CAS: 26305-03-3; (6S,9S,12S,13S,17S,20S,21S)-13,21-Dihydroxy-12,20-Diisobutyl-6,9-Diisopropyl-2,17-Dimethyl-4,7,10,15,18-Pentaoxo-5,8,11,16,19-Pentaazatricosan-23-Oic Acid

该化合物是一种有效且有选择性的抑制分子,抑制了分泌蛋白,特别是累氨和,并源自于某些细菌物种的发酵* 链切切片*,其特点是独特的结构,包括一个带有特定序列的peptide脊柱,使其能有效地与目标酶的活跃地点捆绑在一起,从而抑制了它们的活动.该物质分子重量约为1,000达,并经常用于生物化学研究,研究蛋白解术过程和酶动能.Pepstatin A具有很高的特性和亲近性,使其在基本研究和应用研究中,包括在蛋白消化和调节研究中,都成为有价值的工具.其有效性通常以抑制单位量化,例如 " 120,000 U/m " 表示其能性.此外,必须谨慎地处理pepstatin A,因为它能够产生生物影响,并且需要适当的储存条件来保持其稳定性和活动.

结构式图片

欧盟法规

ECHA物质C&L通报REACH预注册

上下游产品

3-methylbutyric acid Fm°C-Val-OH N-[(9H-fluoren-9-ylmethoxy)carbonyl]-L-alanine (3S,4S)-(9-fluorenylmethoxycarbonyl)-4-amino-3-hydroxy-6-methylheptanoic acidN-(3-(2,3,4,6-tetra-O-acetyl-α-D-mannopyranosyloxy)propylcarbonyl)-N'-(pepstatinyl)propane-1,3-diamine N-(t-butyloxycarbonyl)-N'-(pepstatinyl)propane-1,3-diamine N-(pepstatinyl)propane-1,3-diamine

合成工艺路线路线简述

  • 合成目标产物 Pepstatin 主要起始原料 Isovaleric Acid And Fmoc-L-Valine And Fmoc-Ala-Oh And Fmoc-Sta-Oh
  • (文献来源)合成步骤主要原料 Isovaleric Acid 和 Fmoc-L-Valine 和 Fmoc-Ala-Oh 和 Fmoc-Sta-Oh
📜海藻糖,Pmsf Pepstatin,苯甲基磺酰氟置于碳,水体系中,化学反应 0.33H,以to Give Final Concentrations Of 10 μg Pepstatin/ml And 1 Mm Pmsf的收率获得胃酶抑素 A
参考文献:Increasing The Trehalose Content Of Organisms By Transforming Them With
标题:Increasing The Trehalose Content Of Organisms By Transforming Them With
摘要:已经分离和克隆了在酵母海藻糖合成酶中发现的两个不同多肽编码的核苷酸序列.从该酶中分离出并表征了第三个多肽,并提供了一种用于分离和克隆编码该多肽的核苷酸序列的方法.这些编码序列可以插入适当的载体中,并用于转化宿主细胞.转化后的细胞将产生比未转化的野生型细胞更多的海藻糖,并具有对各种压力的耐受性,特别是对水的可用性降低的耐受性增加.该发明可用于提高生物体的耐受性,增加食品的储存寿命,并在传统和安全的食品(例如面包酵母)中以工业规模经济地生产海藻糖.

专利信息


专利号:US-7169589-B2
优先权日:2000-07-28
标题 :Silicatein-mediated synthesis of amorphous silicates and siloxanes and use thereof
发明人:MUELLER WERNER E G; SCHROEDER HEINZ C; LORENZ BERND; KRASKO ANATOLI
权利人:MUELLER WERNER E G; SCHROEDER HEINZ C; LORENZ BERND; KRASKO ANATOLI
摘要:Silicatein is an enzyme of silicate-forming organisms used for the synthesis of their silicate scaffold. The present invention relates to the use of highly-expressed and highly active recombinant silicatein, silicatein isolated from natural sources after gene induction as well as silicatein-fusion proteins for the synthesis of amorphous silicon dioxide (silicic acids and silicates), siloxanes as well as modification of these compounds and their technical use.

