盐酸吐根碱

• 常用名: 盐酸吐根碱
• 英文名: Emetine hydrochloride
• CAS号: 14198-59-5
• 分子量: 517.100
• 密度: 1.17g/cm3
• 沸点: 624.8ºC at 760 mmHg
• 分子式: C₂₉H₄₁ClN₂O₄
• 熔点: N/A
• 闪点: 331.7ºC

盐酸吐根碱用途

Emetine hydrochloride 是从吐根根部提取的,是一种有效的抗原生动物和催吐剂。Emetine hydrochloride 可以抑制病毒聚合酶 (viral polymerases),并可以抑制寨卡病毒和埃博拉病毒感染。Emetine hydrochloride 有效抑制自噬 (autophagy),具有抗疟疾,抗菌和抗阿米巴虫作用。

盐酸吐根碱名称

• 中文名: 盐酸吐根碱
• 英文名: (2S,3R,11bS)-2-[[(1R)-6,7-dimethoxy-1,2,3,4-tetrahydroisoquinolin-1-yl]methyl]-3-ethyl-9,10-dimethoxy-2,3,4,6,7,11b-hexahydro-1H-benzo[a]quinolizine,hydrochloride

盐酸吐根碱生物活性

• 描述: Emetine hydrochloride 是从吐根根部提取的,是一种有效的抗原生动物和催吐剂。Emetine hydrochloride 可以抑制病毒聚合酶 (viral polymerases),并可以抑制寨卡病毒和埃博拉病毒感染。Emetine hydrochloride 有效抑制自噬 (autophagy),具有抗疟疾,抗菌和抗阿米巴虫作用。
• 相关类别:
  研究领域 >> 感染
  信号通路 >> 细胞周期/DNA损伤 >> DNA/RNA合成
  信号通路 >> 自噬 >> 自噬
  信号通路 >> 抗感染 >> 细菌
• 体外研究: 盐酸依美汀在SNB-19细胞中积聚SQSTM1和MAP1LC3B,表明自噬被阻断[1]。盐酸依美汀剂量依赖性降低感染非洲原形ZIKV MR766的HEK293细胞中NS1蛋白水平(IC50=52.9 nM)。盐酸依美汀可直接抑制ZIKV NS5 RNA聚合酶活性,IC50为121 nM[1]。细胞自噬实验[1]细胞株：SNB-19细胞浓度：25、50、100、200nm孵育时间：24 h结果：显示SQSTM1和MAP1LC3B的积累,表明自噬被阻断。
• 体内研究: 盐酸依美汀(1,2 mg/kg/天；IP；持续3天)显著降低ZIKV感染的Ifnar1–/——小鼠的血清病毒载量[1]。盐酸依美汀(1 mg/kg/天；眼眶后注射；6天)可使3个月大的含紫云英的SJL雌性小鼠的循环ZIKV水平降低约10倍[1]。Emetine(0.002,0.02,0.2,2 mg/kg/天；i.p.)不仅以剂量依赖性方式降低血糖水平,而且还诱导C57Bl/6雄性小鼠(20-25 g)的血糖水平持续降低[2]。动物模型：Ifnar1-/-小鼠[1]剂量：1,2mg/kg给药：IP；每日1次,连续3天结果：显著降低了ZIKV感染Ifnar1-/-小鼠的血清病毒载量。
• 参考文献:

  [1]. Yang S, et al. Emetine inhibits Zika and Ebola virus infections through two molecular mechanisms: inhibitingviral replication and decreasing viral entry. Cell Discov. 2018 Jun 5;4:31.

  [2]. Hudson LK, et al. Emetine Di-HCl attenuates Type 1 diabetes mellitus in mice. Mol Med. 2016 Jun 10;22

  [3]. Matthews H, et al. Drug repositioning as a route to anti-malarial drug discovery: preliminary investigation of the in vitro anti-malarial efficacy of emetine dihydrochloride hydrate. Malar J. 2013 Oct 9;12:359.

  [4]. Khandelwal N, et al. Emetine inhibits replication of RNA and DNA viruses without generating drug-resistant virusvariants. Antiviral Res. 2017 Aug;144:196-204.

  [5]. Sands, M, et al. (1977). Antibacterial activity of emetine. Transactions of the Royal Society of Tropical Medicine and Hygiene, 71(5), 454-455.

