CAS: 1510-21-0; Cholesteryl Hemisuccinate

该化合物是胆固醇的衍生物,其特点是有附于胆固醇脊柱的肝脏组,该化合物通常用于生化和制药应用,特别是在药物运载系统中,并作为脂质配方的一个成分,它具有两栖特性,即具有水利(抽水)和水排(排水)特性,因此有助于形成脂肪双层和小鼠.胆固醇可以提高疏水药物的溶性,便利其跨生物膜的运输.此外,众所周知,该化合物能够与各种生物分子形成稳定的复合体,有助于定向药物的交付.该化合物通常被认为具有生物兼容性,适合用于医药应用.其结构特征有助于其在改变聚膜特性和影响细胞相互作用方面的作用,这对于新治疗战略的发展至关重要.

结构式图片

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CAS号108-30-5 丁二酸酐 | CAS号57-88-5 胆固醇 | CAS号543-20-4 丁二酰氯 | CAS号2387-23-7 N,N’-二环己基脲

合成工艺路线路线简述

  • 合成目标产物 Cholesteryl Hemisuccinate 主要起始原料 Succinic Anhydride And Cholesterol
  • (文献来源)合成步骤主要原料 Succinic Anhydride 和 Cholesterol
5-Cholesten-3β-Yl 2-(Trimethylsilyl)Ethyl Butanedioate置于四丁基氟化铵体系中,用 四氢呋喃 用作溶剂,以81%的收率获得胆固醇琥珀酸单酯
参考文献:Pouzar,Vladimir; Drasar,Pavel; Cerny,Ivan,Synthetic Communications,1984,Vol. 14,# 6,P. 501-507
标题:Pouzar,Vladimir; Drasar,Pavel; Cerny,Ivan,Synthetic Communications,1984,Vol. 14,# 6,P. 501-507

海关参考信息

专利信息


专利号:US-2008300418-A1
优先权日:2004-11-08
标 题:Synthesis of Cardiolipin Analogues and Uses Thereof
发明人:AHMAD MOGHIS U; UKKALAM MURALI K; ALI SHOUKATH M; AHMAD IMRAN
权利人:AHMAD MOGHIS U; UKKALAM MURALI K; ALI SHOUKATH M; AHMAD IMRAN
摘要:The invention provides novel synthetic methodologies for preparing cardiolipin, migrated caridiolipin (1,2-positional isomer of cardiolipin) and their analogues having varying fatty acids and/or alkyl chains with varying length and degrees of saturation/unsaturation. The method comprises (a) reacting an optically pure 1,2-O-dialkyl-sn-glycerol or 1,2-O-dialkyl-sn-glycerol with one or more phosphoramidite reagent(s), wherein a phosphite triester is produced; (b) coupling the product of (a) with glycerol, wherein a protected cardiolipin is produced; and (c) deprotecting the protected cardiolipin, such that cardiolipin is prepared. The cardiolipins and analogues thereof, prepared by the present methods, can be incorporated into liposomes, which can also include active agents such as hydrophobic or hydrophilic drugs, antisense nucleotides or diagnostic agents. Such liposomes can be used to treat diseases or can be used in diagnostic and/or analytical assays.

专利号:US-2004110228-A1
优先权日:2002-04-01
标 题:Combinatorial organic synthesis of unique biologically active compounds
发明人:MCALPINE SHELLI R; TAYLOR RACHEL E; BOLLA MEGAN L; SEGALL ANCA M
摘要:The invention provides a method for making a combinatorial library of cyclic compounds, such as Holliday junction-trapping compounds, comprising the steps of (a) obtaining a plurality of trimers according to the generic structure X 1- X 2- X 3 , wherein X 1 , X 2 and X 3 can be independently any naturally or nonnaturally occurring amino acids or peptidomimetics thereof; (b) optionally coupling a spacer S to the trimer at either end; (c) cyclizing two trimers or trimer-spacer conjugates in a head-to-tail orientation; thereby obtaining a combinatorial library of compounds, wherein the library does not include an unmodifed or naturally occurring Holliday Junction-trapping compounds. The invention additionally provides methods macrocyclic compounds that are synergimycin derivatives.

专利号:US-2024325572-A1
优先权日:2021-07-15
标 题 :N-heterocyclyl substituted 2-cyano-3-(naphthalen-2-yl)acrylamide derivatives as fluorophors for detection of amyloid and amyloid-like proteins for diagnosis of neurodegenerative disorders
发明人:SARRAF STELLA T
权利人:AMYDIS INC
摘要:Provided herein is the design and synthesis of novel molecular rotor fluorophores of formula I useful for detection of amyloid or amyloid like proteins. The fluorophores are designed to exhibit enhanced fluorescence emission upon associating with amyloid or amyloid like proteins as compared to unbound compound. Also disclosed herein are the compounds for use in methods for diagnosis and treatment of diseases associated with an amyloid or amyloid like proteins, such as e.g. Alzheimer's disease or traumatic brain injury (TBI), Parkinson's disease, vascular dementia, amyotrophic lateral sclerosis, Down syndrome, traumatic brain injury, chronic traumatic encephalopathy, schizophrenia or depression. Exemplary compounds are e.g. N-heterocyclyl substituted 2-cyano-3-(naphthalen-2-yl)acrylamide derivatives, such as e.g. (E)-2-cyano-N-(2-(2-hydroxy)ethoxy)ethyl)-3-(6-(pyrrolidin-1-yl)naphthalen-2-yl) acrylamide (example 1): Experimental data on in-vitro binding studies with amyloid beta is provided.

