CAS: 24386-93-4; (2R,3R,4S,5R)-2-(4-Amino-5-Iodo-7H-Pyrrolo[2,3-D]Pyrimidin-7-yl)-5-(Hydroxymethyl)Tetrahydrofuran-3,4-Diol

该化合物是一种强效和选择性的腺素活性抑制剂,广泛用于生物化学和药理研究,其主要优势在于能够有效阻塞腺活性,导致细胞内腺素水平的提高,这对研究肾上腺素中导信号路径很有价值.该化合物具有很高的特性,最大限度地减少目标外影响,并经常用于调查炎症,缺血症和...

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166247-63-8 908130-61-0 69-33-0

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上下游产品

4-chloro-5-iodo-7-(α-D-ribofuranosyl)-7H-pyrrolo[2,3-d]pyrimidine 4-chloro-5-iodo-7-[(2,3,5-tri-O-benzoyl)-β-D-ribofuranosyl]-7H-pyrrolo[2,3-d]pyrimidine 4-amino-5-phenyl-7-(β-D-ribofuranosyl)-7H-pyrrolo[2,3-d]pyrimidine 4-amino-5-(4-methoxyphenyl)-7-(β-D-ribofuranosyl)-7H-pyrrolo[2,3-d]pyrimidine 4-amino-5-[4-(methylthio)phenyl]-7-(β-D-ribofuranosyl)-7H-pyrrolo[2,3-d]pyrimidine

合成工艺路线路线简述

  • 合成目标产物 5-Iodotubercidin 主要起始原料 4-Chloro-7H-Pyrrolo[2,3-D]Pyrimidine
  • (文献来源)合成步骤主要原料 4-Chloro-7H-Pyrrolo[2,3-D]Pyrimidine
📜4-氯-5-碘-7H-吡咯并[2,3-D]嘧啶置于氨,Sodium Hydride体系中,用 甲醇,乙腈 用作溶剂,化学反应 16.83H,反应生成5-碘代杀结核菌素
参考文献:腺苷激酶抑制剂.1. 5-碘代结核菌素类似物的合成,酶抑制和抗癫痫活性.
标题:腺苷激酶抑制剂.1. 5-碘代结核菌素类似物的合成,酶抑制和抗癫痫活性.
摘要:腺苷受体激动剂产生多种治疗上有用的药理学.然而,迄今为止,由于剂量限制的副作用,它们未能成功进行临床开发.腺苷激酶抑制剂(akis)代表了另一种策略,因为akis可以以更多位点和事件特异性的方式提高局部腺苷水平,从而以更大的治疗窗口引发所需的药理作用.从5-碘代小球蛋白(ic50 = 0.026 Microm)和5'-氨基-5'-脱氧腺苷(ic50 = 0.17 Microm)作为分离的人ak的主要抑制剂开始,各种吡咯并[2,3-D]嘧啶核苷类似物通过使用钠盐介导的糖基化方法将5-取代的4-取代的4-氯吡咯并[2,3-D]嘧啶碱基与核糖类似物偶联来设计和制备.5'-氨基-5' 发现5-溴和5-碘结核菌素的β-脱氧类似物是迄今为止报道的最有效的aki(ic50S <0.001 Microm).在大鼠最大电击(mes)诱发的癫痫发作试验中,几种有效的akis表现出抗惊厥活性.
Doi:10.1021/jm000024G

海关参考信息

专利信息


专利号:US-8026349-B2
优先权日:2004-08-20
标题 :Polynucleotide synthesis labeling chemistry
发明人:HARTSEL STEPHANIE A; KAISER ROBERT J; DELANEY MICHAEL O
权利人:DHARMACON INC
摘要:Methods and compositions for making nucleoside phosphoramidites and nucleic acids, including mono-, di-, and polynucleotides, comprising a linker covalently attached to a levulinyl moiety are provided. A levulinyl-protected linking moiety affords an orthogonal approach to modifying a polynucleotide during or after solid phase synthesis with a molecule of interest, for example, a conjugate or a dye.

