angiotensin II | 32044-01-2

• 分子结构分类: 有机化合物 - 有机酸及其衍生物 - 羧酸及其衍生物
• 英文名称: angiotensin II
• 英文别名: angiotensin II acetate；human angiotensin II (acetate salt)；Asp-arg-val-tyr-ile-his-pro-phe acetate salt；acetic acid;(3S)-3-amino-4-[[(2S)-1-[[(2S)-1-[[(2S)-1-[[(2S,3S)-1-[[(2S)-1-[(2S)-2-[[(1S)-1-carboxy-2-phenylethyl]carbamoyl]pyrrolidin-1-yl]-3-(1H-imidazol-5-yl)-1-oxopropan-2-yl]amino]-3-methyl-1-oxopentan-2-yl]amino]-3-(4-hydroxyphenyl)-1-oxopropan-2-yl]amino]-3-methyl-1-oxobutan-2-yl]amino]-5-(diaminomethylideneamino)-1-oxopentan-2-yl]amino]-4-oxobutanoic acid
• CAS: 32044-01-2
• 化学式: C₂H₄O₂*C₅₀H₇₁N₁₃O₁₂
• 分子量: 1106.25
• InChiKey: VBTZKFAHKJXHBA-PIONDTTLSA-N

计算性质

• 辛醇/水分配系数(LogP)：
  -1.22
• 重原子数：
  79
• 可旋转键数：
  29
• 环数：
  4.0
• sp3杂化的碳原子比例：
  0.5
• 拓扑面积：
  446
• 氢给体数：
  14
• 氢受体数：
  17

反应信息

• 作为产物：
  描述：

  Z-Asp(OBzl)-Arg(NO2)-Val-Tyr(Bzl)-Ile-His(Bzl)-Pro-Phe-OBzl 在 钯 氢气 、 溶剂黄146 作用下， 以 水 、 N,N-二甲基甲酰胺 为溶剂， 反应 42.0h， 以63%的产率得到angiotensin II
  参考文献：
  名称：

  Rapid Peptide Synthesis in Liquid Phase. Preparation of Angiotensin II and Delta-sleep-inducing Peptide by the “Hold-in-Solution” Method

  摘要：

  通过制备保护型血管紧张素II（Z-Asp(OBzl)-Arg(NO2)-Val-Tyr(Bzl)-Ile-His(Bzl)-Pro-Phe-OBzl，化合物1）和保护型δ睡眠诱导肽（Z-Trp-Ala-Gly-Gly-Asp(OBzl)-Ala-Ser(Bzl)-Gly-Glu(OBzl)-OBzl，化合物2），展示了一种新的快速肽合成技术。在1,2-二氯乙烷中，通过重复以下操作序列来延长肽链：使用1-乙基-3-(3-二甲基氨基丙基)碳二亚胺盐酸盐和1-羟基苯并三唑对氨基酸或肽的苄酯进行Boc-氨基酸的酰化；清洗有机层；α-氨基保护基的酸解；中和；以及清洗。在整个合成过程中，生长中的肽链始终保持在有机层中而不被分离。保护型肽1和2分别以其C端氨基酸酯为基准，得到了78%和53%的总收率，随后经过氢化分别得到了血管紧张素II和δ睡眠诱导肽，从而证明了这种方法在快速肽合成中的实用性。

  DOI：

  10.1246/bcsj.55.2165

文献信息

• DPP3 IN PATIENTS INFECTED WITH CORONAVIRUS
  申请人：4TEEN4 Pharmaceuticals GmbH

  公开号：EP3922993A1

  公开（公告）日：2021-12-15

  Subject matter of the present invention is a method for (a) diagnosing or predicting the risk of life-threatening deterioration or an adverse event or (b) diagnosing or prognosing the severity or (c) predicting or monitoring the success of a therapy or intervention or (d) therapy guidance or therapy stratification or (e) patient management in a patient infected with a coronavirus, the method comprising: • determining the level of dipeptidyl peptidase 3 (DPP3) in a sample of bodily fluid of said patient, • comparing said level of determined DPP3 to a pre-determined threshold, and • correlating said level of determined DPP3 with the risk of life-threatening deterioration or an adverse event, or • correlating said level of determined DPP3 with the severity, or • correlating said level of determined DPP3 with the success of a therapy or intervention, or • correlating said level of DPP3 with a certain therapy or intervention, or • correlating said level of DPP3 with the management of said patient. Subject matter of the present invention is an inhibitor of the activity of DPP3 for use in therapy or intervention in a patient infected with a coronavirus.

