Nα-benzoyl-L-phenylalanine-L-valine-L-arginine-p-nitroanilide hydrochloride | 38789-84-3

• 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: Nα-benzoyl-L-phenylalanine-L-valine-L-arginine-p-nitroanilide hydrochloride
• 英文别名: N-α-benzoyl-Phe-Val-Arg-p-NA；n-benzoyl-L-phenylalanyl-L-valyl-L-arginine-p-nitroanilide.HCl；N-Benzoyl-Phe-Val-Arg-p-nitroanilide hydrochloride；N-[(2S)-1-[[(2S)-1-[[(2S)-5-(diaminomethylideneamino)-1-(4-nitroanilino)-1-oxopentan-2-yl]amino]-3-methyl-1-oxobutan-2-yl]amino]-1-oxo-3-phenylpropan-2-yl]benzamide;hydrochloride
• CAS: 38789-84-3
• 化学式: C₃₃H₄₀N₈O₆*ClH
• 分子量: 681.192
• InChiKey: PYVSMZDQQUZGPF-JAQKLANPSA-N

计算性质

• 辛醇/水分配系数(LogP)：
  2.89
• 重原子数：
  48
• 可旋转键数：
  15
• 环数：
  3.0
• sp3杂化的碳原子比例：
  0.3
• 拓扑面积：
  227
• 氢给体数：
  7
• 氢受体数：
  7

文献信息

• Process for determining inhibitor-enzyme complexes
  申请人：CORNELL RESEARCH FOUNDATION, INC.

  公开号：EP0048989A2

  公开（公告）日：1982-04-07

  This invention relates to methods for detecting, identifying and quantifying enzymes, for example, human proteolytic enzymes. The method broadly comprises forming an immobilized or insoluble complex comprising enzyme, enzyme inhibitor and enzyme inhibitor-antibody reactive site and then detecting and identifying, preferably quantitatively, one or more enzymes bound to the complex. In a preferrend embodiment, a matrix, e.g. solid or semisolid surface or permeable matrix, has affixed thereto enzyme inhibitor-antibody or an immunologically active (inhibitor binding) fragment of such an antibody. This insoluble enzyme inhibitor interacting matrix is then contacted with biological fluid, e.g. body fluid, to bind one or more predetermined enzyme inhibitor-enzyme complexes, if present in the biological fluid. The bound enzyme is then detected, identified and preferably quantified.

  本发明涉及检测、鉴定和定量酶的方法，例如人类蛋白水解酶。该方法大致包括形成由酶、酶抑制剂和酶抑制剂-抗体反应位点组成的固定化或不溶性复合物，然后检测和鉴定（最好是定量检测和鉴定）与该复合物结合的一种或多种酶。 在一个优选的实施方案中，基质（例如固体或半固体表面或可渗透基质）上贴有酶抑制剂-抗体或这种抗体的免疫活性（抑制剂结合）片段。然后将这种不溶性酶抑制剂相互作用基质与生物液体（如体液）接触，以结合生物液体中存在的一种或多种预定的酶抑制剂-酶复合物。然后对结合的酶进行检测、鉴定和优选定量。
• Bile acids and biguanides as protease inhibitors for preserving the integrity of peptides in the gut
  申请人：Axcess Limited

  公开号：EP2873420A1

  公开（公告）日：2015-05-20

  The present invention relates to a compound for use in a method of treatment of the human or animal body by therapy, in which method (i) the human or animal body is treated by administering one or more therapeutic peptides, and (ii) said compound is administered to inhibit degradation of said one or more peptides by one or more gut proteases, wherein the compound is a bile acid or a biguanide, or a pharmaceutically acceptable salt of a bile acid or a biguanide, wherein said bile acid is chosen from chenodeoxycholic acid, ursodeoxycholic acid, glycochenodeoxycholic acid and glycodeoxycholic acid.

  本发明涉及一种用于人或动物机体治疗方法的化合物，在该方法中，(i)通过施用一种或多种治疗肽对人或动物机体进行治疗，(ii)施用所述化合物以抑制一种或多种肠道蛋白酶对所述一种或多种肽的降解、 其中所述化合物是胆汁酸或双胍，或胆汁酸或双胍的药学上可接受的盐，其中所述胆汁酸选自辰去氧胆酸、熊去氧胆酸、甘辰去氧胆酸和甘去氧胆酸。
• BILE ACIDS AND BIGUANIDES AS PROTEASE INHIBITORS FOR PRESERVING THE INTEGRITY OF PEPTIDES IN THE GUT
  申请人：Axcess Limited

  公开号：EP2361091B1

  公开（公告）日：2015-01-21
• Inhibitors Of Neurotrypsin
  申请人：Sonderegger Peter

  公开号：US20090170950A1

  公开（公告）日：2009-07-02

  The invention relates to a method for determining whether a compound is a neurotrypsin inhibitor, characterized in that the compound is incubated together with neurotrypsin, a variant thereof or a fragment comprising the protease domain and with a protein or peptide comprising agrin, a variant thereof or a fragment comprising the α- or the β-cleavage site of agrin, in an aqueous buffer solution, and the amount of cleavage of agrin is measured. Additionally, the invention relates to inhibitors of neurotrypsin found by this method, in particular to compounds of formula wherein Hal 1 and Hal 2 are fluorine, chlorine or bromine, and the use of such inhibitors for the treatment and/or prophylaxis of diseases caused by deficiency of synapses, for example skeletal muscle atrophy, schizophrenia, and cognitive disturbance.
• US4118481A
  申请人：——

  公开号：US4118481A

  公开（公告）日：1978-10-03