| Size | Price | |
|---|---|---|
| 500mg | ||
| 1g | ||
| Other Sizes |
| ln Vitro |
The suppression of SARS-CoV-2 replication by amantadine sulfate (0-500 µM, 26 hours) ranges in IC50 values from 83 to 119 µM [4]. The growth of HepG2 and SMMC-7721 cells is markedly inhibited by amantadine sulfate (0-100 µg/mL, 24-72 hours) [6]. Inducing apoptosis, amantadine sulfate (0-75 µg/mL, 48 hours) stops the cell cycle in the G0/G1 phase [6]. In 48 hours, amantadine sulfate (0-75 µg/mL) decreases Bcl-2, increases Bax protein and mRNA levels, and decreases cell cycle-related genes and proteins (cyclin D1, cyclin E, and CDK2) [6].
|
|---|---|
| ln Vivo |
Amantadine sulfate (25 mg/kg, IP, once day for 3 days) can reduce surgery-induced neuroinflammation and learning and memory deficits [5].
|
| Cell Assay |
Cell Viability Assay[4]
Cell Types: Vero E6 Cell Tested Concentrations: 500 µM, 100 µM, 20 µM, 4 µM and 8 nM Incubation Duration: 26 hrs (hours) Experimental Results: Causes concentration-dependent reduction of virus (IC50=83 µM) 26 post-infection The nucleic acid concentration in the supernatant is 10-500 µM. Results in a concentration-dependent reduction of viral nucleic acid in the cytoplasm (IC50=119 µM) 26 hrs (hours) post-infection. Cell proliferation assay[6] Cell Types: Human HCC cell lines (HepG2 and SMMC-7721) and normal liver cells (L02 cells) Tested Concentrations: 0, 1, 2, 5, 10, 25, 50 and 100 µg/mL Incubation Duration: 24, 48 and 72 hrs (hours) Experimental Results: Inhibited cell proliferation in a time- and dose-dependent manner in HepG2 and SMMC-7721 cells. Cell cycle analysis[6] Cell Types: HepG2 and SMMC-7721 Cell Tested Concentrations: 0, 10, 25, 50 and 75 µg/mL Incubation Duration: 48 hrs (hours) Experimental Results: Significant increase in the number of HepG2 and SMMC-7721 cells in G0/G1 phase in a dose-dependent manner, and Dramatically diminished the numbe |
| Animal Protocol |
Animal/Disease Models: Fischer 344 rats (4 months old, male, 290-330 g, 15 rats per group) [5]
Doses: 25 mg/kg Route of Administration: IP, one time/day for 3 days (first dose in 15 minutes before administration) Experimental Results: Inhibited surgery-induced neuroinflammation and learning and memory impairment, increased GDNF (glial cell line-derived neuronal neuron) co-localized with hippocampal glial fibrillary acidic protein (an astrocyte marker) nutritional factors). |
| References | |
| Additional Infomation |
Amantadine sulfate is an alkylammonium sulfate salt obtained by combining amantadine and sulfuric acid in a 2:1 ratio. Used as an antiviral and antiparkinson drug. It has a role as an antiparkinson drug, an antiviral drug, a dopaminergic agent, a NMDA receptor antagonist and a non-narcotic analgesic. It contains an adamantan-1-aminium.
Amantadine Sulfate is the sulfate salt of amantadine, a synthetic tricyclic amine with antiviral, antiparkinsonian, and antihyperalgesic activities. Amantadine appears to exert its antiviral effect against the influenza A virus by interfering with the function of the transmembrane domain of the viral M2 protein, thereby preventing the release of infectious viral nucleic acids into host cells; furthermore, this agent prevents virus assembly during virus replication. Amantadine exerts its antiparkinsonian effects by stimulating the release of dopamine from striatal dopaminergic nerve terminals and inhibiting its pre-synaptic reuptake. This agent may also exert some anticholinergic effect through inhibition of N-methyl-D-aspartic acid (NMDA) receptor-mediated stimulation of acetylcholine, resulting in antihyperalgesia. An antiviral that is used in the prophylactic or symptomatic treatment of influenza A. It is also used as an antiparkinsonian agent, to treat extrapyramidal reactions, and for postherpetic neuralgia. The mechanisms of its effects in movement disorders are not well understood but probably reflect an increase in synthesis and release of dopamine, with perhaps some inhibition of dopamine uptake. |
| Molecular Formula |
C10H17N.H2O4S
|
|---|---|
| Molecular Weight |
249.32716
|
| Exact Mass |
400.239
|
| CAS # |
31377-23-8
|
| Related CAS # |
Amantadine;768-94-5;Amantadine hydrochloride;665-66-7
|
| PubChem CID |
124108
|
| Appearance |
Typically exists as solid at room temperature
|
| Density |
1.066g/cm3
|
| Boiling Point |
225.7ºC at 760 mmHg
|
| Melting Point |
300 °C
|
| Flash Point |
96ºC
|
| LogP |
5.656
|
| Hydrogen Bond Donor Count |
4
|
| Hydrogen Bond Acceptor Count |
6
|
| Rotatable Bond Count |
0
|
| Heavy Atom Count |
27
|
| Complexity |
225
|
| Defined Atom Stereocenter Count |
0
|
| SMILES |
S(O)(O)(=O)=O.C12(N)CC3CC(CC(C3)C1)C2
|
| InChi Key |
MYWTWSQFJLXGGQ-UHFFFAOYSA-N
|
| InChi Code |
InChI=1S/2C10H17N.H2O4S/c2*11-10-4-7-1-8(5-10)3-9(2-7)6-10;1-5(2,3)4/h2*7-9H,1-6,11H2;(H2,1,2,3,4)
|
| Chemical Name |
adamantan-1-amine;sulfuric acid
|
| HS Tariff Code |
2934.99.9001
|
| Storage |
Powder -20°C 3 years 4°C 2 years In solvent -80°C 6 months -20°C 1 month |
| Shipping Condition |
Room temperature (This product is stable at ambient temperature for a few days during ordinary shipping and time spent in Customs)
|
| Solubility (In Vitro) |
May dissolve in DMSO (in most cases), if not, try other solvents such as H2O, Ethanol, or DMF with a minute amount of products to avoid loss of samples
|
|---|---|
| Solubility (In Vivo) |
Note: Listed below are some common formulations that may be used to formulate products with low water solubility (e.g. < 1 mg/mL), you may test these formulations using a minute amount of products to avoid loss of samples.
