吐根碱二盐酸盐作用机制 - Medchemexpress - MCE中国

1、Product Data SheetEmetine dihydrochlorideCat. No.: HY-B1479ACAS No.: 316-42-7分式: CHClNO分量: 553.56作靶点: Parasite; DNA/RNA Synthesis; Autophagy; Bacterial作通路: Anti-infection; Cell Cycle/DNA Damage; Autophagy储存式: Powder -20C 3 years4C 2 yearsIn solvent -80C 6 months-20C 1 month溶解性数据体外实验 DMSO : 50 mg/mL

2、(90.32 mM; Need ultrasonic)SolventMass1 mg 5 mg 10 mgConcentration制备储备液1 mM 1.8065 mL 9.0324 mL 18.0649 mL5 mM 0.3613 mL 1.8065 mL 3.6130 mL10 mM 0.1806 mL 0.9032 mL 1.8065 mL请根据产品在不同溶剂中的溶解度选择合适的溶剂配制储备液；旦配成溶液，请分装保存，避免反复冻融造成的产品失效。储备液的保存式和期限：-80C, 6 months; -20C, 1 month。-80C 储存时，请在 6 个内使，-20C 储存时，请在

3、1 个内使。体内实验请根据您的实验动物和给药式选择适当的溶解案。以下溶解案都请先按照 In Vitro 式配制澄清的储备液，再依次添加助溶剂：为保证实验结果的可靠性，澄 的储备液可以根据储存条件，适当保存；体内实验的作液，建议您现现配，当天使； 以下溶剂前显的百分 指该溶剂在您配制终溶液中的体积占；如在配制过程中出现沉淀、析出现象，可以通过加热和/或超声的式助溶1. 请依序添加每种溶剂： 10% DMSO 40% PEG300 5% Tween-80 45% salineSolubility: 2.5 mg/mL (4.52 mM); Clear solution此案可获得 2.5 mg/mL

4、 (4.52 mM，饱和度未知) 的澄清溶液。以 1 mL 作液为例，取 100 L 25.0 mg/mL 的澄 DMSO 储备液加到 400 L PEG300 中，混合均匀；向上述体系中加50 L Tween-80，混合均匀；然后继续加 450 L 理盐定容 1 mL。2. 请依序添加每种溶剂： 10% DMSO 90% (20% SBE-CD in saline)Solubility: 2.5 mg/mL (4.52 mM); Clear solution此案可获得 2.5 mg/mL (4.52 mM，饱和度未知) 的澄清溶液。Page 1 of 2 www.MedChemE以 1 mL

5、 作液为例，取 100 L 25.0 mg/mL 的澄均匀。DMSO 储备液加到 900 L 20% 的 SBE-CD 理盐溶液中，混合BIOLOGICAL ACTIVITY物活性 Emetine dihydrochloride 从吐根根部提取的， 种有效的抗原动物和催吐剂。Emetine dihydrochloride 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 dihydrochloride 有效抑制噬 (autophagy)，具有抗疟疾，抗 和抗阿巴作。体外研究 Emetine dihydrochloride accu

6、mulates SQSTM1 and MAP1LC3B in SNB-19 cells, indicating autophagy is blocked1.Emetine dihydrochloride dose-dependently decreases NS1 protein level in HEK293 cells infected with the Africanprototype, ZIKV MR766 (IC50=52.9 nM). Emetine dihydrochloride directly inhibits ZIKV NS5 RNA polymerase activity

7、with an IC50 of 121 nM1.Cell Autophagy Assay1Cell Line: SNB-19 cellsConcentration: 25, 50, 100, 200 nMIncubation Time: For 24 hoursResult: Showed the accumulation of SQSTM1 and MAP1LC3B, indicating autophagy wasblocked.体内研究 Emetine dihydrochloride (1, 2 mg/kg/day; IP; for 3 days) significantly reduc

8、es the serum viral load of ZIKV infectedIfnar1/ mice1.Emetine dihydrochloride (1 mg/kg/day; retro-orbital injection; for six days) reduces the levels of circulating ZIKVapproximately 10-fold in three-month-old female SJL mice with ZIKVBR1.Emetine (0.002, 0.02, 0.2, 2 mg/kg/day; i.p.) not only attenu

9、ates blood glucose levels in dose-dependent way but alsoinduces a persistent attenuation of blood glucose levels in C57Bl/6 male mice (20-25 g)2.Animal Model: Ifnar1/ mice1Dosage: 1, 2 mg/kgAdministration: IP; once daily for 3 daysResult: Significantly reduced the serum viral load of ZIKV infected I

10、fnar1/ mice.户使本产品发表的科研献 Cell Rep. 2020 Jan 7;30(1):98-111.e5. Biomed J. 2020 May 23.See more customer validations on HYPERLINK www.MedChemE www.MedChemEREFERENCESPage 2 of 3 www.MedChemE1. Yang S, et al. Emetine inhibits Zika and Ebola virus infections through two molecular mechanisms: inhibitingvir

11、al 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;223. Matthews H, et al. Drug repositioning as a route to anti-malarial drug discovery: preliminary investigation of the in vitr

12、o anti-malarial efficacy of emetinedihydrochloride 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. 2017Aug;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.McePdfHeightCaution: Product has not