) targeting human epidermal growth factor receptor 2 (HER2) as representative examples of labeled compounds for use as an injectable composition to locate abnormal tissue, specifically tumors within an animal or human using a PET scan.

    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:EP-0097994-B1
    优先权日:1982-06-24
    标 题:Method for the solid-phase synthesis of retro-inverso polypeptides
    摘要:This invention relates to a method for the solid-phase synthesis of polypeptides containing retro-inverted peptide bonds, using polydimethylacrylamide-co-acryloylsarcosimethylester resin cross-linked with N, N min -ethylene-bis-acrylamide as the insoluble support for lengthening the polypeptide chain in stages by the addition of suitable amino acid derivatives and/or peptides in succession. In particular, the method described in the present invention allows the easy preparation, on the polymer matrix, of monoacylated gem-diamino residues using the reagent I, I-bis (trifluoroacetoxy) iodobenzene in mixed aqueous-organic solvents.

    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-5593863-A
    优先权日:1992-02-28
    标 题:Administration of an RNA stem loop structure to modulate protein synthesis
    发明人:EBERWINE JAMES H; SPENCER CORINNE
    权利人:UNIV PENNSYLVANIA
    摘要:A method for modulating synthesis of a selected protein in a cell or tissue by contacting the cell or tissue with at least a portion of a mRNA stem loop structure are provided. Compositions containing a mRNA stem loop structure are also provided.

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    主要参考文献


    1: Leung K. Poly(ethylene glycol)-coated gold nanocages bioconjugated with [Nle(4),d-Phe(7)]-α-melanotropin-stimulating hormone. 2011 May 29 [updated 2011 Jul 14]. Molecular Imaging and Contrast Agent Database (MICAD) [Internet]. Bethesda (MD): National Center for Biotechnology Information (US); 2004-2013. Available from http://www.ncbi.nlm.nih.gov/books/NBK56364/ Peptides. 2007 May;28(5):1020-8. Epub 2007 Feb 17. Epub 2006 May 22. Epub 2006 May 4.
    19: Loir B, Sales F, Deraemaecker R, Morandini R, Garcia-Borron JC, Ghanem G. alpha-Melanotropin immunoreactivity in human melanoma exudate is related to necrosis. Eur J Cancer. 1998 Feb;34(3):424-6.

    合成参考文献


    参考文献:10.1111/j.1939-1676.2011.0745.x
    摘要:McFarlane D, Paradis MR, Zimmel D, Sykes B, Brorsen BW, Sanchez A, Vainio K. The effect of geographic location, breed, and pituitary dysfunction on seasonal adrenocorticotropin and α-melanocyte-stimulating hormone plasma concentrations in horses. J Vet Intern Med. 2011 Jul;25(4):872–81. doi: 10.1111/j.1939-1676.2011.0745.x.
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