CAS: 1005491-05-3; 6-Ethynyl-1-(Pentan-3-yl)-1,3-Dihydro-2H-Imidazo[4,5-B]Pyrazin-2-One
该化合物是一种化学化合物,在制药研究中引起注意,特别是其潜在的治疗用途,被归类为小分子,并已知与特定的生物目标相互作用,这可能会对其药理作用产生影响;该化合物的结构包括药物设计中典型的功能组,允许与各种生物途径互动;Tirasemitiv因其在调节某些生理过程方面的作用而进行了研究,其功效和安全特征是正在进行的研究的主题;与药物开发管道中的许多化合物一样,其特性,包括溶性,稳定性和生物利用率,对于确定其作为治疗剂的潜力至关重要;有必要开展进一步研究,以充分阐明其行动机制并评估其临床相关性.
- ⚠️《2026年兴奋剂目录》
- 英文名称6-Ethynyl-1-(Pentan-3-yl)-1,3-Dihydro-2H-Imidazo[4,5-B]Pyrazin-2-One
- 中文名称Tirasemtiv(CK-2017357)抑制剂
- IUPAC名称6-ethynyl-1-(pentan-3-yl)-1,3-dihydro-2H-imidazo[4,5-b]pyrazin-2-one
- CAS编号1005491-05-3
- MFCD编号:MFCD28023588
- FDA UNII编号:G8WSM7R635
- 分子式:C12H14N4O分子量:230.27
- 产品CID: 12350
- 同类组份化合物CAS1005491-05-3
- 产品分类生物化工 → 生化试剂 → 激动剂抑制剂
物理性质
MSDS等安全信息
上下游产品
1-(戊-3-基)-6-((三甲基硅基)乙炔基)-1H-咪唑并[4,5-B]吡嗪-2(3H)-酮 1-(Pentan-3-yl)-6-((Trimethylsilyl)Ethynyl)-1H-Imidazo[4,5-B]Pyrazin-2-Ol 1005491-06-46-Bromo-1-(Pentan-3-yl)-1H-Imidazo[4,5-B]Pyrazin-2(3H)-One
合成工艺路线路线简述
📜3-氨基戊烷置于bis-Triphenylphosphine-Palladium(II) Chloride,Potassium Fluoride,Copper(L) Iodide,水,三乙胺体系中,用 四氢呋喃,甲醇,N,N-二甲基甲酰胺 用作溶剂,化学反应 21.5H,反应生成Tirasemtiv(Ck-2017357)抑制剂
参考文献:发现首个直接快速骨骼肌肌钙蛋白激活剂tirasemtiv
标题:发现首个直接快速骨骼肌肌钙蛋白激活剂tirasemtiv
摘要:报告了快速骨骼肌第一个激活剂的鉴定和优化.从高通量筛选(hts)中鉴定出化合物1,随后发现该化合物通过与肌钙蛋白复合物的相互作用来改善肌肉功能.优化1效价,代谢稳定性,并导致tirasemtiv的发现(物理性质25),它已经被广泛表征在临床试验中对肌萎缩侧索硬化的治疗.
Doi:10.1021/acsmedchemlett.7B00546
专利信息
专利号:US-10034848-B2
优先权日:2014-11-03
标 题:Increase of protein synthesis ameliorates synaptopathy-related neurological disorders
发明人：HSUEH YI-PING
权利人:ACADEMIA SINICA
摘要:Disclosed herein is a method for increasing the dendritic spine formation or dendritic spine density in a subject, who is affected by a dendritic spine defect caused by the impairment in neurofibromin (NF1 protein), valosin-containing protein (VCP), atlastin-1 (ATL1), or superoxide dismutase 1 (SOD1). Accordingly, also disclosed herein is a method for treating a subject having or suspected of having a synaptopathy caused by the impairment in NF1, VCP, ATL1, or SOD1.
专利号:US-2016120831-A1
优先权日:2014-11-03
标 题 :Increase of protein synthesis ameliorates synaptopathy-related neurological disorders
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: Hansen R, Saikali KG, Chou W, Russell AJ, Chen MM, Vijayakumar V, Stoltz RR, Baudry S, Enoka RM, Morgans DJ, Wolff AA, Malik FI. Tirasemtiv amplifies skeletal muscle response to nerve activation in humans. Muscle Nerve. 2014 Dec;50(6):925-31. doi: 10.1002/mus.24239.
2: Galli RA, Borsboom TC, Gineste C, Brocca L, Rossi M, Hwee DT, Malik FI, Bottinelli R, Gondin J, Pellegrino MA, de Winter JM, Ottenheijm CAC. Tirasemtiv enhances submaximal muscle tension in an Acta1:p.Asp286Gly mouse model of nemaline myopathy. J Gen Physiol. 2024 Apr 1;156(4):e202313471. doi: 10.1085/jgp.202313471. Epub 2024 Feb 20.
3: Shefner JM, Cudkowicz ME, Hardiman O, Cockcroft BM, Lee JH, Malik FI, Meng L, Rudnicki SA, Wolff AA, Andrews JA; VITALITY-ALS Study Group. A phase III trial of tirasemtiv as a potential treatment for amyotrophic lateral sclerosis. Amyotroph Lateral Scler Frontotemporal Degener. 2019;0(0):1-11. doi: 10.1080/21678421.2019.1612922. Erratum in: Amyotroph Lateral Scler Frontotemporal Degener. 2019 Nov;20(7-8):630. doi: 10.1080/21678421.2019.1639381. 64(6):3026-3034. doi: 10.1021/acs.jmedchem.0c01412. Epub 2021 Mar 11. 26(1-2):103-112. doi: 10.1080/21678421.2024.2423707. Epub 2024 Nov 8. 30(14):1305-1320. doi: 10.1093/hmg/ddab112.
合成参考文献
参考文献:10.1007/s13539-014-0149-7
摘要:Morley JE, von Haehling S, Anker SD. Are we closer to having drugs to treat muscle wasting disease J cachexia sarcopenia muscle. 2014 May 28;5(2):83–7. doi: 10.1007/s13539-014-0149-7.
参考文献:10.1177/1358863x14534516
摘要:Bauer TA, Wolff AA, Hirsch AT, Meng LL, Rogers K, Malik FI, Hiatt WR. Effect of tirasemtiv, a selective activator of the fast skeletal muscle troponin complex, in patients with peripheral artery disease. Vasc Med. 2014 Aug;19(4):297–306. doi: 10.1177/1358863x14534516.
参考文献:10.1016/j.prrv.2018.03.003
摘要:Kariyawasam D, Carey KA, Jones KJ, Farrar MA. New and developing therapies in spinal muscular atrophy. Paediatr Respir Rev. 2018 Sep;28():3–10. doi: 10.1016/j.prrv.2018.03.003.
参考文献:10.14283/jfa.2019.11
摘要:Rooks D, Roubenoff R. Development of Pharmacotherapies for the Treatment of Sarcopenia. The Journal of Frailty & Aging. 2019 Apr 30;8(3):120–30. doi: 10.14283/jfa.2019.11.
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