| Size | Price | Stock | Qty |
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| 50mg |
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| 100mg |
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| 250mg |
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| 500mg |
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| 1g |
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| Other Sizes |
Ajmaline (also known as Gilurytmal and Ritmos) is a natual alkaloid and a sodium channel blocker. It belongs to class Ia antiarrhythmic agent that can be used to treat arrhythmia. Ajmaline is also often used to bring out typical findings of ST elevations in patients suspected of having Brugada syndrome.
| ln Vitro |
Human embryonic kidney (HEK) cells expressing wild-type and mutant HERG channels were used in electrophysiological investigations, as were Xenopus laevis oocytes (two-electrode voltage clamp). With an IC50 of 1.0μM in HEK cells and 42.3μM in Xenopus oocytes, ajmaline inhibits HERG current [2].
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| References |
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| Additional Infomation |
Aymarin is an alkaloid found in the roots of Rauwolfia serpentina and other plant sources. It is a class Ia antiarrhythmic drug, its mechanism of action primarily involving altering the waveform and threshold of myocardial action potentials. Aymarin possesses potent sodium channel blocking activity and a very short half-life, making it well-suited for acute intravenous treatment. In some countries, aymarin is widely used to treat atrial fibrillation patients with Wolff-Parkinson-White syndrome and well-tolerated monomorphic ventricular tachycardia. Furthermore, it has been used for many years to treat bundle branch block and syncope to enhance cardiac conduction function. In these cases, abnormally prolonged HV intervals are considered evidence of subhistorical His bundle block, suggesting the need for a permanent pacemaker. Aymarin has been reported in Rauvolfia yunnanensis, Rauvolfia cubana, and other organisms with relevant data. Aymarin is an alkaloid found in the roots of Rauvolfia sperpentina and other plant sources. It is a class IA antiarrhythmic drug, and its mechanism of action appears to be through altering the waveform and threshold of the myocardial action potential. Drug Indications Used as an antiarrhythmic drug. Mechanism of Action Class I antiarrhythmic drugs interfere with sodium channels. Class IA drugs prolong the action potential (right shift), thereby improving abnormal heart rhythms. This drug has a high affinity for Nav1.5 sodium channels.
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| Molecular Formula |
C20H26N2O2
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|---|---|
| Molecular Weight |
326.44
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| Exact Mass |
326.199
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| CAS # |
4360-12-7
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| Related CAS # |
4410-48-4 (HCl);4360-12-7;
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| PubChem CID |
6100671
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| Appearance |
White to off-white solid powder
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| Density |
1.373g/cm3
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| Boiling Point |
519.406ºC at 760 mmHg
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| Melting Point |
189ºC
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| Flash Point |
285.155ºC
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| Index of Refraction |
1.701
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| LogP |
1.557
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| Hydrogen Bond Donor Count |
2
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| Hydrogen Bond Acceptor Count |
4
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| Rotatable Bond Count |
1
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| Heavy Atom Count |
24
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| Complexity |
570
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| Defined Atom Stereocenter Count |
9
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| SMILES |
CC[C@H]1[C@@H]2C[C@H]3[C@H]4[C@@]5(C[C@@H]([C@H]2[C@H]5O)N3[C@@H]1O)C6=CC=CC=C6N4C
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| InChi Key |
CJDRUOGAGYHKKD-KBPCXUENSA-N
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| InChi Code |
InChI=1S/C20H26N2O2/c1-3-10-11-8-14-17-20(12-6-4-5-7-13(12)21(17)2)9-15(16(11)18(20)23)22(14)19(10)24/h4-7,10-11,14-19,23-24H,3,8-9H2,1-2H3/t10-,11-,14-,15-,16-,17-,18+,19-,20+/m0/s1
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| Chemical Name |
(5aR,6S,8S,9S,10R,11S,11aS,12aR,13R)-9-ethyl-5-methyl-5a,6,8,9,10,11,11a,12-octahydro-5H-6,10
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| Synonyms |
TachmalinSiddiqui Takycor CardiorythmineNSC 15627 Rauwolfin (+)-Ajmaline Raugalline Rauwolfine Ritmos Gilurytmal Merabitol Ignazin Rhytmaton Rytmalin
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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 : ≥ 100 mg/mL (~306.34 mM)
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|---|---|
| Solubility (In Vivo) |
Solubility in Formulation 1: ≥ 2.5 mg/mL (7.66 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 (7.66 mM) (saturation unknown) in 10% DMSO + 90% (20% SBE-β-CD in 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 900 μL of 20% SBE-β-CD physiological saline solution and mix evenly. Preparation of 20% SBE-β-CD in Saline (4°C，1 week): Dissolve 2 g SBE-β-CD in 10 mL saline to obtain a clear solution. View More
Solubility in Formulation 3: ≥ 2.5 mg/mL (7.66 mM) (saturation unknown) in 10% DMSO + 90% Corn Oil (add these co-solvents sequentially from left to right, and one by one), clear solution. |
| Preparing Stock Solutions | 1 mg | 5 mg | 10 mg | |
| 1 mM | 3.0634 mL | 15.3168 mL | 30.6335 mL | |
| 5 mM | 0.6127 mL | 3.0634 mL | 6.1267 mL | |
| 10 mM | 0.3063 mL | 1.5317 mL | 3.0634 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 |
| NCT03491475 | Unknown status | Drug: Ajmaline test | Brugada Syndrome | Universitair Ziekenhuis Brussel | 2018-03-26 | |
| NCT04580992 | Unknown status | Drug: Ajmaline | Brugada Syndrome Cardiac Death Channelopathies Ventricular Fibrillation |
Universitair Ziekenhuis Brussel | 2020-11-16 | |
| NCT02933437 | Unknown status | Drug: Ajmaline | Brugada Syndrome Sudden Death |
St George's, University of London | 2017-10-22 | Phase 2 |
| NCT00702117 | Completed | Drug: flecainide Drug: ajmaline Drug: procainamide |
Atrial Fibrillation Brugada Syndrome Tachycardia, Ventricular |
Hospital Clinic of Barcelona | 2008-06 | Phase 4 |
| NCT03524079 | Completed | Drug: Ajmaline 17-(Chloroacetate) Monohydrochloride | Brugada Syndrome | IRCCS Policlinico S. Donato | 2018-04-19 |
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