专利号:WO-9517903-A1
优先权日:1993-12-28
标 题:Modular design and synthesis of oxazolone-derived molecules
发明人:HOGAN JOSEPH C JR; CASEBIER DAVID; FURTH PAUL; TU CHENG
权利人:ARQULE PARTNERS L P; HOGAN JOSEPH C JR; CASEBIER DAVID; FURTH PAUL; TU CHENG
摘要:The design and synthesis of novel oxazolone-derived molecular modules and the use of the modules in the construction of new molecules and fabricated materials is disclosed. The new molecules and fabricated materials are molecular recognition agents useful in the design and synthesis of drugs, and have applications in separations and materials science.

专利号:US-6451543-B1
优先权日:1998-08-31
标题:Lipid matrix-assisted chemical ligation and synthesis of membrane polypeptides
发明人:KOCHENDOERFER GERD G; HUNTER CHRISTIE L; KENT STEPHEN B H; BOTTI PAOLO
权利人:GRYPHON SCIENCES
摘要:The present invention relates to methods and compositions for lipid matrix-assisted chemical ligation and synthesis of membrane polypeptides that are incorporated in a lipid matrix. The invention is exemplified in production of a prefolded membrane polypeptide embedded within a lipid matrix via stepwise chemoselective chemical ligation of unprotected peptide segments, where at least one peptide segment is embedded in a lipid matrix. Any chemoselective reaction chemistry amenable for ligation of unprotected peptide segments can be employed. Suitable lipid matrices include liposomes, micelles, cell membrane patches and optically isotropic cubic lipidic phase matrices. Prefolded synthetic and semi-synthetic membrane polypeptides synthesized according to the methods and compositions of the invention also permit site-specific incorporation of one or more detectable moieties, such as a chromophore, which can be conveniently introduced during synthesis. The methods and compositions of the invention have multiple uses. For example, they can be used to assay ligand binding to membrane polypeptides and domains comprising a receptor, and thus are extremely useful for structure/function studies, drug screening/selection/design, and diagnostics and the like, including high-throughput applications. The methods and compositions of the invention are particularly suited for FRET analyses of previously inaccessible membrane polypeptides.

专利号:US-7659391-B2
优先权日:2001-11-05
标 题:Method for the in vitro synthesis of short double stranded RNAs
发明人:DE BACKER MARIANNE DENISE; HARRIS ADAM N
权利人:JANSSEN PHARMACEUTICA NV
摘要:The present invention relates to the field of synthesis of short double-stranded RNAs. An in vitro transcription method using bacteriophage polymerases and target sequence-specific single-stranded DNA oligonucleotides as templates is disclosed. The present invention finds particularly advantageous use in the synthesis of short interfering RNAs (siRNAs) that have been shown to function as key intermediates in triggering sequence-specific RNA degradation during posttranscriptional gene silencing in plants and RNA interference in invertebrates and vertebrate systems.

专利号:WO-9720061-A1
优先权日:1995-11-30
标题:Synthesis of hyaluronic acid
发明人:WONG CHI-HUEY; DELUCA CLAUDIO
权利人:SCRIPPS RESEARCH INST; WONG CHI HUEY; DELUCA CLAUDIO
摘要:A preparative enzymatic synthesis of hyaluronic acid (HA) from UDP-N-acetyl-D-glucosamine (UDP-GlcNAc) and UDP-glucuronic acid (UDP-GlcA) catalyzed by hyaluronic acid synthase is coupled with regeneration of the sugar nucleotides. Polymerizing UDP-GlcA and UDP-GlcNAc to form hyaluronic acid results in the formation of released UDP. The released UDP is, in turn, employed in the regeneration of UDP-GlcA and UDP-GlcNAc. Use of the released UDP for regenerating UDP-GlcA and UDP-GlcNAc prevents a build-up of these compounds and prevents or reduces feed back inhibition of the hyaluronic acid synthase reaction that would otherwise be caused by such build-up. Accordingly, the product yield is enhanced by the recycling of these compounds.

