| Size | Price | Stock | Qty |
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| 100mg |
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| 250mg | |||
| 500mg | |||
| Other Sizes |
| Targets |
Ethamivan targets the medullary respiratory center in the central nervous system. It acts as a respiratory stimulant (analeptic), increasing the rate and depth of respiration. The compound's precise molecular targets are not fully characterized but are believed to involve modulation of neurotransmitter systems in the brainstem that control breathing.
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| ln Vitro |
In vitro activity data for Ethamivan are limited in publicly available literature. As a respiratory stimulant, its effects are primarily studied in vivo. The compound may modulate neurotransmitter release or receptor activity in the brainstem. Specific in vitro potency data are not extensively documented.
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| ln Vivo |
In vivo, Ethamivan acts as a respiratory stimulant, increasing the rate and depth of respiration. It was previously used for the treatment of respiratory depression associated with drug overdose, COPD, and other conditions. The compound stimulates the medullary respiratory center, leading to increased ventilation. Its use has largely been replaced by newer respiratory stimulants and mechanical ventilation.
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| Enzyme Assay |
The in vitro receptor binding assay for Ethamivan would involve measuring its affinity for potential targets in the central nervous system. However, the compound's precise molecular targets are not well characterized. Radiolabeled ligand binding studies using brain membrane preparations could be performed to identify binding sites. Specific protocols are not documented in publicly available literature.
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| Cell Assay |
In vitro cellular assays for Ethamivan are not well documented in publicly available literature. The compound's effects are primarily studied in vivo. Potential cellular assays could involve measuring neurotransmitter release or neuronal activity in brainstem preparations. However, specific protocols are not available.
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| Animal Protocol |
In vivo animal experiments for Ethamivan typically use rodent models of respiratory depression. The compound is administered via intravenous or intraperitoneal routes at various doses. Respiratory rate, tidal volume, and blood gas parameters are measured. The compound's ability to reverse respiratory depression induced by drugs or hypoxia is assessed. Specific protocols are available from pharmacological studies of respiratory stimulants.
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| ADME/Pharmacokinetics |
Ethamivan has a molecular weight of 222.28 (C12H18N2O2). As a small molecule respiratory stimulant, it is administered intravenously and distributes into the central nervous system. The compound is metabolized in the liver and excreted via the kidneys. Specific PK parameters including half-life and clearance are available from historical pharmacology studies.
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| Toxicity/Toxicokinetics |
Ethamivan has been used clinically as a respiratory stimulant. Common adverse effects may include hypertension, tachycardia, anxiety, and seizures at high doses. The compound is contraindicated in patients with epilepsy or severe cardiovascular disease. Its use has declined due to the availability of safer and more effective respiratory stimulants and mechanical ventilation.
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| Additional Infomation |
Etamivan is a phenol with its C-2 and C-4 positions substituted with methoxy and N,N-diethylaminocarbonyl groups, respectively. It is a respiratory stimulant associated with nikethamide and is now largely discontinued. It belongs to the phenol and methoxybenzene classes of compounds. Etamivan (international nonproprietary name: INN; US nonproprietary name: Etamivan) is marketed under the trade name Analepticon. Etamivan is a respiratory stimulant similar to nikethamide and is currently discontinued in the United States.
Ethamivan (CAS#: 304-84-7) is a respiratory stimulant (analeptic) that acts on the medullary respiratory center to increase the rate and depth of respiration. It was previously used for the treatment of respiratory depression associated with drug overdose, COPD, and other conditions. Ethamivan's use has largely been replaced by newer therapies. The compound is not commonly used in modern clinical practice. |
| Molecular Formula |
C12H17NO3
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|---|---|
| Molecular Weight |
223.27
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| Exact Mass |
223.121
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| CAS # |
304-84-7
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| PubChem CID |
9363
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| Appearance |
White to off-white solid powder
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| Density |
1.115g/cm3
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| Boiling Point |
401.4ºC at 760mmHg
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| Melting Point |
96-97ºC
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| Flash Point |
196.6ºC
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| Index of Refraction |
1.536
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| LogP |
1.882
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| Hydrogen Bond Donor Count |
1
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| Hydrogen Bond Acceptor Count |
3
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| Rotatable Bond Count |
4
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| Heavy Atom Count |
16
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| Complexity |
228
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| Defined Atom Stereocenter Count |
0
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| SMILES |
O=C(N(CC)CC)C1=CC=C(O)C(OC)=C1
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| InChi Key |
BQJODPIMMWWMFC-UHFFFAOYSA-N
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| InChi Code |
InChI=1S/C12H17NO3/c1-4-13(5-2)12(15)9-6-7-10(14)11(8-9)16-3/h6-8,14H,4-5H2,1-3H3
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| Chemical Name |
N,N-diethyl-4-hydroxy-3-methoxybenzamide
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| Synonyms |
NSC-406087; NSC 406087; Analepticon, Etamivan, Ethamivan
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| HS Tariff Code |
2934.99.9001
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| 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)
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| Solubility (In Vitro) |
DMSO : ≥ 36 mg/mL (~161.24 mM)
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|---|---|
| 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 | 4.4789 mL | 22.3944 mL | 44.7888 mL | |
| 5 mM | 0.8958 mL | 4.4789 mL | 8.9578 mL | |
| 10 mM | 0.4479 mL | 2.2394 mL | 4.4789 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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