专利号:US-9114159-B2
优先权日:2005-08-17
标 题 :Transcription factors in neuronal dendrites-dendritic protein synthesis and cell death
发明人:EBERWINE JAMES H; BARRETT LINDY E
权利人:EBERWINE JAMES H; BARRETT LINDY E; UNIV PENNSYLVANIA
摘要:The present invention relates to methods of altering the competence of a dendrite and/or the viability of a neuron by modulating the level of Elk-1 in a dendrite. The present invention also provides methods of altering the ATP levels in a neuron, methods of isolating at least one protein of a mitochondrial permeability transition pore complex, methods of introducing an RNA into a neuron, methods of translating an RNA in a dendrite, methods of monitoring risk of neurodegeneration of a neuron, and methods of treatment for neurodegenerative diseases.

专利号:WO-2024097977-A1
优先权日:2022-11-04
标题:Silk nanoparticle synthesis: tuning size, dispersity, and surface chemistry for drug delivery
发明人:SHAIDANI SAWNAZ; FALCUCCI THOMAS; FOSTER OLIVIA; SAHOO JUGAL KISHORE; HASTURK ONUR; KAPLAN DAVID L; JACOBUS CHARLOTTE S
权利人:TUFTS COLLEGE
摘要:Methods disclosed herein relate to generating silk nanoparticles with a low polydispersity index (PDI). Methods include adding a silk solution dropwise into a volatile solvent that is miscible with water, thereby forming a precipitate-bearing solution and applying shear forces to the precipitate-bearing solution for a length of time sufficient to achieve evaporation of at least 95% of the volatile solvent, thereby producing a population of silk fibroin nanoparticles in water having a polydispersity index (PDI) of 0.35 or less, including but not limited to, a PDI of 0.330 or less, 0.325 or less, 0.315 or less, 0.310 or less, 0.30 or less, 0.275 or less, 0.250 or less, 0.225 or less, or 0.200 or less. Parameters related to silk fibroin molecular weight, silk fibroin concentration, shear force application, and temperature may all be modified to achieve silk nanoparticles of a particular size exhibiting particular PDIs.

专利号:EP-1578931-A4
优先权日:2002-07-16
标 题:METHODS FOR IDENTIFYING COMPOUNDS THAT MODULATE THE SYNTHESIS OF IL-4 RECEPTOR-MEDIATED IGE USING ADENOSINE KINASE

专利号:US-2004096436-A1
优先权日:2002-08-02
标 题:Methods for inhibiting protein kinases in cancer cells
发明人:CARSON DENNIS A; ROSENBACH MICHAEL D; CARRERA CARLOS J; LEONI LORENZO M
权利人:UNIV CALIFORNIA; SALMEDIX INC
摘要:The present invention provides methods of treating cancer using inhibitors of protein kinases. The inhibitors of protein kinases are combined with agents that inhibit a cellular ATP synthetic pathway. Inhibitors of ATP synthesis include inhibitors of de novo purine biosynthesis, inhibitors of the salvage pathway of ATP biosynthesis, and inhibitors of the enzyme inosine monophosphate dehydrogenase.

专利号:WO-2004007680-A2
优先权日:2002-07-16
标题:Methods of identifying compounds that modulate il-4 receptor-mediated ige synthesis utilizing an adenosine kinase

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合成参考文献


参考文献:10.1124/mol.119.115964
摘要:Lee TD, Lee OW, Brimacombe KR, Chen L, Guha R, Lusvarghi S, Tebase BG, Klumpp-Thomas C, Robey RW, Ambudkar SV, Shen M, Gottesman MM, Hall MD. A High-Throughput Screen of a Library of Therapeutics Identifies Cytotoxic Substrates of P-glycoprotein. Molecular Pharmacology. 2019 Nov;96(5):629–40. doi: 10.1124/mol.119.115964.
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