CAS: 186139-09-3; Trodusquemine
该化合物是一种合成化合物,在生物化学和药理领域引起了人们的兴趣,主要被承认为具有选择性地抑制蛋白磷酶2A(PP2A)的作用,这是一种酶,在包括细胞生长和分裂在内的各种细胞过程中发挥着关键作用.通过Trodusquemine抑制PP2A,可能会对癌症研究产生影响,因为它可能会影响肿瘤的生长和扩散.该化合物展示了一种复杂的分子结构,有助于其生物活动.已经研究过Trodusquemine对代谢途径及其潜在治疗应用的影响,特别是在肥胖和新陈代谢紊乱的情况下.此外,其致癌特性,如吸收,分布,代谢和排泄,对于了解其功效和安全特征至关重要.
- 英文名称Trodusquemine
- 中文名称(3R,6R)-6-((3S,5R,7R,8R,9S,10S,13R,14S,17R)-3-((3-((4-((3-氨基丙基)氨基)丁基)氨基)丙基)氨基)-7-羟基-10,13-二甲基己十氢化-1H-H[A]菲-17-基)-2-甲基庚烷-3-基基硫酸盐
- IUPAC名称(3R,6R)-6-((3S,5R,7R,8R,9S,10S,13R,14S,17R)-3-((3-((4-((3-aminopropyl)amino)butyl)amino)propyl)amino)-7-hydroxy-10,13-dimethylhexadecahydro-1H-cyclopenta[a]phenanthren-17-yl)-2-methylheptan-3-yl hydrogen sulfate
- CAS编号186139-09-3
- FDA UNII编号:KKC12PIF16
- 分子式:C37H72N4O5S分子量:685.0564
- 产品CID: 2533942
- 同类组份化合物CAS186139-09-3 (free base)1309370-85-1 (phosphate)1309370-86-2 (lactate)
物理性质
合成工艺路线路线简述
海关参考信息
- 2905122000-异丙醇
2905141000-异丁醇
2905142000-仲丁醇
2904100000-仅含磺基的衍生物及其盐和乙酯 - 💡 提示：海关信息按照顺序优先匹配，如需确认的海关信息，请参考相关资料。
- 详情请参考：📖 海关编码查询和海关进出口税则
专利信息
专利号:WO-2008110941-A3
优先权日:2007-03-14
标题 :New process of synthesis of a squalamine and/or trodusquemine precursor
发明人：BRUNEL JEAN MICHEL; VIDAL NICOLAS; PAGES JEAN-MARIE; LETOURNEUX YVES
权利人:UNIV AIX MARSEILLE II; BRUNEL JEAN MICHEL; VIDAL NICOLAS; PAGES JEAN-MARIE; LETOURNEUX YVES
摘要:The invention relates to a new process of synthesis of a squalamine and/or trodusquemine precursor like 24-substituted oxy-7-substitutedoxycholestan-3- one, preferably of 24β-benzoyloxy-7α-hydroxycholestan-3-one.
专利号:US-10906888-B2
优先权日:2016-07-14
标 题:Pyrimidine carboxamides as inhibitors of Vanin-1 enzyme
发明人：CASIMIRO-GARCIA AGUSTIN; STROHBACH JOSEPH WALTER; HEPWORTH DAVID; LOVERING FRANK ELDRIDGE; CHOI CHULHO; ALLAIS CHRISTOPHE PHILIPPE; WRIGHT STEPHEN WAYNE
权利人:PFIZER
摘要:Compounds, pharmaceutically acceptable salts thereof, are disclosed wherein the compounds have the structure of (I) as defined in the specification. Corresponding pharmaceutical compositions, methods of treatment, methods of synthesis, and intermediates are also disclosed.
专利号:US-10308615-B2
优先权日:2015-05-29
标 题:Heterocyclic compounds as inhibitors of Vanin-1 enzyme
发明人：CASIMIRO-GARCIA AGUSTIN; CONDON JEFFREY SCOTT; FLICK ANDREW CHRISTOPHER; GOPALSAMY ARIAMALA; KIRINCICH STEVEN J; MATHIAS JOHN PAUL; STROBACH JOSEPH WALTER; XIANG JASON SHAOYUN; XING LI HUANG; WANG XIAOLUN
权利人:PFIZER
摘要:Compounds, pharmaceutically acceptable salts thereof, are disclosed wherein the compounds have the structure of n nas defined in the specification. Corresponding pharmaceutical compositions, methods of treatment, methods of synthesis, and intermediates are also disclosed.
