| Size | Price | Stock | Qty |
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| 50mg |
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| 100mg |
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| 250mg | |||
| Other Sizes |
| ln Vitro |
Almitrine decreases the open probability of Ca2+-dependent K+ channels with a high conductance (152±13 pS) in order to reduce their activity. This effect has an IC50 value of 0.22 μM. GH3 cells were found to exhibit the inhibitory action of Almitrine on Ca2+-dependent K+ channels. Even at doses up to 10 μM, almitrine has no effect on whole-cell voltage-dependent K+, Ca2+, or Na+ currents in rat or rabbit cells. On the other hand, in rat chemoreceptor cells, almitrine at this dosage dramatically suppressed the Ca2+-dependent component of K+ current [1].
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| ln Vivo |
Amitripline operates through peripheral arterial chemoreceptors to augment carotid sinus nerve output and minute ventilation. Almitrine also has pulmonary vasculature, inducing dose-dependent constriction and dilatation. Low doses of Almitrine augment hypoxic pulmonary vasoconstriction and may improve the overall ventilation/perfusion ratio [2].
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| References | |
| Additional Infomation |
Amitraline dimethylsulfonate is the dimethylsulfonate form of amitraline. It is a central nervous system stimulant containing amitraline. Amitraline mesylate is the mesylate form of amitraline, a diphenylmethylpiperazine derivative, which is also a respiratory stimulant used to improve oxygenation. After systemic administration, amitraline targets and binds to peripheral chemoreceptors located on the carotid body, thereby activating these receptors. This enhances respiration, increases arterial blood oxygen partial pressure, and decreases arterial blood carbon dioxide partial pressure. This respiratory stimulant enhances respiration by stimulating peripheral chemoreceptors located on the carotid body. This drug can increase arterial blood oxygen partial pressure in patients with chronic obstructive pulmonary disease (COPD) while decreasing arterial blood carbon dioxide partial pressure. It may also help treat nocturnal oxygen saturation without affecting sleep quality.
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| Molecular Formula |
C28H37F2N7O6S2
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|---|---|
| Molecular Weight |
669.7635
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| Exact Mass |
669.221
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| CAS # |
29608-49-9
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| Related CAS # |
29608-49-9 (mesylate);27469-53-0;
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| PubChem CID |
6918543
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| Appearance |
White to off-white solid powder
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| Boiling Point |
606.2ºC at 760 mmHg
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| Vapour Pressure |
1.21E-14mmHg at 25°C
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| LogP |
5.575
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| Hydrogen Bond Donor Count |
4
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| Hydrogen Bond Acceptor Count |
15
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| Rotatable Bond Count |
10
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| Heavy Atom Count |
45
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| Complexity |
694
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| Defined Atom Stereocenter Count |
0
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| InChi Key |
MRDBGMJEPGXQHJ-UHFFFAOYSA-N
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| InChi Code |
InChI=1S/C26H29F2N7.2CH4O3S/c1-3-13-29-24-31-25(30-14-4-2)33-26(32-24)35-17-15-34(16-18-35)23(19-5-9-21(27)10-6-19)20-7-11-22(28)12-8-20;2*1-5(2,3)4/h3-12,23H,1-2,13-18H2,(H2,29,30,31,32,33);2*1H3,(H,2,3,4)
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| Chemical Name |
6-[4-[bis(4-fluorophenyl)methyl]piperazin-1-yl]-2-N,4-N-bis(prop-2-enyl)-1,3,5-triazine-2,4-diamine;methanesulfonic acid
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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 Note: Please store this product in a sealed and protected environment, avoid exposure to moisture. |
| 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 : ~100 mg/mL (~149.31 mM)
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|---|---|
| Solubility (In Vivo) |
Solubility in Formulation 1: ≥ 2.5 mg/mL (3.73 mM) (saturation unknown) in 10% DMSO + 40% PEG300 + 5% Tween80 + 45% Saline (add these co-solvents sequentially from left to right, and one by one), clear solution.
For example, if 1 mL of working solution is to be prepared, you can add 100 μL of 25.0 mg/mL clear DMSO stock solution to 400 μL PEG300 and mix evenly; then add 50 μL Tween-80 to the above solution and mix evenly; then add 450 μL normal saline to adjust the volume to 1 mL. Preparation of saline: Dissolve 0.9 g of sodium chloride in 100 mL ddH₂ O to obtain a clear solution. Solubility in Formulation 2: ≥ 2.5 mg/mL (3.73 mM) (saturation unknown) in 10% DMSO + 90% Corn Oil (add these co-solvents sequentially from left to right, and one by one), clear solution. For example, if 1 mL of working solution is to be prepared, you can add 100 μL of 25.0 mg/mL clear DMSO stock solution to 900 μL of corn oil and mix evenly. (Please use freshly prepared in vivo formulations for optimal results.) |
| Preparing Stock Solutions | 1 mg | 5 mg | 10 mg | |
| 1 mM | 1.4931 mL | 7.4654 mL | 14.9307 mL | |
| 5 mM | 0.2986 mL | 1.4931 mL | 2.9861 mL | |
| 10 mM | 0.1493 mL | 0.7465 mL | 1.4931 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.
| NCT Number | Recruitment | interventions | Conditions | Sponsor/Collaborators | Start Date | Phases |
| NCT05216575 | Unknown status | Drug: Administration of Almitrine | ARDS Hypoxemia |
Centre Hospitalier Universitaire de Nice | 2021-01-01 | |
| NCT04380727 | Completed | COVID-19 Hypoxic Respiratory Failure |
Central Hospital, Nancy, France | 2020-03-20 | ||
| NCT04357457 | Completed | Drug: Almitrine Drug: Placebo |
Covid 19 Hypoxemic Respiratory Failure |
Assistance Publique - Hôpitaux de Paris | 2020-09-03 | Phase 3 |
| NCT06322758 | Not yet recruiting | Other: Tidal volume customization in the acute respiratory distress syndrome |
Acute Respiratory Distress Syndrome ARDS |
Assistance Publique - Hôpitaux de Paris | 2024-09-01 | Not Applicable |
| NCT05193526 | Active, not recruiting | Other: No intervention | Acute Respiratory Distress Syndrome Related to SARS-CoV-2 |
Centre Hospitalier Intercommunal Creteil | 2021-11-15 |
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