二鹽酸吐根堿水合物作用機制 - Medchemexpress - MCE中國

1、Product Data SheetEmetine dihydrochloride hydrateCat. No.: HY-B1479BCAS No.: 7083-71-8分式: CHNO . HCl . HO分量: 571.58作靶點: Parasite; DNA/RNA Synthesis; Autophagy; Bacterial作通路: Anti-infection; Cell Cycle/DNA Damage; Autophagy儲存式: Powder -20C 3 years4C 2 yearsIn solvent -80C 6 months-20C 1 month溶解性數(shù)據(jù)體外實

2、驗 DMSO : 16.5 mg/mL (28.87 mM; Need ultrasonic and warming)SolventMass1 mg 5 mg 10 mgConcentration制備儲備液1 mM 1.7495 mL 8.7477 mL 17.4954 mL5 mM 0.3499 mL 1.7495 mL 3.4991 mL10 mM 0.1750 mL 0.8748 mL 1.7495 mL請根據(jù)產(chǎn)品在不同溶劑中的溶解度選擇合適的溶劑配制儲備液；旦配成溶液，請分裝保存，避免反復凍融造成的產(chǎn)品失效。儲備液的保存式和期限：-80C, 6 months; -20C, 1 mont

3、h。-80C 儲存時，請在 6 個內(nèi)使，-20C 儲存時，請在 1 個內(nèi)使。體內(nèi)實驗請根據(jù)您的實驗動物和給藥式選擇適當?shù)娜芙獍?。以下溶解案都請先按?In Vitro 式配制澄清的儲備液，再依次添加助溶劑：為保證實驗結(jié)果的可靠性，澄 的儲備液可以根據(jù)儲存條件，適當保存；體內(nèi)實驗的作液，建議您現(xiàn)現(xiàn)配，當天使； 以下溶劑前顯的百分 指該溶劑在您配制終溶液中的體積占；如在配制過程中出現(xiàn)沉淀、析出現(xiàn)象，可以通過加熱和/或超聲的式助溶1. 請依序添加每種溶劑： 10% DMSO 40% PEG300 5% Tween-80 45% salineSolubility: 2.08 mg/mL (3.64 m

4、M); Clear solution此案可獲得 2.08 mg/mL (3.64 mM，飽和度未知) 的澄清溶液。以 1 mL 作液為例，取 100 L 20.8 mg/mL 的澄 DMSO 儲備液加到 400 L PEG300 中，混合均勻；向上述體系中加50 L Tween-80，混合均勻；然后繼續(xù)加 450 L 理鹽定容 1 mL。2. 請依序添加每種溶劑： 10% DMSO 90% (20% SBE-CD in saline)Solubility: 2.08 mg/mL (3.64 mM); Clear solution此案可獲得 2.08 mg/mL (3.64 mM，飽和度未知)

5、的澄清溶液。Page 1 of 2 www.MedChemE以 1 mL 作液為例，取 100 L 20.8 mg/mL 的澄均勻。DMSO 儲備液加到 900 L 20% 的 SBE-CD 理鹽溶液中，混合3. 請依序添加每種溶劑： 10% DMSO 90% corn oilSolubility: 2.08 mg/mL (3.64 mM); Clear solution此案可獲得 2.08 mg/mL (3.64 mM，飽和度未知) 的澄 溶液，此案不適于實驗周 期在半個以上的實驗。以 1 mL 作液為例，取 100 L 20.8 mg/mL 的澄 DMSO 儲備液加到 900 L 油中，混

6、合均勻。BIOLOGICAL ACTIVITY物活性 Emetine dihydrochloride hydrate 從吐根根部提取的， 種有效的抗原動物和催吐劑。Emetine dihydrochloride hydrate 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 hydrate 有效抑制噬 (autophagy)，具有抗瘧疾，抗 和抗阿巴作。體外研究 Emetine dihydrochloride hydrate accumulates SQSTM1 and MAP1LC3B in SN

7、B-19 cells, indicating autophagy isblocked1.Emetine dihydrochloride hydrate dose-dependently decreases NS1 protein level in HEK293 cells infected with theAfrican prototype, ZIKV MR766 (IC50=52.9 nM). Emetine dihydrochloride directly inhibits ZIKV NS5 RNA polymeraseactivity with an IC50 of 121 nM1.Ce

8、ll 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.體內(nèi)研究 Emetine dihydrochloride hydrate (1, 2 mg/kg/day; IP; for 3 days) significantly reduces the serum viral

9、 load of ZIKVinfected Ifnar1/ mice1.Emetine dihydrochloride hydrate (1 mg/kg/day; retro-orbital injection; for six days) reduces the levels of circulatingZIKV approximately 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 attenuates blood

10、 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 Ifnar1/ mic

11、e.戶使本產(chǎn)品發(fā)表的科研獻 Cell Rep. 2020 Jan 7;30(1):98-111.e5.Page 2 of 3 www.MedChemE Biomed J. 2020 May 23.See more customer validations on HYPERLINK www.MedChemE www.MedChemEREFERENCES1. Yang S, et al. Emetine inhibits Zika and Ebola virus infections through two molecular mechanisms: inhibitingviral replica

12、tion 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 vitro anti-mal

13、arial 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: Pr