专利号:US-2002022022-A1
优先权日:2000-05-19
标题 :Inhibition of cell proliferation and matrix synthesis by antioxidants and NAD(P)H oxidase inhibitors
发明人:SHI YI; ZALEWSKI ANDREW
摘要:The present invention is directed to a method for the prophylactic and therapeutic treatment of diseases or disorders associated with the abnormal proliferation and extracellular matrix synthesis of smooth muscle cells (SMC) and fibroblasts due to activation of NAD(P)H and/or increased ROS generation. The method involves the administration of an NAD(P)H oxidase inhibitor(s) and/or antioxidant(s) to a mammal in an amount sufficient to treat the disease or disorder prophylactically or therapeutically. The NAD(P)H oxidase inhibitor inhibits the synthesis or translocation of NAD(P)H subunits, thereby blocking the generation of intracellular reactive oxygen species (ROS) and thus the proliferation and extracellular matrix synthesis of SMC and fibroblasts. Similarly, the administration of antioxidants blocks the generation of intracellular ROS, thereby inhibiting SMC and fibroblast proliferation and extracellular matrix synthesis. In addition to the prevention and treatment of vascular disease, such as atherosclerosis, graft disease, and restenosis, NAD(P)H oxidase inhibitors and antioxidants may be useful for the prevention and treatment of other conditions by decreasing cell proliferation and extracellular matrix synthesis associated therewith. These conditions include arthritis, keloid formation, cancer, tissue and organ fibrosis, and complications related to organ transplantation, metabolic syndrome, and radiation therapy.

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品牌试剂参考报价(招募中)

📌 第三方产品分析报告

✅ COA系统入驻 | 共享模式

主要参考文献


1: Du C, Wang J, Liu X, Li H, Geng D, Yu L, Chen Y, Zhang J. Construction of Pepstatin A-Conjugated ultrasmall SPIONs for targeted positive MR imaging of epilepsy-overexpressed P-glycoprotein. Biomaterials. 2020 Feb;230:119581. doi: 10.1016/j.biomaterials.2019.119581. Epub 2019 Oct 31.
139:199-212. doi: 10.1016/j.ijbiomac.2019.07.133. Epub 2019 Jul 30. 24(2):332. doi: 10.3390/molecules24020332.
4: Arodola OA, Soliman ME. Hybrid 2D/3D-quantitative structure-activity relationship and modeling studies perspectives of pepstatin A analogs as cathepsin D inhibitors. Future Med Chem. 2018 Jan;10(1):5-26. doi: 10.4155/fmc-2017-0077. Epub 2017 Dec 13.

合成参考文献


参考文献:10.1007/s00395-010-0089-0
摘要:Carneiro-Ramos MS, Diniz GP, Nadu AP, Almeida J, Vieira RLP, Santos RAS, Barreto-Chaves MLM. Blockage of Angiotensin II type 2 receptor prevents thyroxine-mediated cardiac hypertrophy by blocking Akt activation. Basic Research in Cardiology. 2010 Feb 14;105(3):325–35. doi: 10.1007/s00395-010-0089-0.
参考文献:10.1186/1476-4598-9-38
摘要:Lynch JT, Rajendran R, Xenaki G, Berrou I, Demonacos C, Krstic-Demonacos M. The role of glucocorticoid receptor phosphorylation in Mcl-1 and NOXA gene expression. Molecular Cancer. 2010 Feb 15;9(1):38. doi: 10.1186/1476-4598-9-38.
参考文献:10.1186/1757-2215-3-1
摘要:Lane D, Matte I, Rancourt C, Piché A. The prosurvival activity of ascites against TRAIL is associated with a shorter disease-free interval in patients with ovarian cancer. Journal of Ovarian Research. 2010 Jan 18;3(1):1. doi: 10.1186/1757-2215-3-1.
参考文献:10.3390/md9060967
摘要:Addad S, Exposito JY, Faye C, Ricard-Blum S, Lethias C. Isolation, characterization and biological evaluation of jellyfish collagen for use in biomedical applications. Mar Drugs. 2011;9(6):967–83.
参考文献:10.1371/journal.pone.0021908
摘要:Follo C, Ozzano M, Mugoni V, Castino R, Santoro M, Isidoro C. Knock-Down of Cathepsin D Affects the Retinal Pigment Epithelium, Impairs Swim-Bladder Ontogenesis and Causes Premature Death in Zebrafish. PLoS ONE. 2011 Jul 01;6(7):e21908. doi: 10.1371/journal.pone.0021908.
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