1. Anti-infection Autophagy
  2. Influenza Virus Autophagy
  3. Rimantadine

Rimantadine (1-Rimantadine) is an orally active inhibitor for M2 protein, which blocks the hydrogen ion channel activity, prevents the entry and replication of the virus, and exhibits board-spectrum antiviral activity. Rimantadine significantly inhibits hepatitis A virus (HAV) replication at the post-entry stage in Huh7 cells. Rimantadine enhances autophagy. Rimantadine has a significant protective effect against H3N2 virus in mouse model.

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Rimantadine

Rimantadine Chemical Structure

CAS No. : 13392-28-4

Size Price Stock Quantity
Liquid + Solvent (Highly Recommended)
10 mM * 1 mL in DMSO
ready for reconstitution
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10 mM * 1 mL in DMSO In-stock
Liquid
10 mg In-stock
25 mg In-stock
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100 mg   Get quote  

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Description

Rimantadine (1-Rimantadine) is an orally active inhibitor for M2 protein, which blocks the hydrogen ion channel activity, prevents the entry and replication of the virus, and exhibits board-spectrum antiviral activity. Rimantadine significantly inhibits hepatitis A virus (HAV) replication at the post-entry stage in Huh7 cells. Rimantadine enhances autophagy. Rimantadine has a significant protective effect against H3N2 virus in mouse model[1][2].

In Vitro

Rimantadine (0-10 μg/mL, 72 h) inhibits the HAV subgenomic replicon and HAV replication in Huh7 and IHH cells infected with HAV HA11-1299 genotype IIIA[1].
Rimantadine (0-10 μg/mL, 48 h) significantly inhibits HAV HM175 genotype IB subgenomic replicon replication dose-dependently in HuhT7 cells[1].
Rimantadine (10 μg/mL, 1 h) significantly inhibits HAV HA11-1299 genotype IIA replication at the post-entry stage in Huh7 cells[1].
Rimantadine (10 μg/mL, 48 h) enhances the expression of LC3, increases the number of lysosomes, and stimulates the fusion of lysosomes and autophagosomes in Huh7 cells[1].

MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.

Cell Autophagy Assay[1]

Cell Line: HAV-infected Huh7 cell
Concentration: 0-10 μg/mL
Incubation Time: 72 h
Result: Induced autophagy.

RT-PCR[1]

Cell Line: HAV-infected Huh7 cell
Concentration: 10 μg/mL
Incubation Time: 1 h
Result: Significantly inhibited HAV replication both at full-time and at post-entry stages by 60% and 70% respectively.

Western Blot Analysis[1]

Cell Line: HAV-infected Huh7 cell
Concentration: 10 μg/mL
Incubation Time: 72 h
Result: Upregulated the expression of LC3A and LC3B.
Inhibited the expression and phosphorylation of mTOR in HAV-infected Huh7 cells.
In Vivo

Rimantadine (5-20 mg/kg/day, p.o., twice daily for 5 d) prolongs survival of ICR mice infected with influenza A (H3N2) virus in combination with Oseltamivir (HY-13317)[2].
Rimantadine (5-10 mg/kg/day, p.o., twice daily for 5 d) reduces the lung viral titers of ICR mice infected with influenza A (H3N2) virus in combination with Oseltamivir[2].

MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.

Animal Model: Male white ICR mice infected with influenza A (H3N2) virus[2]
Dosage: 5, 10, 20, 40 or 80 mg/kg/day
Administration: Intraperitoneal injection (i.p.) twice daily for 5 d
Result: Fully protected infected animals with 80 mg/kg/day incombination with 10 mg/kg/day Oseltamivir.
Decreased the infectious virus content.
Clinical Trial
Molecular Weight

179.30

Formula

C12H21N

CAS No.
Appearance

Liquid (Density: 1.033±0.06 g/cm3)

Color

Colorless to light yellow

SMILES

CC(C1(C[C@H](C2)C3)C[C@H]3C[C@H]2C1)N

Shipping

Room temperature in continental US; may vary elsewhere.

Storage

-20°C, protect from light

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

Solvent & Solubility
In Vitro: 

DMSO : 25 mg/mL (139.43 mM; ultrasonic and warming and heat to 60°C; Hygroscopic DMSO has a significant impact on the solubility of product, please use newly opened DMSO)

Preparing
Stock Solutions
Concentration Solvent Mass 1 mg 5 mg 10 mg
1 mM 5.5772 mL 27.8862 mL 55.7724 mL
5 mM 1.1154 mL 5.5772 mL 11.1545 mL
View the Complete Stock Solution Preparation Table

* Please refer to the solubility information to select the appropriate solvent. Once prepared, please aliquot and store the solution to prevent product inactivation from repeated freeze-thaw cycles.
Storage method and period of stock solution: -80°C, 6 months; -20°C, 1 month (protect from light). When stored at -80°C, please use it within 6 months. When stored at -20°C, please use it within 1 month.

  • Molarity Calculator

  • Dilution Calculator

Mass (g) = Concentration (mol/L) × Volume (L) × Molecular Weight (g/mol)

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Concentration (start) × Volume (start) = Concentration (final) × Volume (final)

This equation is commonly abbreviated as: C1V1 = C2V2

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In Vivo:

Select the appropriate dissolution method based on your experimental animal and administration route.

