| Size | Price | Stock | Qty |
|---|---|---|---|
| 5mg |
|
||
| 10mg | |||
| Other Sizes |
| Targets |
Budiodarone targets multiple cardiac ion channels, primarily potassium, sodium, and calcium channels, to exert its antiarrhythmic effects. By inhibiting these channels, it modulates the cardiac action potential, prolonging repolarization and stabilizing the electrical activity of the heart. This balanced, multi-channel inhibition is characteristic of amiodarone and its analogs, distinguishing them from other antiarrhythmic agents that typically target a single channel type.
|
|---|---|
| ln Vitro |
The half-life of briodalone (ATI-2042) tartrate flower is only 7 hours, and its distribution volume is only 13 L/kg [1].
The in vitro activity of Budiodarone is characterized by its ability to inhibit cardiac ion channels. As an amiodarone analog, it exhibits balanced blocking activity against potassium, sodium, and calcium channels in isolated cell systems. This multi-channel blockade is responsible for its Class III antiarrhythmic effects, which include prolongation of the action potential duration and refractory period. Its activity is typically assessed using patch-clamp techniques on various cardiac cell lines. |
| ln Vivo |
In vivo, Budiodarone has shown antiarrhythmic efficacy in animal models and clinical studies. It has demonstrated a reduction in atrial fibrillation burden in phase 2 clinical trials. Its shorter plasma half-life (approximately 7 hours) and smaller volume of distribution (13 L/kg) compared to amiodarone suggest a more predictable pharmacokinetic profile and potentially faster offset of action, which may translate to a better safety profile in vivo.
|
| Enzyme Assay |
The in vitro activity of Budiodarone on cardiac ion channels is typically assessed using electrophysiological techniques. In a standard cell-free or cell-based assay, human embryonic kidney (HEK) cells expressing specific ion channels (e.g., hERG for potassium channels) are used. Cells are voltage-clamped, and the effect of increasing concentrations of Budiodarone on the ion current is measured. The half-maximal inhibitory concentration (IC50) for each channel type is then determined.
|
| Cell Assay |
Cellular assays for Budiodarone involve studying its effects on cardiac myocytes or cell lines expressing cardiac ion channels. A typical protocol uses a patch-clamp technique in the whole-cell configuration. Cells are superfused with a physiological solution, and a recording electrode is used to measure ion currents. Budiodarone is applied at various concentrations, and the percent inhibition of the specific ion current (e.g., IKr, INa, ICa) is calculated to determine its potency.
|
| Animal Protocol |
The in vivo efficacy of Budiodarone has been evaluated in animal models of atrial fibrillation, such as sterile pericarditis models in canines or rapid atrial pacing models. In these models, Budiodarone is administered intravenously or orally. The primary endpoint is the reduction in the duration and frequency of atrial fibrillation episodes, measured via continuous electrocardiogram (ECG) recording. These studies help establish the dose-response relationship and efficacy profile.
|
| ADME/Pharmacokinetics |
Budiodarone tartrate has a molecular weight of 1135.4 and a molecular formula of C₃₁H₃₇I₂NO₁₁. It is typically supplied as a tartrate salt with high purity for research and clinical-trial use. Its solubility is greater than 100 mg/mL in DMSO. In vivo, it has a relatively short plasma half-life of approximately 7 hours and a small volume of distribution of 13 L/kg, which contrasts with the very long half-life of amiodarone.
|
| Toxicity/Toxicokinetics |
The safety and toxicity of Budiodarone have been evaluated in preclinical and clinical studies. As an ion channel inhibitor, its primary toxicity is related to its antiarrhythmic mechanism, with potential proarrhythmic effects, including the risk of Torsades de Pointes, which is a concern for all Class III antiarrhythmic agents. Phase 2 clinical trials have been designed to assess its safety and tolerability, with the goal of demonstrating a favorable risk-benefit profile compared to amiodarone.
|
| References | |
| Additional Infomation |
Budiodarone (ATI-2042) is a novel antiarrhythmic agent developed as a chemical analog of amiodarone. It has shown promising Phase 2 results in reducing atrial fibrillation burden. Its shorter half-life is a key differentiator from amiodarone, potentially allowing for more flexible dosing and easier management of side effects. The compound was investigated in clinical trials, including the PASCAL study, for the treatment of paroxysmal atrial fibrillation.
|
| Molecular Formula |
C31H37I2NO11
|
|---|---|
| Molecular Weight |
853.434534788132
|
| Exact Mass |
853.045
|
| CAS # |
478941-93-4
|
| Related CAS # |
Budiodarone;335148-45-3
|
| PubChem CID |
25227360
|
| Appearance |
White to yellow solid powder
|
| Hydrogen Bond Donor Count |
4
|
| Hydrogen Bond Acceptor Count |
12
|
| Rotatable Bond Count |
16
|
| Heavy Atom Count |
45
|
| Complexity |
812
|
| Defined Atom Stereocenter Count |
3
|
| SMILES |
CC[C@H](C)OC(=O)CC1=C(C2=CC=CC=C2O1)C(=O)C3=CC(=C(C(=C3)I)OCCN(CC)CC)I.[C@@H]([C@H](C(=O)O)O)(C(=O)O)O
|
| InChi Key |
CAMFTHAPYYLIIG-YRSVLNEHSA-N
|
| InChi Code |
InChI=1S/C27H31I2NO5.C4H6O6/c1-5-17(4)34-24(31)16-23-25(19-10-8-9-11-22(19)35-23)26(32)18-14-20(28)27(21(29)15-18)33-13-12-30(6-2)7-3;5-1(3(7)8)2(6)4(9)10/h8-11,14-15,17H,5-7,12-13,16H2,1-4H3;1-2,5-6H,(H,7,8)(H,9,10)/t17-;1-,2-/m01/s1
|
| Chemical Name |
[(2S)-butan-2-yl] 2-[3-[4-[2-(diethylamino)ethoxy]-3,5-diiodobenzoyl]-1-benzofuran-2-yl]acetate;(2R,3R)-2,3-dihydroxybutanedioic acid
|
| HS Tariff Code |
2934.99.9001
|
| 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)
|
| Solubility (In Vitro) |
DMSO : ~100 mg/mL (~117.17 mM)
|
|---|---|
| Solubility (In Vivo) |
Solubility in Formulation 1: ≥ 1 mg/mL (1.17 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 10.0 mg/mL clear DMSO stock solution to 400 μL of PEG300 and mix evenly; then add 50 μL of Tween-80 to the above solution and mix evenly; then add 450 μL of 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: ≥ 1 mg/mL (1.17 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 10.0 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: ≥ 1 mg/mL (1.17 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 | 1.1717 mL | 5.8587 mL | 11.7174 mL | |
| 5 mM | 0.2343 mL | 1.1717 mL | 2.3435 mL | |
| 10 mM | 0.1172 mL | 0.5859 mL | 1.1717 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.
Products are for research use only; We do not sell to patients
Copyright 2020 InvivoChem LLC | All Rights Reserved
