CAS: 866405-64-3; 6-(4-(2-(Piperidin-1-yl)Ethoxy)Phenyl)-3-(Pyridin-4-yl)Pyrazolo[1,5-A]Pyrimidine

该化合物是一个小分子抑制剂,主要以其在研究AMP活性蛋白质动脉(AMPK)途径中的作用而闻名,其特点是有能力有选择地抑制AMPK的活动,AMPK是细胞能量固态的关键调节器.多索摩地因已证明影响各种生物过程,包括新陈代谢,细胞生长和区别.该化合物经常用于研究,以探讨其对代谢性疾病,癌症和其他与能源管制有关的条件的影响.从结构上讲,多斯摩地貌特征是有助于其生物活动的功能组的独特安排,通常在实验室环境中为实验目的管理,其影响在各种细胞类型和动物模型中研究.与许多研究化学品一样,多斯摩地文的安全特征和潜在治疗应用继续受到调查,突出其在生物化学和药理学领域的重要性.

结构式图片

物理性质

MSDS等安全信息

欧盟法规

ECHA物质C&L通报

上下游产品

3-(吡啶-4-基)-6-(4-甲氧基苯基)-吡唑并(1,5-A)嘧啶 6-(4-Methoxyphenyl)-3-(Pyridin-4-yl)Pyrazolo[1,5-A]Pyrimidine 216661-58-4
4-[3-(吡啶-4-基)吡唑并[1,5-A]嘧啶-6-基]苯酚 6-(4-Hydroxyphenyl)-3-(Pyridin-4-yl)Pyrazolo[1,5-A]Pyrimidine 515880-87-2

合成工艺路线路线简述

  • 71597-85-8 + 705263-10-1 = 866405-64-3
    反应条件:1.1 Reagents: Sodium Carbonate Catalysts: Tetrakis(Triphenylphosphine)Palladium Solvents: 1,4-Dioxane,Water; Rt; 40 Min,110 °C2.1 Reagents: N-Bromosuccinimide Solvents: Dichloromethane; 0 °C; 2 H,Rt3.1 Reagents: Cesium Carbonate Catalysts: Sodium Iodide Solvents: Dimethylformamide; 18 H,65 °C4.1 Reagents: Sodium Carbonate Catalysts: Dichlorobis(Triphenylphosphine)Palladium Solvents: 1,4-Dioxane,Water; Rt; 40 Min,110 °C
    标题:Ampk Inhibitor Bml-275 Induces Neuroprotection Through Decreasing Cyt C And Aif Expression After Transient Brain Ischemia
    作者:Hu,Yue; Et Al
    参考文献:Bioorganic & Medicinal Chemistry 日期:2021 卷标:52]

    1820-80-0 + 2065-75-0 = 866405-64-3
    反应条件:1.1 Reagents: Acetic Acid Solvents: Ethanol; 6 H,Reflux2.1 Reagents: Sodium Carbonate Catalysts: Tetrakis(Triphenylphosphine)Palladium Solvents: 1,4-Dioxane,Water; Rt; 40 Min,110 °C3.1 Reagents: N-Bromosuccinimide Solvents: Dichloromethane; 0 °C; 2 H,Rt4.1 Reagents: Cesium Carbonate Catalysts: Sodium Iodide Solvents: Dimethylformamide; 18 H,65 °C5.1 Reagents: Sodium Carbonate Catalysts: Dichlorobis(Triphenylphosphine)Palladium Solvents: 1,4-Dioxane,Water; Rt; 40 Min,110 °C
    标题:Ampk Inhibitor Bml-275 Induces Neuroprotection Through Decreasing Cyt C And Aif Expression After Transient Brain Ischemia
    作者:Hu,Yue; Et Al
    参考文献:Bioorganic & Medicinal Chemistry 日期:2021 卷标:52]

    1692-15-5 + 945376-96-5 = 866405-64-3
    反应条件:1.1 Reagents: Sodium Carbonate Catalysts: Dichlorobis(Triphenylphosphine)Palladium Solvents: 1,4-Dioxane,Water; Rt; 40 Min,110 °C
    标题:Ampk Inhibitor Bml-275 Induces Neuroprotection Through Decreasing Cyt C And Aif Expression After Transient Brain Ischemia
    作者:Hu,Yue; Et Al
    参考文献:Bioorganic & Medicinal Chemistry 日期:2021 卷标:52]