专利号:US-9321728-B2
优先权日:2012-04-25
标题:Beta-alanine derivatives, pharmaceutically acceptable salts thereof, and pharmaceutical composition comprising same as active ingredient
发明人：AHN JIN HEE; PAGIRE H S; RHEE SANG DAL; KIM KI YOUNG; JUNG WON HOON; BAE MYUNG-AE; SONG JIN SOOK; KIM KWANG-ROK; KWAK HYUN JUNG
权利人:KOREA RES INST CHEM TECH; HANDOK PHARMACEUTICALS CO LTD
摘要:The present invention relates to a beta-alanine derivative, pharmaceutically acceptable salts thereof, and a pharmaceutical composition including the same as an active ingredient. The novel beta-alanine derivative and pharmaceutically acceptable salts thereof according to the present invention may effectively inhibit the activity of DGAT1, which is an enzyme serving as a catalyst in the final step of the synthesis of neutral lipids, to thereby be effectively used as a pharmaceutical composition for preventing or treating various lipid metabolism-related disorders selected from the group consisting of obesity, dyslipidemia, fatty liver, insulin resistance syndrome, and hepatitis.
专利号:WO-2008110941-A2
优先权日:2007-03-14
标题 :New process of synthesis of a squalamine and/or trodusquemine precursor
专利号:US-9771379-B2
优先权日:2015-09-24
标题:N-(2-(2-amino-6-substituted-4,4a,5,6-tetrahydropyrano[3,4-d][1,3]OXAZIN-8a(8H)-yl)-thiazol-4-yl) amides
发明人：BRODNEY MICHAEL AARON; BUTLER CHRISTOPHER RYAN; ZHANG LEI; O'NEILL BRIAN THOMAS
权利人:PFIZER
摘要:The present invention is directed to compounds, tautomers and pharmaceutically acceptable salts of the compounds which are disclosed, wherein the compounds have the structure of Formula I, n nwherein the variables R 1 , R 2 , R 3 , R 4 and X are as defined in the specification. Corresponding pharmaceutical compositions, methods of treatment, methods of synthesis, and intermediates are also disclosed.
供应商参考报价(招募中)
品牌试剂参考报价(招募中)
📌 第三方产品分析报告
主要参考文献
1: Lantz KA, Hart SG, Planey SL, Roitman MF, Ruiz-White IA, Wolfe HR, McLane MP. Inhibition of PTP1B by trodusquemine (MSI-1436) causes fat-specific weight loss in diet-induced obese mice. Obesity (Silver Spring). 2010 Aug;18(8):1516-23. doi: 10.1038/oby.2009.444. doi: 10.1016/j.bbrc.2015.01.040. doi: 10.1080/14756360701809910 . doi: 10.1021/jm200506x. doi: 10.1016/j.pbb.2010.05.010.
6: Salmi C, Loncle C, Vidal N, Letourneux Y, Brunel JM. New stereoselective titanium reductive amination synthesis of 3-amino and polyaminosterol derivatives possessing antimicrobial activities. Eur J Med Chem. 2008 Mar;43(3):540-7. doi: 10.1016/j.bbrc.2014.06.026. doi: 10.1016/j.tins.2015.06.006.
9: Krishnan N, Koveal D, Miller DH, Xue B, Akshinthala SD, Kragelj J, Jensen MR, Gauss CM, Page R, Blackledge M, Muthuswamy SK, Peti W, Tonks NK. Targeting the disordered C terminus of PTP1B with an allosteric inhibitor. Nat Chem Biol. 2014 Jul;10(7):558-66. doi: 10.1038/nchembio.1528.
合成参考文献
参考文献:10.1038/s42003-020-01140-8
摘要:Limbocker R, Mannini B, Ruggeri FS, Cascella R, Xu CK, Perni M, Chia S, Chen SW, Habchi J, Bigi A, Kreiser RP, Wright AK, Albright JA, Kartanas T, Kumita JR, Cremades N, Zasloff M, Cecchi C, Knowles TPJ, Chiti F, Vendruscolo M, Dobson CM. Trodusquemine displaces protein misfolded oligomers from cell membranes and abrogates their cytotoxicity through a generic mechanism. Communications Biology. 2020 Aug 13;3(1):435. doi: 10.1038/s42003-020-01140-8.
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