专利号:WO-9925385-A1
优先权日:1997-11-17
标 题:A method of increasing nucleic acid synthesis with ultrasound
发明人:UNGER EVAN C; MCCREERY THOMAS; SADEWASSER DAVID
权利人:IMARX PHARMACEUTICAL CORP
摘要:The present invention is directed to a method of increasing nucleic acid synthesis in a cell comprising administering to the cell a therapeutically effective amount of ultrasound for a therapeutically effective time such that said administration of said ultrasound results in said increased nucleic acid synthesis. The nucleic acid sequence may comprise an endogenous sequence or an exogenous sequence.

专利号:US-2024299311-A1
优先权日:2022-04-05
标题 :Ionizable cationic lipids and lipid nanoparticles
发明人:KARMALI PRIYA PRAKASH; TANIS STEVEN
权利人:KARMALI PRIYA PRAKASH; TANIS STEVEN; CAPSTAN THERAPEUTICS INC
摘要:Ionizable cationic lipids, methods for synthesizing them, as well as intermediates useful in synthesis of these lipids and methods of synthesizing the intermediates are disclosed. The ionizable cationic lipids are useful as a component of lipid nanoparticles (LNP), which in turn can be used for the delivery of nucleic acids into cells in vivo or ex vivo. LNP compositions are also disclosed, including LNP comprising a functionalized lipid to enable conjugation of a binding moiety, and targeted LNP (tLNP), that is a LNP in which a binding moiety has been conjugated to the functionalized lipid and can serve as a targeting moiety to direct the tLNP to a desired tissue or cell type.

专利号:US-2008051323-A1
优先权日:2004-08-21
标 题 :Chloroquine drug compositions and methods for their synthesis
发明人:KOSAK KENNETH M
权利人:KOSAK KENNETH M
摘要:This invention discloses compositions of chloroquine-coupled active agents, including methods for their preparation. The prior art has shown that chloroquines given as free drug in high enough concentration, enhances the release of various agents from cellular endosomes into the cytoplasm. The purpose of these compositions is to provide a controlled amount of chloroquine at the same site where the active agent is delivered, thereby reducing the overall dosage needed. n The compositions comprise a chloroquine substance coupled to an active agent directly or through a variety of pharmaceutical carrier substances. The carrier substances include polysaccharides, synthetic polymers, proteins, micelles and other substances for carrying and releasing the chloroquine compositions in the body for therapeutic effect. The compositions can also include a biocleavable linkage for carrying and releasing active agents for therapeutic or other medical uses. The invention also discloses carrier compositions that are coupled to targeting molecules for targeting the delivery of chloroquine substances and active agents to their site of action.
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主要参考文献

[Slepushkin VA, Simoes S, Dazin P, Newman MS, Guo LS, Pedroso de Lima MC, et al. Sterically stabilized pH-sensitive liposomes. Intracellular delivery of aqueous contents and prolonged circulation in vivo J Biol Chem. 1997;272(4):2382–8, doi: 10.1074/jbc.272.4.2382]

合成参考文献


摘要:S109 | PARCEDC | List of 7074 potential endocrine disrupting compounds (EDCs) by PARC T4.2 | DOI:10.5281/zenodo.10944198
参考文献:10.1101/280503|10.2210/pdb6g1k/pdb|10.7554/elife.36615|10.7554/elife.36615.029
摘要:Vinayagam D, Mager T, Apelbaum A, Bothe A, Merino F, Hofnagel O, Gatsogiannis C, Raunser S. Author response: Electron cryo-microscopy structure of the canonical TRPC4 ion channel. 2018 Apr 30;(). doi: 10.7554/elife.36615.029.
参考文献:10.1038/s41586-018-0081-7
摘要:Walsh RM, Roh SH, Gharpure A, Morales-Perez CL, Teng J, Hibbs RE. Structural principles of distinct assemblies of the human α4β2 nicotinic receptor. Nature. 2018 May;557(7704):261–5.
参考文献:10.1248/bpb.b19-00259
摘要:Ibaraki H, Kanazawa T, Kurano T, Oogi C, Takashima Y, Seta Y. Anti-RelA siRNA-Encapsulated Flexible Liposome with Tight Junction-Opening Peptide as a Non-invasive Topical Therapeutic for Atopic Dermatitis. Biological & Pharmaceutical Bulletin. 2019 Jul 01;42(7):1216–25. doi: 10.1248/bpb.b19-00259.
参考文献:10.1126/science.abb8008
摘要:Kumar A, Planchais C, Fronzes R, Mouquet H, Reyes N. Binding mechanisms of therapeutic antibodies to human CD20. Science. 2020 Aug 14;369(6505):793–9. doi: 10.1126/science.abb8008.
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