CAS: 459168-41-3; (5-Chloro-1H-Indol-2-yl)(4-Methylpiperazin-1-yl)Methanone
该化合物是三胺H4受体(H4R)的选择性强强敌,具有高度亲近性(Ki < 5nM),与其他抗体亚型具有特殊性,其行动机制包括阻塞H4R中介信号路径,使其成为调查H4R在炎症和免疫反应中的作用的宝贵工具.该化合物显示出有利的药效活性特性,包括口服生物利用率和代谢稳定性,促进了活性研究.JNJ-77120在临床前研究中广泛用于探索在过敏炎,普里图斯和自免疫紊乱等条件下的治疗潜力.其精密特征支持可靠和可复制的实验结果.
- 英文名称(5-Chloro-1H-Indol-2-yl)(4-Methylpiperazin-1-yl)Methanone
- 中文名称1-[(5-氯-1H-吲哚-2-基)羰基]-4-甲基哌嗪
- IUPAC名称(5-chloro-1H-indol-2-yl)(4-methylpiperazin-1-yl)methanone
- 其它别名(5-Chloro-1H-Indol-2-yl)-(4-Methyl-Piperazin-1-yl)-Methanone; (5-Chloro-1H-Indol-2-yl)-(4-Methylpiperazin-1-yl)Methanone; (5-Chloro-1H-Indol-2-yl)(4-Methylpiperazin-1-yl)Methanone
- CAS编号459168-41-3
- MFCD编号:MFCD04343337
- EINECS号:636-930-4
- FDA UNII编号:4H1AU2V37X
- 分子式:C14H16ClN3O分子量:277.76
- 产品CID: 1459906
- 产品分类生物化工 → 抑制剂 → 神经信号通路(Neuronal Signaling)
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
CAS号109-01-3 N-甲基哌嗪 | CAS号10517-21-2 5-氯吲哚-2-甲酸合成工艺路线路线简述
📜N-甲基哌嗪,5-氯吲哚-2-羧酸置于n-甲基吗啉,4,4'-双甲氧基三苯甲基氯体系中,用 乙腈 作为反应溶剂,化学反应 28.5H,以81%的收率获得产物1-[(5-氯-1H-吲哚-2-基)羰基]-4-甲基哌嗪
参考文献:组胺 H4 受体拮抗剂 1-[(5-Chloro-1H-Indol-2-yl)Carbonyl]-4-Methylpiperazine 的简便合成方法和晶体结构
标题:组胺 H4 受体拮抗剂 1-[(5-Chloro-1H-Indol-2-yl)Carbonyl]-4-Methylpiperazine 的简便合成方法和晶体结构
摘要:摘要 1-[(5-Chloro-1H-Indol-2-yl)Carbonyl]-4-Methylpiperazine (Jnj 7777120) 是已知的组胺 H4 受体参考化合物.描述了其合成的简便方法和晶体结构.
DOI:10.1515/hc.2011.035
海关参考信息
- 2903919090-氯苯
2912110000-甲醛
2921211000-乙二胺
2924191000-二甲基甲酰胺 - 💡 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:US-11384076-B2
优先权日:2017-08-18
标 题:Synthesis, pharmacology and use of new and selective FMS-like tyrosine kinase 3 (FLT3) FLT3 inhibitors
发明人：MAHBOOBI SIAVOSH; SELLMER ANDREAS; PONGRATZ HERWIG; PILSL BERNARDETTE; KRÄMER OLIVER; KINDLER THOMAS; BEYER MANDY
权利人:UNIV REGENSBURG; UNIV DER JOHANNES GUTENBERG UNIV MAINZ
摘要:The present invention relates to small molecule compounds of formula (I) and their use as FLT3 inhibitors for the treatment of various diseases, such as acute myeloid leukemia (AML). The present invention further relates to methods of synthesizing the compounds and methods of treatment.
专利号:EP-3668867-B1
优先权日:2017-08-18
标 题 :Synthesis, pharmacology and use of new and selective fms-like tyrosine kinase 3 (flt3) flt3 inhibitors
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: Kovacova-Hanuskova E, Gavliakova S, Buday T, Kosutova P, Mokra D, Urbanova-Fulmekova A, Mokry J, Plevkova J. The effect of selective antagonist of H4 receptor JNJ7777120 on nasal symptoms, cough, airway reactivity and inflammation in guinea pigs. Respir Physiol Neurobiol. 2015 Sep 15;216:9-14. doi: 10.1016/j.resp.2015.05.007. Epub 2015 May 21. doi: 10.1124/jpet.114.215152. Epub 2014 Sep 2. doi: 10.1371/journal.pone.0069106. Print 2013.
4: Coruzzi G, Pozzoli C, Adami M, Grandi D, Guido N, Smits R, de Esch I, Leurs R. Strain-dependent effects of the histamine H₄ receptor antagonist JNJ7777120 in a murine model of acute skin inflammation. Exp Dermatol. 2012 Jan;21(1):32-7. doi: 10.1111/j.1600-0625.2011.01396.x. doi: 10.1016/j.bmcl.2011.09.001. Epub 2011 Sep 8. doi: 10.1124/mol.111.071266. Epub 2011 Jan 25. Review. doi: 10.1124/mol.110.068395. Epub 2010 Dec 6. doi: 10.1007/s00011-009-8245-4. Epub 2007 Feb 23.
合成参考文献
参考文献:10.1021/jm7014217
摘要:Smits RA, Lim HD, Hanzer A, Zuiderveld OP, Guaita E, Adami M, Coruzzi G, Leurs R, de Esch IJ. Fragment based design of new H4 receptor-ligands with anti-inflammatory properties in vivo. J Med Chem. 2008 Apr 24;51(8):2457–67. doi: 10.1021/jm7014217.
参考文献:10.1007/s11882-008-0005-y
摘要:Huang JF, Thurmond RL. The new biology of histamine receptors. Curr Allergy Asthma Rep. 2008 Mar;8(1):21–7. doi: 10.1007/s11882-008-0005-y.
参考文献:10.1186/1471-2407-11-195
摘要:Fang Z, Yao W, Xiong Y, Li J, Liu L, Shi L, Zhang W, Zhang C, Nie L, Wan J. Attenuated expression of HRH4 in colorectal carcinomas: a potential influence on tumor growth and progression. BMC Cancer. 2011 May 24;11():195:1–11.
参考文献:10.1007/s10753-014-9898-x
摘要:Lamraoui A, Adi-Bessalem S, Laraba-Djebari F. Modulation of tissue inflammatory response by histamine receptors in scorpion envenomation pathogenesis: involvement of H4 receptor. Inflammation. 2014 Oct;37(5):1689–704. doi: 10.1007/s10753-014-9898-x.
参考文献:10.1007/s00210-015-1179-1
摘要:Werner K, Neumann D, Seifert R. High constitutive Akt2 activity in U937 promonocytes: effective reduction of Akt2 phosphorylation by the histamine H2-receptor and the β2-adrenergic receptor. Naunyn Schmiedebergs Arch Pharmacol. 2016 Jan;389(1):87–101. doi: 10.1007/s00210-015-1179-1.
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