Injection Formulations
Injection Formulation 1: DMSO : Tween 80： Saline = 10 : 5 : 85 (i.e. 100 μL DMSO stock solution → 50 μL Tween 80 → 850 μL Saline)(e.g. IP/IV/IM/SC) *Preparation of saline: Dissolve 0.9 g of sodium chloride in 100 mL ddH ₂ O to obtain a clear solution. Injection Formulation 2: DMSO : PEG300 ：Tween 80 : Saline = 10 : 40 : 5 : 45 (i.e. 100 μL DMSO → 400 μLPEG300 → 50 μL Tween 80 → 450 μL Saline) Injection Formulation 3: DMSO : Corn oil = 10 : 90 (i.e. 100 μL DMSO → 900 μL Corn oil) Example: Take the Injection Formulation 3 (DMSO : Corn oil = 10 : 90) as an example, if 1 mL of 2.5 mg/mL working solution is to be prepared, you can take 100 μL 25 mg/mL DMSO stock solution and add to 900 μL corn oil, mix well to obtain a clear or suspension solution (2.5 mg/mL, ready for use in animals). View More
Injection Formulation 4: DMSO : 20% SBE-β-CD in saline = 10 : 90 [i.e. 100 μL DMSO → 900 μL (20% SBE-β-CD in saline)] Oral Formulations
Oral Formulation 1: Suspend in 0.5% CMC Na (carboxymethylcellulose sodium) Oral Formulation 2: Suspend in 0.5% Carboxymethyl cellulose Example: Take the Oral Formulation 1 (Suspend in 0.5% CMC Na) as an example, if 100 mL of 2.5 mg/mL working solution is to be prepared, you can first prepare 0.5% CMC Na solution by measuring 0.5 g CMC Na and dissolve it in 100 mL ddH2O to obtain a clear solution; then add 250 mg of the product to 100 mL 0.5% CMC Na solution, to make the suspension solution (2.5 mg/mL, ready for use in animals). View More
Oral Formulation 3: Dissolved in PEG400 (Please use freshly prepared in vivo formulations for optimal results.) |
| Preparing Stock Solutions | 1 mg | 5 mg | 10 mg | |
| 1 mM | 4.0107 mL | 20.0537 mL | 40.1075 mL | |
| 5 mM | 0.8021 mL | 4.0107 mL | 8.0215 mL | |
| 10 mM | 0.4011 mL | 2.0054 mL | 4.0107 mL |
*Note: Please select an appropriate solvent for the preparation of stock solution based on your experiment needs. For most products, DMSO can be used for preparing stock solutions (e.g. 5 mM, 10 mM, or 20 mM concentration); some products with high aqueous solubility may be dissolved in water directly. Solubility information is available at the above Solubility Data section. Once the stock solution is prepared, aliquot it to routine usage volumes and store at -20°C or -80°C. Avoid repeated freeze and thaw cycles.
Calculation results
Working concentration： mg/mL；
Method for preparing DMSO stock solution： mg drug pre-dissolved in μL DMSO (stock solution concentration mg/mL). Please contact us first if the concentration exceeds the DMSO solubility of the batch of drug.
Method for preparing in vivo formulation:：Take μL DMSO stock solution, next add μL PEG300, mix and clarify, next addμL Tween 80, mix and clarify, next add μL ddH2O，mix and clarify.
(1) Please be sure that the solution is clear before the addition of next solvent. Dissolution methods like vortex, ultrasound or warming and heat may be used to aid dissolving.
(2) Be sure to add the solvent(s) in order.
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