    1932-03-2 + 945376-95-4 = 866405-64-3
    反应条件:1.1 Reagents: Cesium Carbonate Catalysts: Sodium Iodide Solvents: Dimethylformamide; 18 H,65 °C2.1 Reagents: Sodium Carbonate Catalysts: Dichlorobis(Triphenylphosphine)Palladium Solvents: 1,4-Dioxane,Water; Rt; 40 Min,110 °C
    标题:Ampk Inhibitor Bml-275 Induces Neuroprotection Through Decreasing Cyt C And Aif Expression After Transient Brain Ischemia
    作者:Hu,Yue; Et Al
    参考文献:Bioorganic & Medicinal Chemistry 日期:2021 卷标:52]

    1629758-13-9 = 866405-64-3
    反应条件:1.1 Reagents: N-Bromosuccinimide Solvents: Dichloromethane; 0 °C; 2 H,Rt2.1 Reagents: Cesium Carbonate Catalysts: Sodium Iodide Solvents: Dimethylformamide; 18 H,65 °C3.1 Reagents: Sodium Carbonate Catalysts: Dichlorobis(Triphenylphosphine)Palladium Solvents: 1,4-Dioxane,Water; Rt; 40 Min,110 °C
    标题:Ampk Inhibitor Bml-275 Induces Neuroprotection Through Decreasing Cyt C And Aif Expression After Transient Brain Ischemia
    作者:Hu,Yue; Et Al
    参考文献:Bioorganic & Medicinal Chemistry 日期:2021 卷标:52
📜4-氯甲基吡啶置于盐酸肼,Hydrazine Hydrate,氢溴酸,Sodium Hydride,溶剂黄146体系中,用 N-甲基吡咯烷酮,乙醇,水,N,N-二甲基甲酰胺,Mineral Oil 作为反应溶剂,化学反应 19.17H,反应生成 6-[4-(2-哌啶-1-基乙氧基)苯基]-3-吡啶-4-基吡唑并[1,5-A]嘧啶
参考文献:一种热休克因子1的抑制剂,其制备方法和应用
标题:一种热休克因子1的抑制剂,其制备方法和应用
摘要:本发明提供了一种热休克因子1(Hsf1)抑制剂及其应用.具体地,本发明提供了一种式i化合物或其药学上可接受的盐,所述化合物具有优异的抑制hsf1活性和抗肿瘤的效果.本发明还提供了含有所述化合物的药物组合物以及其在抑制hsf1方面的应用.

海关参考信息

专利信息


专利号:US-2023096053-A1
优先权日:2019-12-06
标 题:Genetically-targeted chemical assembly: building functional structures and materials in living cells, tissues, and animals
发明人：DEISSEROTH KARL A; BAO ZHENAN; LIU JIA; RAMAKRISHNAN CHARU; KIM YOON SEOK; TOM ARIANE C
权利人:UNIV LELAND STANFORD JUNIOR
摘要:Compositions and methods are provided for genetically modifying cells to guide in situ chemical synthesis of electroactive, conductive, or insulating polymers on plasma membranes, organelle membranes, or subcellular surfaces of cells. In particular, compositions and methods are provided for genetically modifying excitable cells such as neurons, muscle cells, and endocrine cells to guide in situ chemical synthesis of polymers on the extracellular side of the plasma membrane. The subject methods can be used in various applications, for example, to assemble polymers in vivo at targeted locations to modulate electrical conduction and create new electrical conduction pathways, allow cell-type-specific neuromodulation, provide a conductive structure on cells for connection to electrodes, sensors, or other external electronic and electrochemical devices, and create a durable structure to replace damaged tissue for use in regenerative medicine.

