CAS: 446859-33-2; 2-(3-(6-Methylpyridin-2-yl)-1H-Pyrazol-4-yl)-1,5-Naphthyridine
该化合物是一个复杂的有机化合物,其特点是多环结构,包括一个环虫肾脏和以环虫酮组替代的丙烯菊酯环.该化合物通常具有有机溶剂中中度至高溶性等特性,视其存在的具体功能组不同而不同.它可能显示生物活动,使其对医药化学感兴趣,特别是制药业.其结构中氮原子的存在表明氢与金属离子的结合和协调潜力,这可能影响其再活性和与生物目标的相互作用.此外,丙烯环上的甲基组可影响该化合物的脂质性和总体药理特性.与许多异环化合物一样,其合成可能涉及多步反应,其稳定性可能受到诸如pH和温度等环境因素的影响.
- 英文名称2-(3-(6-Methylpyridin-2-yl)-1H-Pyrazol-4-yl)-1,5-Naphthyridine
- 中文名称2-(3-(6-甲基吡啶-2-基)-1H-吡唑-4-基)-1,5-萘啶
- IUPAC名称2-(3-(6-methylpyridin-2-yl)-1H-pyrazol-4-yl)-1,5-naphthyridine
- 其它别名ALK5 INHIBITOR I; 2-(3-(6-METHYLPYRIDIN-2-YL)-1H-PYRAZOL-4-YL)-1,5-NAPHTHYRIDINE; TGF-BETA RI KINASE INHIBITOR II; TRANSFORMING GROWTH FACTOR-BETA TYPE I RECEPTOR KINASE INHIBITOR I; 2-(3-(6-Methylpyridine-2-yl)-1H-pyrazol-4-yl)-1,5-naphthyridine; 2-[3-(6-Methyl-2-pyridinyl)-1H-pyrazol-4-yl]-1,5-naphthyridine; RepSox
- CAS编号446859-33-2
- MFCD编号:MFCD09037561
- EINECS号:663-924-9
- FDA UNII编号:JT8ZW3H2ST
- 分子式:C17H13N5
- 分子量:287.33
- 产品CID: 1454516
- 产品分类生物化工 → 抑制剂 → TGF→beta/Smad信号通路抑制剂(TGF→beta/Smad)
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
N,N-dimethyl-formamide dimethyl acetalN,N-dimethyl-formamide dimethyl acetal 1-(6-methylpyridin-2-yl)-2-(1,5-naphthyridin-2-yl)ethan-1-one 5-Amino-2-methylpyridine 2-methyl-[1,5]naphthyridine合成工艺路线路线简述
2-甲基-1,5-萘啶置于双(三甲基硅烷基)氨基钾,溶剂黄146体系中,用 四氢呋喃,N,N-二甲基甲酰胺,甲苯 作为反应溶剂,化学反应 24.0H,反应生成 2-(3-(6-甲基吡啶-2-基)-1H-吡唑-4-基)-1,5-萘啶
参考文献:1,5-萘啶衍生物的鉴定为一系列新的有效和选择性的i型tgf-β受体抑制剂.
标题:1,5-萘啶衍生物的鉴定为一系列新的有效和选择性的i型tgf-β受体抑制剂.
摘要:筛选命中1的优化导致鉴定了新型1,5-萘啶氨基噻唑和吡唑衍生物,它们是转化生长因子βi型受体alk5的有效抑制剂.分别以ic50 = 6和4 Nm抑制alk5自磷酸化的化合物15和19在结合和细胞分析中均显示出强大的活性,并显示出超过p38促分裂原活化蛋白激酶的选择性.描述了与人alk5结合的19的x射线晶体结构,证实了对接研究提出的结合模式.
DOI:10.1021/jm0400247
海关参考信息
- 2933310010-吡啶
2939800000-其他生物碱 - 💡 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。
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专利信息
专利号:WO-2022191130-A1
优先权日:2021-03-08
标 题:Method for proliferating cardiomyocytes, method for producing cardiomyocytes, and cardiomyocyte proliferating agent
发明人：YAMASHITA JUN; YOSHIOKA MIKI
权利人:UNIV KYOTO
摘要:Provided are a method for proliferating cardiomyocytes, a method for producing cardiomyocytes, and a cardiomyocyte proliferating agent capable of contributing to cardiac regenerative medicine, that make it possible to induce proliferation of human cardiomyocytes by a drug. The method for proliferating cardiomyocytes, method for producing cardiomyocytes, and cardiomyocyte proliferating agent, including a step for culturing cardiomyocytes in the presence of one or more compounds selected from the group consisting of ALK inhibitors, cytochrome P450 omega hydroxylase inhibitors, and fatty acid synthesis inhibitors
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主要参考文献
1: Xu D, Liu G, Zhao M, Wan X, Qu Y, Murayama R, Hashimoto K. Effects of arketamine on depression-like behaviors and demyelination in mice exposed to chronic restrain stress: A role of transforming growth factor-β1. J Affect Disord. 2024 Sep 3;367:745-755. doi: 10.1016/j.jad.2024.08.222. Epub ahead of print. 74(2):40. doi: 10.1007/s12031-024-02206-6. 18(1):7. doi: 10.1186/s13036-024-00405-8.
5: Guo D, Zhang B, Han L, Rensing NR, Wong M. Cerebral vascular and blood brain- barrier abnormalities in a mouse model of epilepsy and tuberous sclerosis complex. Epilepsia. 2024 Feb;65(2):483-496. doi: 10.1111/epi.17848. Epub 2023 Dec 16.
6: Taga H, Kishida T, Inoue Y, Yamamoto K, Kotani SI, Masashi T, Ukimura O, Mazda O. TGF-β inhibitor treatment of H₂O₂-induced cystitis models provides biochemical mechanism for elucidating interstitial cystitis/painful bladder syndrome patients. PLoS One. 2023 Nov 6;18(11):e0293983. doi: 10.1371/journal.pone.0293983.
合成参考文献
参考文献:10.5966/sctm.2013-0193
摘要:Jajosky AN, Coad JE, Vos JA, Martin KH, Senft JR, Wenger SL, Gibson LF. RepSox slows decay of CD34+ acute myeloid leukemia cells and decreases T cell immunoglobulin mucin-3 expression. Stem Cells Transl Med. 2014 Jul;3(7):836–48.
参考文献:10.1038/s41401-019-0264-2
摘要:Tu W, Fu Y, Xie X. RepSox, a small molecule inhibitor of the TGFβ receptor, induces brown adipogenesis and browning of white adipocytes. Acta Pharmacologica Sinica. 2019 Jun 24;40(12):1523–31. doi: 10.1038/s41401-019-0264-2.
参考文献:10.1021/jm0400247
摘要:Gellibert F, Woolven J, Fouchet MH, Mathews N, Goodland H, Lovegrove V, Laroze A, Nguyen VL, Sautet S, Wang R, Janson C, Smith W, Krysa G, Boullay V, De Gouville AC, Huet S, Hartley D. Identification of 1,5-naphthyridine derivatives as a novel series of potent and selective TGF-beta type I receptor inhibitors. J Med Chem. 2004 Aug 26;47(18):4494–506. doi: 10.1021/jm0400247.
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