盐酸吐根碱物理化学性质

• 密度: 1.17g/cm3
• 沸点: 624.8ºC at 760 mmHg
• 分子式: C₂₉H₄₁ClN₂O₄
• 分子量: 517.100
• 闪点: 331.7ºC
• 精确质量: 516.275513
• PSA: 52.19000
• LogP: 6.01210
• InChIKey: HUEYSSLYFJVUIS-MRFSYGAJSA-N
• SMILES: CCC1CN2CCc3cc(OC)c(OC)cc3C2CC1CC1NCCc2cc(OC)c(OC)cc21.Cl
• 蒸汽压: 4.54E-16mmHg at 25°C

盐酸吐根碱靶点实验

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实验名称：Primary cell-based high-throughput screening assay for identification of compounds th... 来源：Johns Hopkins Ion Channel Center 靶标：regulator of G-protein signaling 4 isoform 2 [Homo sapiens] External Id：JHICC_RGS_Act_HTS

实验名称：Luminescence-based cell-based primary high throughput screening assay to identify ago... 来源：The Scripps Research Institute Molecular Screening Center 靶标：mu-type opioid receptor isoform MOR-1 [Homo sapiens] External Id：OPRM1-OPRD1_AG_LUMI_1536_1X%ACT PRUN

实验名称：Fluorescence-based cell-based primary high throughput screening assay to identify ago... 来源：The Scripps Research Institute Molecular Screening Center 靶标：muscarinic acetylcholine receptor M1 [Homo sapiens] External Id：CHRM1_AG_FLUO8_1536_1X%ACT PRUN

实验名称：uHTS identification of small molecule activators of the adaptive arm of the Unfolded ... 来源：Burnham Center for Chemical Genomics 靶标：N/A External Id：BCCG-A405-UPR-XBP1-PrimaryAgonist-Assay

实验名称：High throughput fluorescence intensity-based biochemical assay to screen for small mo... 来源：University of Pittsburgh Molecular Library Screening Center 靶标：furin (paired basic amino acid cleaving enzyme), isoform CRA_a [Homo sapiens] External Id：MH080376 Biochemical HTS for Inhibitors of the Proprotein Convertase Furin.

实验名称：Fluorescence polarization to screen for inhibitor that competite the binding of FadD2... 来源：Broad Institute 靶标：FATTY-ACID-CoA LIGASE FADD28 (FATTY-ACID-CoA SYNTHETASE) External Id：2147-01_Inhibitor_SinglePoint_HTS_Activity

实验名称：Flow Cytometric HTS Screen for inhibitors of the ABC transporter ABCB6 for Validation... 来源：NMMLSC 靶标：ATP-binding cassette sub-family B member 6, mitochondrial [Homo sapiens] External Id：UNMCMD_ABCB6_1o_ValidationSet

实验名称：Counterscreen for inhibitors of the Steroid Receptor Coactivator 1 (SRC1; NCOA1): Lum... 来源：The Scripps Research Institute Molecular Screening Center 靶标：transactivating tegument protein VP16 [Human herpesvirus 1] External Id：VP16_INH_LUMI_1536_3X%INH CSRUN for SRC1

实验名称：HSF-1 induced GFP reporter and Doxycycline induced RFP reporter Measured in Cell-Base... 来源：Broad Institute 靶标：Hsf1 protein External Id：2038-03_Inhibitor_Dose_CherryPick_Activity_Set4

实验名称：Primary Screen Inhibitors of CD40 Signaling in BL2 Cells Measured in Cell-Based Syste... 来源：Broad Institute 靶标：N/A External Id：7124-01_Inhibitor_SinglePoint_HTS_Activity

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盐酸吐根碱英文别名

• (-)-Emetine hydrochloride
• Cephaeline methyl ether HCl
• 6',7',10,11-Tetramethoxyemetan hydrochloride (1:1)
• Cephaeline methyl ether hydrochloride
• Emetin-hydrochlorid
• EMETINE HYDROCHLORIDE
• 2H-Benzo[a]quinolizine, 3-ethyl-1,3,4,6,7,11b-hexahydro-9,10-dimethoxy-2-[[(1R)-1,2,3,4-tetrahydro-6,7-dimethoxy-1-isoquinolinyl]methyl]-, (2S,3R,11bS)-, hydrochloride (1:1)
• Emetine monohydrochloride
• Emetan, 6',7',10,11-tetramethoxy-, monohydrochloride
• emetine chloride