专利号:US-11617804-B2
优先权日:2014-07-18
标题:Hyaluronic acid-based nanoparticles as biosensors for imaging-guided surgery and drug delivery vehicles and methods associated therewith
发明人：MOHS AARON MICHAEL; HILL TANNER KINKADE; KELKAR SNEHA SANJAY; KRIDEL STEVE
权利人:UNIV WAKE FOREST
摘要:The present invention relates to intraoperative fluorescent imaging (IFI) used both pre-clinically using in-vivo models, as well as clinically to map sentinel lymph nodes in breast cancer, skin cancer, GI cancer, lung cancer, prostate cancer and several other cancers. IFI can be used to image solid tumors both non-specifically in hepatobiliary and breast cancers as well as in prostate and ovarian cancer. In one embodiment, two-dimensional resolution to 10 μm 2 is possible with optical imaging, significantly higher than other imaging modalities. n In one embodiment, the present invention relates to a series of self-assembled nanoparticles using HLA (hyaluronic acid) as both a polymeric backbone as well as targeting ligand. In some embodiments, the present invention relates to the synthesis of HLA conjugates, and the effect of variation of the hydrophobic ligand structure and conjugation level on nanoparticle self-assembly, size, ICG loading efficiency, and ICG fluorescence quenching and reactivation.

专利号:CN-112870358-A
优先权日:2019-11-29
标 题:Use of deubiquitinase USP20 in reducing cholesterol synthesis and improving metabolic syndrome

专利号:CN-112870358-B
优先权日:2019-11-29
标 题:Use of deubiquitinase USP20 for reducing cholesterol synthesis and improving metabolic syndrome

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主要参考文献


1: Valizadeh-Arshad Z, Shahbazi E, Hashemizadeh S, Moradmand A, Jangkhah M, Kiani S. In Vitro Differentiation of Neural-Like Cells from Human Embryonic Stem Cells by A Combination of Dorsomorphin, XAV939, and A8301. Cell J. 2018 Jan;19(4):545-551. doi: 10.22074/cellj.2018.4232. Epub 2017 Nov 4.
2: Łabuzek K, Liber S, Gabryel B, Bułdak Ł, Okopień B. Erratum to: Ambivalent effects of compound C (dorsomorphin) on inflammatory response in LPS-stimulated rat primary microglial cultures. Naunyn Schmiedebergs Arch Pharmacol. 2017 Mar;390(3):327-328. doi: 10.1007/s00210-017-1348-5. doi: 10.1016/j.jvs.2016.03.462. Epub 2016 Jun 30.
4: Madhu V, Dighe AS, Cui Q, Deal DN. Dual Inhibition of Activin/Nodal/TGF-β and BMP Signaling Pathways by SB431542 and Dorsomorphin Induces Neuronal Differentiation of Human Adipose Derived Stem Cells. Stem Cells Int. 2016;2016:1035374. doi: 10.1155/2016/1035374. Epub 2015 Dec 20.

合成参考文献


参考文献:10.1016/j.ejphar.2011.06.042
摘要:Thandapilly SJ, Louis XL, Yang T, Stringer DM, Yu L, Zhang S, Wigle J, Kardami E, Zahradka P, Taylor C, Anderson HD, Netticadan T. Resveratrol prevents norepinephrine induced hypertrophy in adult rat cardiomyocytes, by activating NO-AMPK pathway. Eur J Pharmacol. 2011 Oct 01;668(1-2):217–24. doi: 10.1016/j.ejphar.2011.06.042.
参考文献:10.1016/j.atherosclerosis.2011.06.043
摘要:Kim YM, Kim MY, Kim HJ, Roh GS, Ko GH, Seo HG, Lee JH, Chang KC. Compound C independent of AMPK inhibits ICAM-1 and VCAM-1 expression in inflammatory stimulants-activated endothelial cells in vitro and in vivo. Atherosclerosis. 2011 Nov;219(1):57–64. doi: 10.1016/j.atherosclerosis.2011.06.043.
参考文献:10.1016/j.taap.2011.06.024
摘要:Son Y, Wang X, Hitron JA, Zhang Z, Cheng S, Budhraja A, Ding S, Lee J, Shi X. Cadmium induces autophagy through ROS-dependent activation of the LKB1–AMPK signaling in skin epidermal cells. Toxicology and Applied Pharmacology. 2011 Sep;255(3):287–96. doi: 10.1016/j.taap.2011.06.024.
参考文献:10.1159/000328516
摘要:Wu Y, Li X, Zhu JX, Xie W, Le W, Fan Z, Jankovic J, Pan T. Resveratrol-activated AMPK/SIRT1/autophagy in cellular models of Parkinson's disease. Neurosignals. 2011;19(3):163–74.
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