For the following dissolution methods, please ensure to first prepare a clear stock solution using an In Vitro approach and then sequentially add co-solvents:
To ensure reliable experimental results, the clarified stock solution can be appropriately stored based on storage conditions. As for the working solution for in vivo experiments, it is recommended to prepare freshly and use it on the same day.
The percentages shown for the solvents indicate their volumetric ratio in the final prepared solution. If precipitation or phase separation occurs during preparation, heat and/or sonication can be used to aid dissolution.

  • Protocol 1

    Add each solvent one by one:  10% DMSO    40% PEG300    5% Tween-80    45% Saline

    Solubility: ≥ 2.5 mg/mL (13.94 mM); Clear solution

    This protocol yields a clear solution of ≥ 2.5 mg/mL (saturation unknown).

    Taking 1 mL working solution as an example, add 100 μL DMSO stock solution (25.0 mg/mL) to 400 μL PEG300, and mix evenly; then add 50 μL Tween-80 and mix evenly; then add 450 μL Saline to adjust the volume to 1 mL.

    Preparation of Saline: Dissolve 0.9 g sodium chloride in ddH₂O and dilute to 100 mL to obtain a clear Saline solution.
  • Protocol 2

    Add each solvent one by one:  10% DMSO    90% (20% SBE-β-CD in Saline)

    Solubility: ≥ 2.5 mg/mL (13.94 mM); Clear solution

    This protocol yields a clear solution of ≥ 2.5 mg/mL (saturation unknown).

    Taking 1 mL working solution as an example, add 100 μL DMSO stock solution (25.0 mg/mL) to 900 μL 20% SBE-β-CD in Saline, and mix evenly.

    Preparation of 20% SBE-β-CD in Saline (4°C, storage for one week): 2 g SBE-β-CD powder is dissolved in 10 mL Saline, completely dissolve until clear.
In Vivo Dissolution Calculator
Please enter the basic information of animal experiments:

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Recommended: Prepare an additional quantity of animals to account for potential losses during experiments.
Please enter your animal formula composition:
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Recommended: Keep the proportion of DMSO in working solution below 2% if your animal is weak.
The co-solvents required include: DMSO, . All of co-solvents are available by MedChemExpress (MCE). , Tween 80. All of co-solvents are available by MedChemExpress (MCE).
Calculation results:
Working solution concentration: mg/mL
Method for preparing stock solution: mg drug dissolved in μL  DMSO (Stock solution concentration: mg/mL).

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

The concentration of the stock solution you require exceeds the measured solubility. The following solution is for reference only. If necessary, please contact MedChemExpress (MCE).
Method for preparing in vivo working solution for animal experiments: Take μL DMSO stock solution, add μL . μL , mix evenly, next add μL Tween 80, mix evenly, then add μL Saline.
 If the continuous dosing period exceeds half a month, please choose this protocol carefully.
Please ensure that the stock solution in the first step is dissolved to a clear state, and add co-solvents in sequence. You can use ultrasonic heating (ultrasonic cleaner, recommended frequency 20-40 kHz), vortexing, etc. to assist dissolution.
Purity & Documentation
References

Complete Stock Solution Preparation Table

* Please refer to the solubility information to select the appropriate solvent. Once prepared, please aliquot and store the solution to prevent product inactivation from repeated freeze-thaw cycles.
Storage method and period of stock solution: -80°C, 6 months; -20°C, 1 month (protect from light). When stored at -80°C, please use it within 6 months. When stored at -20°C, please use it within 1 month.

Optional Solvent Concentration Solvent Mass 1 mg 5 mg 10 mg 25 mg
DMSO 1 mM 5.5772 mL 27.8862 mL 55.7724 mL 139.4311 mL
5 mM 1.1154 mL 5.5772 mL 11.1545 mL 27.8862 mL
10 mM 0.5577 mL 2.7886 mL 5.5772 mL 13.9431 mL
15 mM 0.3718 mL 1.8591 mL 3.7182 mL 9.2954 mL
20 mM 0.2789 mL 1.3943 mL 2.7886 mL 6.9716 mL
25 mM 0.2231 mL 1.1154 mL 2.2309 mL 5.5772 mL
30 mM 0.1859 mL 0.9295 mL 1.8591 mL 4.6477 mL
40 mM 0.1394 mL 0.6972 mL 1.3943 mL 3.4858 mL
50 mM 0.1115 mL 0.5577 mL 1.1154 mL 2.7886 mL
60 mM 0.0930 mL 0.4648 mL 0.9295 mL 2.3239 mL
80 mM 0.0697 mL 0.3486 mL 0.6972 mL 1.7429 mL
100 mM 0.0558 mL 0.2789 mL 0.5577 mL 1.3943 mL
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Help & FAQs
  • Do most proteins show cross-species activity?

    Species cross-reactivity must be investigated individually for each product. Many human cytokines will produce a nice response in mouse cell lines, and many mouse proteins will show activity on human cells. Other proteins may have a lower specific activity when used in the opposite species.

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Rimantadine
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