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Amantadine
本产品不向个人销售,仅用作科学研究,不用于任何人体实验及非科研性质的动物实验。
Amantadine图片
CAS NO:768-94-5

金刚烷胺
1-Adamantanamine
1-Aminoadamantane
Amantadine (1-Adamantanamine) 是一种口服有效的抗甲型流感 (influenza A) 病毒的抗病毒剂。Amantadine 对NMDAM2等多种离子通道均有抑制作用。Amantadine 还具有抗正痘病毒 (orthopoxvirus) 和抗癌活性。Amantadine 可用于帕金森病,术后认知功能障碍 (POCD) 和 COVID-19 的研究。
生物活性

Amantadine (1-Adamantanamine) is an orally avtive and potent antiviral agent with activity againstinfluenza Aviruses. Amantadine inhibits several ion channels such asNMDAandM2, and also inhibits Coronavirus ion channels. Amantadine also has anti-orthopoxvirusand anticancer activity. Amantadine can be used for Parkinson's disease, postoperative cognitive dysfunction (POCD) and COVID-19 research[1][2][3][4][5][6].

IC50& Target

CDK2

 

Bcl-2

 

Bax

 

体外研究
(In Vitro)

Amantadine (0-500 μM, 26 h) inhibits SARS-CoV-2 replication, with IC50concentrations between 83 and 119 μM[4].
Amantadine (0-100 μg/mL, 24-72 h) markedly inhibits the proliferation of HepG2 and SMMC-7721 cells[6].
Amantadine (0-75 μg/mL, 48 h) arrests the cell cycle at the G0/G1 phase and induces apoptosis[6].
Amantadine (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.
体内研究
(In Vivo)

Amantadine (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.
Clinical Trial
分子量

151.25

性状

Solid

Formula

C10H17N

CAS 号

768-94-5

中文名称

金刚烷胺

运输条件

Room temperature in continental US; may vary elsewhere.

储存方式

4°C, protect from light

*In solvent : -80°C, 6 months; -20°C, 1 month (protect from light)

溶解性数据
In Vitro: 

DMSO : 1 mg/mL(6.61 mM;ultrasonic and warming and heat to 60℃)

配制储备液
浓度溶剂体积质量1 mg5 mg10 mg
1 mM6.6116 mL33.0578 mL66.1157 mL
5 mM1.3223 mL6.6116 mL13.2231 mL
10 mM---------
*

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 (protect from light)。-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: 10% DMSO    40%PEG300   5%Tween-80   45% saline

    Solubility: ≥ 0.5 mg/mL (3.31 mM); Clear solution

    此方案可获得 ≥ 0.5 mg/mL (3.31 mM,饱和度未知) 的澄清溶液。

    以 1 mL 工作液为例,取 100 μL 5.0 mg/mL 的澄清 DMSO 储备液加到 400 μL PEG300 中,混合均匀;向上述体系中加入50 μL Tween-80,混合均匀;然后继续加入 450 μL生理盐水定容至 1 mL。

    将 0.9 g 氯化钠,完全溶解于 100 mL ddH2O 中,得到澄清透明的生理盐水溶液
  • 2.

    请依序添加每种溶剂: 10% DMSO    90% (20%SBE-β-CDin saline)

    Solubility: ≥ 0.5 mg/mL (3.31 mM); Clear solution

    此方案可获得 ≥ 0.5 mg/mL (3.31 mM,饱和度未知) 的澄清溶液。

    以 1 mL 工作液为例,取 100 μL 5.0 mg/mL 的澄清 DMSO 储备液加到 900 μL20% 的 SBE-β-CD 生理盐水水溶液中,混合均匀。

    将 2 g 磺丁基醚 β-环糊精加入 5 mL 生理盐水中,再用生理盐水定容至 10 mL,完全溶解,澄清透明
  • 3.

    请依序添加每种溶剂: 10% DMSO    90%corn oil

    Solubility: ≥ 0.5 mg/mL (3.31 mM); Clear solution

    此方案可获得 ≥ 0.5 mg/mL (3.31 mM,饱和度未知) 的澄清溶液,此方案不适用于实验周期在半个月以上的实验。

    以 1 mL 工作液为例,取 100 μL 5.0 mg/mL 的澄清 DMSO 储备液加到 900 μL玉米油中,混合均匀。

*以上所有助溶剂都可在本网站选购。
 
 
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