  本发明的主题是一种用于(a)诊断或预测威胁生命的恶化风险或不良事件，或(b)诊断或预后严重程度，或(c)预测或监测治疗或干预的成功，或(d)治疗指导或治疗分层，或(e)感染冠状病毒患者的患者管理的方法，该方法包括： - 确定所述患者体液样本中二肽基肽酶 3 (DPP3) 的水平、 - 将所述测定的 DPP3 水平与预设阈值进行比较，以及 - 将所述测定的 DPP3 水平与危及生命的病情恶化或不良事件的风险相关联，或 - 将所述测定的 DPP3 水平与严重程度相关联，或 - 将所述测定的 DPP3 水平与治疗或干预的成功相关联，或 - 将所述 DPP3 水平与某种疗法或干预措施相关联，或 - 将所述 DPP3 水平与所述患者的管理相关联。 本发明的主题是一种用于治疗或干预冠状病毒感染患者的 DPP3 活性抑制剂。
• Angiotensin II alone or in combination for the treatment of hypotension
  申请人：The George Washington University a Congressionally Chartered Not-for-Profit Corporation

  公开号：US10028995B2

  公开（公告）日：2018-07-24

  The present invention relates, inter alia, to a method comprising administering to a subject having high output shock and undergoing treatment with a catecholamine at a dose equivalent to at least about 0.2 mcg/kg/min of norepinephrine a dose of angiotensin II which is effective to raise the blood pressure of the subject to a mean arterial pressure (MAP) of about 65 mm or above, and which is effective to reduce the dose of the catecholamine required to maintain a MAP of about 65 mm to the equivalent of about 0.05-0.2 mcg/kg/min norepinephrine or less, or to the equivalent of about 0.05 mcg/kg/min norepinephrine or less.

  本发明尤其涉及一种方法，该方法包括向患有高输出性休克并正在接受儿茶酚胺治疗的受试者施用剂量至少相当于约 0.2 微克/千克/分钟去甲肾上腺素的剂量的血管紧张素 II，该剂量能有效地将受试者的血压升至约 65 毫米或以上的平均动脉压（MAP），并能有效地将维持约 65 毫米的 MAP 所需的儿茶酚胺剂量减少至相当于约 0.05-0.2 微克/千克/分钟去甲肾上腺素或更少，或相当于约 0.05 微克/千克/分钟去甲肾上腺素或更少。
• Treatment for reducing adverse events including chemotherapy discomfort and other conditions
  申请人：Siamon Al

  公开号：US11000540B1

  公开（公告）日：2021-05-11

  This disclosure relates to treatments for reducing the side effects associated with treatment of a medication or drug, such as a chemotherapy medication, being experienced by a patient. This may be accomplished by administering to a patient taking the medication, a buffered aqueous liquid having a pH of about 10 to about 11.5.

  本公开涉及减少患者在接受药物治疗（如化疗药物）时所产生的副作用的治疗方法。这可以通过向服用药物的患者施用 pH 值约为 10 至 11.5 的缓冲水液来实现。
• Anti-NPR1 antibodies and uses thereof
  申请人：Regeneron Pharmaceuticals, Inc.

  公开号：US11306148B2

  公开（公告）日：2022-04-19

  The present invention provides monoclonal antibodies that bind to the natriuretic peptide receptor 1 (NPR1) protein, and methods of use thereof. In various embodiments of the invention, the antibodies are fully human antibodies that bind to NPR1. In some embodiments, the antibodies of the invention are useful for activating NPR1 activity, thus providing a means of treating or preventing a disease, disorder or condition associated with NPR1 in humans.

  本发明提供了与利钠肽受体 1（NPR1）蛋白结合的单克隆抗体及其使用方法。在本发明的各种实施方案中，抗体是与 NPR1 结合的全人抗体。在一些实施方案中，本发明的抗体可用于激活 NPR1 的活性，从而提供一种治疗或预防与人类 NPR1 相关的疾病、紊乱或病症的方法。
• Photokinetic delivery of biologically active substances using pulsed incoherent light
  申请人：——

  公开号：US20040131687A1

  公开（公告）日：2004-07-08

  The invention relates generally to transdermal and transmembrane delivery of biologically active substances through the skin, sub-dermal tissues, blood vessels and cellular membranes without causing damage to the cellular surface, tissue or membrane. The invention provides compositions and methods for enhanced transdermal and transmembrane delivery of biologically active substances using pulsed incoherent light. The invention further provides a device for the application of the pulsed incoherent light to cellular surfaces and membranes using those compositions and methods.

  本发明一般涉及生物活性物质通过皮肤、皮下组织、血管和细胞膜的透皮和跨膜给药，而不会对细胞表面、组织或膜造成损伤。本发明提供了利用脉冲非相干光增强生物活性物质透皮和跨膜递送的组合物和方法。本发明进一步提供了使用这些组合物和方法将脉冲非相干光应用于细胞表面和细胞膜的装置。