| Size | Price | Stock | Qty |
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| 50mg |
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| 100mg |
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| 250mg | |||
| Other Sizes |
| Targets |
Peripheral chemoreceptors on carotid bodies; Ca2+-dependent K+ channel. Almitrine Dimesylate acts as an agonist of peripheral chemoreceptors located on the carotid bodies, thereby stimulating the respiratory system. Additionally, it inhibits the activity of Ca2+-dependent K+ channels by decreasing their open probability, with an IC50 of 0.22 µM. This dual mechanism contributes to its respiratory stimulant effects.
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| 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].
Almitrine Dimesylate inhibits Ca2+-dependent K+ channel activity in vitro with an IC50 of 0.22 µM. It has been shown to selectively inhibit K+ channels in rat chemoreceptor cells. The compound acts as an agonist at peripheral chemoreceptors, enhancing respiratory drive. Its in vitro potency and selectivity have been characterized in various electrophysiological and binding assays. The compound is soluble in DMSO and ethanol but insoluble in water. |
| 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].
In vivo, Almitrine Dimesylate enhances respiration by acting on carotid body chemoreceptors. In patients with chronic obstructive pulmonary disease, the drug increases arterial oxygen tension while decreasing arterial carbon dioxide tension. It is used therapeutically for hypoxic chronic pulmonary diseases. The compound has been shown to improve gas exchange and reduce hypoxemia in clinical settings. Its effects on ventilation and blood gases have been well documented in both animal models and human studies. |
| Enzyme Assay |
In vitro assays for Almitrine Dimesylate typically involve patch-clamp electrophysiology to measure K+ channel activity. Chemoreceptor cells are isolated from rat carotid bodies and cultured. The compound is applied at varying concentrations, and changes in channel open probability are recorded. The IC50 for Ca2+-dependent K+ channel inhibition is determined to be 0.22 µM. Receptor binding assays may also be performed using radiolabeled ligands to assess affinity for peripheral chemoreceptor sites.
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| Cell Assay |
In vitro cell-based assays are not commonly reported for Almitrine Dimesylate, as its primary mechanism involves direct action on chemoreceptor cells and ion channels. However, chemoreceptor cell cultures from carotid bodies may be used to assess the compound's effects on cellular excitability and neurotransmitter release. Electrophysiological recordings are the primary method for evaluating its activity at the cellular level. Cells are typically maintained in appropriate culture media and studied using patch-clamp techniques.
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| Animal Protocol |
In vivo animal studies for Almitrine Dimesylate have been conducted in various species, including rats and dogs, to evaluate its respiratory stimulant effects. The compound is typically administered orally or intravenously. Arterial blood gas measurements are taken to assess changes in oxygen and carbon dioxide tensions. Doses are optimized to achieve therapeutic effects without significant toxicity. The compound has also been studied in animal models of hypoxic respiratory failure.
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| ADME/Pharmacokinetics |
Almitrine Dimesylate is soluble in DMSO (100 mg/mL) and ethanol (100 mg/mL) but insoluble in water. For in vivo administration, it can be formulated as a homogeneous suspension using CMC-Na at concentrations ≥5 mg/mL. The molecular weight is 669.76. Detailed pharmacokinetic parameters such as half-life, volume of distribution, and clearance are not extensively documented in publicly available sources. The compound is intended for research use only and not for therapeutic purposes.
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| Toxicity/Toxicokinetics |
Toxicological data for Almitrine Dimesylate are limited in publicly available sources. The compound is intended for research use only and is not approved for human therapeutic applications. Standard safety precautions should be taken when handling the compound. It should be stored as a powder at -20°C for up to 3 years or at 4°C for up to 2 years. In solvent, it can be stored at -80°C for up to 2 years or at -20°C for up to 1 year.
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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.
Almitrine Dimesylate is a respiratory stimulant that acts as an agonist of peripheral chemoreceptors on the carotid bodies. It also inhibits Ca2+-dependent K+ channels with an IC50 of 0.22 µM. The drug has been used clinically for hypoxic chronic pulmonary diseases but is now primarily a research tool. It is not approved for therapeutic use in many countries and is available only for research purposes. Synonyms include Almitrine bismesylate and Vectarion. |
| 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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