| 生物活性 | Amantadine (1-Adamantanamine) hydrochloride is an orally avtive and potent antiviral agent with activity againstinfluenza Aviruses. Amantadine hydrochloride inhibits several ion channels such asNMDAandM2, and also inhibits Coronavirus ion channels. Amantadine hydrochloride also has anti-orthopoxvirusand anticancer activity. Amantadine hydrochloride can be used for Parkinson's disease, postoperative cognitive dysfunction (POCD) and COVID-19 research[1][2][3][4][5][6]. |
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体外研究
(In Vitro) | Amantadine hydrochloride (0-500 μM, 26 h) inhibits SARS-CoV-2 replication, with IC50concentrations between 83 and 119 μM[4].
Amantadine hydrochloride (0-100 μg/mL, 24-72 h) markedly inhibits the proliferation of HepG2 and SMMC-7721 cells[6].
Amantadine hydrochloride (0-75 μg/mL, 48 h) arrests the cell cycle at the G0/G1 phase and induces apoptosis[6].
Amantadine hydrochloride (0-75 μg/mL, 48 h) reduces the levels of the cell cycle-related genes and proteins (cyclin D1, cyclin E and CDK2), reduces Bcl-2 and increases the Bax protein and mRNA levels[6].
Cell Viability Assay[4] | Cell Line: | Vero E6 cells | | Concentration: | 500 μM, 100 μM, 20 μM, 4 μM, and 8 nM | | Incubation Time: | 26 h | | Result: | Caused a concentration-dependent reduction (IC50=83 μM) of viral nucleic acids in the supernatant 26 h after infection at 10-500 μM. Caused a concentration-dependent reduction (IC50=119 μM) of viral nucleic acids in the cytosol 26 h after infection. |
Cell Proliferation Assay[6] | Cell Line: | Human HCC cell lines (HepG2 and SMMC-7721) and normal hepatocellular cells (L02 cells) | | Concentration: | 0, 1, 2, 5, 10, 25, 50 and 100 μg/mL | | Incubation Time: | 24, 48 and 72 h | | Result: | Inhibited cellular proliferation in a time- and dose-dependent manner in HepG2 and SMMC-7721 cells. |
Cell Cycle Analysis[6] | Cell Line: | HepG2 and SMMC-7721 cells | | Concentration: | 0, 10, 25, 50 and 75 μg/mL | | Incubation Time: | 48 h | | Result: | Significantly increased the population of HepG2 and SMMC-7721 cells in the G0/G1 phase in a dose-dependent manner, and significantly decreased the number of HepG2 cells in the S phase. |
Apoptosis Analysis[6] | Cell Line: | HepG2 and SMMC-7721 cells | | Concentration: | 0, 10, 25, 50 and 75 μg/mL | | Incubation Time: | 48 h | | Result: | Markedly increased the percentage of apoptotic HepG2 and SMMC-7721 cells (early- and late-stage apoptosis) in a dose-dependent manner. |
Western Blot Analysis[6] | Cell Line: | HepG2 and SMMC-7721 cells | | Concentration: | 0, 10, 25, 50 and 75 μg/mL | | Incubation Time: | 48 h | | Result: | Showed downregulation of cyclin D1, cyclin E and CDK2, and showed a decrease in Bcl-2 levels and an increase of Bax levels in HepG2 and SMMC-7721 cells. |
RT-PCR[6] | Cell Line: | HepG2 and SMMC-7721 cells | | Concentration: | 0, 10, 25, 50 and 75 μg/mL | | Incubation Time: | 48 h | | Result: | Revealed an increase in Bax and decrease in Bcl-2 genes. |
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体内研究
(In Vivo) | Amantadine hydrochloride (25 mg/kg, IP, once daily for 3 days) inhibits surgery induced neuroinflammation and learning and memory impairment[5].
| Animal Model: | Fischer 344 rats (Four-month old, male, 290-330 g, 15 rats each group)[5] | | Dosage: | 25 mg/kg | | Administration: | IP, once daily for 3 days (the first dose at 15 min before surgery) | | Result: | Inhibited surgery induced neuroinflammation and learning and memory impairment, increased GDNF (glial cell line-derived neurotrophic factor) that was co-localized with glial fibrillary acidic protein (an astrocytic marker) in the hippocampus. |
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| 运输条件 | Room temperature in continental US; may vary elsewhere. |
| 储存方式 | 4°C, sealed storage, away from moisture *In solvent : -80°C, 6 months; -20°C, 1 month (sealed storage, away from moisture) |
| 溶解性数据 | In Vitro: DMSO : 100 mg/mL(532.74 mM;Need ultrasonic) H2O : ≥ 50 mg/mL(266.37 mM) *"≥" means soluble, but saturation unknown. 配制储备液 | 1 mM | 5.3274 mL | 26.6368 mL | 53.2737 mL | | 5 mM | 1.0655 mL | 5.3274 mL | 10.6547 mL | | 10 mM | 0.5327 mL | 2.6637 mL | 5.3274 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；一旦配成溶液，请分装保存，避免反复冻融造成的产品失效。
储备液的保存方式和期限：-80℃, 6 months; -20℃, 1 month (sealed storage, away from moisture)。-80℃ 储存时，请在 6 个月内使用，-20℃ 储存时，请在 1 个月内使用。 In Vivo: 请根据您的实验动物和给药方式选择适当的溶解方案。以下溶解方案都请先按照In Vitro方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，澄清的储备液可以根据储存条件，适当保存；体内实验的工作液，建议您现用现配，当天使用；
以下溶剂前显示的百
分比是指该溶剂在您配制终溶液中的体积占比；如在配制过程中出现沉淀、析出现象，可以通过加热和/或超声的方式助溶 1. 请依序添加每种溶剂： PBS Solubility: 6.88 mg/mL (36.65 mM); Clear solution; Need ultrasonic and warming and heat to 60℃
*以上所有助溶剂都可在本网站选购。 |
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