| Size | Price | Stock | Qty |
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| 25mg |
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| 250mg |
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| 1g |
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Purity: ≥98%
Dronedarone HCl (formerly SR-33589; D4689; W3083; D03914; S-7529; RL01735), the hydrochloride salt of dronedarone, is a non-iodinated amiodarone analog approved for the treatment for Atrial fibrillation (AF). Dronedarone acts as a multichannel blocker targeting several ion channels such as potassium channel, sodium channel and calcium channel.
| ln Vitro |
Dronedarone (SR-33589) is a multichannel blocker for atrial fibrillation. It is a powerful inhibitor of the acetylcholine-activated K+ current from atrial and sinoatrial nodal tissue, and inhibits the rapid delayed rectifier more potently than slow and inward rectifier K+ currents and inhibits L-type calcium current. Under whole-cell patch clamp, it blocks IKr (IC50=3 μM) and ICa-L (IC50=0.18 μM). The effects on ICa-L are use- and frequency-dependent. Dronedarone suppresses current carried by human ether-a-go-go gene (HERG)-expressing oocytes (analagous to IKr) with an IC50 of 9 μM[1]. In guinea pig ventricular myocytes, dronedarone demonstrates a state dependent suppression of the fast Na+ channel current with an IC50 of 0.7±0.1 μM, when the holding potential is −80 mV[2].
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| ln Vivo |
At 3 mg/kg IV, the incidence of ventricular fibrillation (VF) is considerably reduced from 80 to 30% (p < 0.05) and at 10 mg/kg IV, both VF and mortality are eliminated [3]. In vivo carotid artery thrombus development was reduced by dronedarone. Dronedarone-treated animals show decreased expression of plasminogen activator inhibitor-1 (PAI1), an inhibitor of the fibrinolytic pathway, in the artery wall and impaired thrombin- and collagen-induced platelet aggregation (P<0.05)[4].
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| Animal Protocol |
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| References |
[1]. Bogdan R, et al. Effect of?dronedarone?on Na+, Ca2+ and HCN channels. Naunyn Schmiedebergs Arch Pharmacol.?2011 Apr;383(4):347-56.?
[2]. Doggrell SA, et al. Dronedarone: an amiodarone analogue. Expert Opin Investig Drugs. 2004 Apr;13(4):415-26. [3]. Manning AS, et al. SR 33589, a new amiodarone-like agent: effect on ischemia- and reperfusion-induced arrhythmias in anesthetized rats. J Cardiovasc Pharmacol. 1995 Sep;26(3):453-61. [4]. Breitenstein A, et al. Dronedarone reduces arterial thrombus formation. Basic Res Cardiol. 2012 Nov;107(6):302 |
| Molecular Formula |
C31H44N2O5S.HCL
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| Molecular Weight |
593.22
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| CAS # |
141625-93-6
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| Related CAS # |
Dronedarone;141626-36-0
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| SMILES |
Cl[H].S(C([H])([H])[H])(N([H])C1C([H])=C([H])C2=C(C=1[H])C(C(C1C([H])=C([H])C(=C([H])C=1[H])OC([H])([H])C([H])([H])C([H])([H])N(C([H])([H])C([H])([H])C([H])([H])C([H])([H])[H])C([H])([H])C([H])([H])C([H])([H])C([H])([H])[H])=O)=C(C([H])([H])C([H])([H])C([H])([H])C([H])([H])[H])O2)(=O)=O
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| InChi Key |
DWKVCQXJYURSIQ-UHFFFAOYSA-N
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| InChi Code |
InChI=1S/C31H44N2O5S.ClH/c1-5-8-12-29-30(27-23-25(32-39(4,35)36)15-18-28(27)38-29)31(34)24-13-16-26(17-14-24)37-22-11-21-33(19-9-6-2)20-10-7-3;/h13-18,23,32H,5-12,19-22H2,1-4H3;1H
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| Chemical Name |
N-[2-butyl-3-[4-[3-(dibutylamino)propoxy]benzoyl]-1-benzofuran-5-yl]methanesulfonamide;hydrochlorideInChi Key: DWKVCQXJYURSIQ-UHFFFAOYSA-N
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| Synonyms |
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| Storage |
Powder -20°C 3 years 4°C 2 years In solvent -80°C 6 months -20°C 1 month |
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| 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) |
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| Solubility (In Vivo) |
Solubility in Formulation 1: ≥ 2.5 mg/mL (4.21 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 (4.21 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 (4.21 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 | 1.6857 mL | 8.4286 mL | 16.8572 mL | |
| 5 mM | 0.3371 mL | 1.6857 mL | 3.3714 mL | |
| 10 mM | 0.1686 mL | 0.8429 mL | 1.6857 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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