CAS: 51833-78-4; Angiotensin (1-7)

该化合物是一种生物活性七乙胺,来源于 renin-angiotensin 系统,以其抗抗血管抑制作用著称.它主要通过马斯受体,血管传播调节,抗炎和抗纤维作用来进行.主要优势包括它可能用于心血管疾病,如高血压和心脏衰竭,因为它有能力改善内皮利功能和减少氧化性压力.此外,血管毒理(1-7)展示肾脏保护特性,并可能调节代谢障碍.它的肺部结构可以精确定位病理途径,成为心血管和代谢治疗研究的有前途的候选者.

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CAS号4474-91-3 血管紧张素II

合成工艺路线路线简述

    📜血管紧张素ii置于angiotensin Converting Enzyme 2,Zinc(II) Chloride体系中,化学反应生成 天冬氨酰-精氨酰-缬氨酰-酪氨酰-异亮氨酰-组氨酰-脯氨酸
    参考文献:Nanokit 耦合电喷雾电离质谱分析单个活细胞中血管紧张素转换酶 2 的活性
    标题:Nanokit 耦合电喷雾电离质谱分析单个活细胞中血管紧张素转换酶 2 的活性
    摘要:血管紧张素转换酶2(ace2)不仅是一种酶,也是严重急性呼吸综合征冠状病毒2(sars-Cov-2)细胞膜上的功能受体.在这里,首先使用 Nanokit 耦合电喷雾电离质谱 (Nanokit-Esi-Ms) 测定单个活细胞中 Ace2 的活性.将微毛细管插入活的 Hace2-Cho 细胞并对细胞质进行电化学分选后,目标 Ace2 酶会水解毛细管内的血管紧张素 Ii,反应生成血管紧张素 1-7.将混合物电喷雾到毛细管尖端后,产物与底物在分子量上进行区分,从而实现单细胞中ace2活性的检测.进一步的测量表明细胞的炎症状态并没有导致ace2催化活性的显着变化,这在单细胞水平上阐明了细胞内ace2活性与炎症之间的关系.所建立的策略将为进一步研究ace2在病毒感染过程中的作用提供具体的分析方法,并扩展基于纳米试剂盒的单细胞分析的应用.
    DOI:10.1016/j.Cclet.2022.05.036

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    专利信息


    专利号:US-2004033532-A1
    优先权日:2002-08-08
    标题 :Use of three-dimensional crystal structure coordinates to design and synthesize domain-selective inhibitors for angiotensin-converting enzyme (ACE)
    发明人:EHLERS MARIO R W; HOLMQUIST BARTON
    摘要:It has now been discovered that the use of the three-dimensional crystal structure coordinates of angiotensin-converting enzyme (ACE) will enable the design and synthesis, by means of computational chemistry and structure-guided drug design, of inhibitors of ACE that are highly selective and specific for either the N domain or the C domain of the enzyme, for the treatment of diverse diseases. The invention also relates to methods and processes for the structure-guided design and synthesis of dual N- and C-domain ACE inhibitors, and inhibitors that operate by competitive, non-competitive, uncompetitive, and irreversible mechanisms.

    专利号:US-7951834-B2
    优先权日:2005-05-27
    标题 :Angiotensin I-converting enzyme (ACE) inhibitors
    发明人:STURROCK EDWARD; NCHINDA ALOYSIUS; CHIBALE KELLY
    权利人:UNIV CAPE TOWN
    摘要:This invention relates to a process for the synthesis of ketomethylene derivatives of the tripeptide Phe-Gly-Pro (“keto-ACEâ€?, compound 5 a ) and analogues thereof. The synthesis process proceeds via an α,β-unsaturated keto intermediate. A key feature of the process involves a Horner-Emmons olefination of the, -unsaturated keto-phosphonate with ethyl glyoxylate. Keto-ACE analogues produced by the process of the invention display C-domain selectivity.

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    ✅ COA系统入驻 | 共享模式

    主要参考文献


    1: Ábrigo J, Simon F, Cabrera D, Cabello-Verrugio C. Angiotensin-(1-7) Prevents Skeletal Muscle Atrophy Induced by Transforming Growth Factor Type Beta (TGF-β) via Mas Receptor Activation. Cell Physiol Biochem. 2016 Nov 14;40(1-2):27-38. [Epub ahead of print] doi: 10.1016/j.peptides.2016.09.009. [Epub ahead of print]

    合成参考文献


    参考文献:10.1074/jbc.m200581200
    摘要:Vickers C, Hales P, Kaushik V, Dick L, Gavin J, Tang J, Godbout K, Parsons T, Baronas E, Hsieh F, Acton S, Patane M, Nichols A, Tummino P. Hydrolysis of Biological Peptides by Human Angiotensin-converting Enzyme-related Carboxypeptidase. Journal of Biological Chemistry. 2002 Apr;277(17):14838–43. doi: 10.1074/jbc.m200581200.
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