Ibutilide (fumarate)
Based on 1 publication(s) in Google Scholar
Ibutilide (U70226E) fumarate, an action potential-prolonging antiarrhythmic, is a potent blocker of the rapidly activating delayed rectifier K+ current (IKr) in AT-1 cells.
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- 純度: 99.69%
- CAS 番号: 122647-32-9
- 分子式: C24H40N2O7S
- 分子量:442.61
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保管条件:
4°C, sealed storage, away from moisture
* In solvent : -80°C, 6 months; -20°C, 1 month (sealed storage, away from moisture)
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生物活性
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化学情報
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溶剤 & 溶解度
- 純度とドキュメンテーション
- 参考文献
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MedChemExpress（MCE）の使用を引用している文献 Ibutilide fumarate
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生物活性
Ibutilide fumarate is a potent IKr blocker with an EC50 value of 20 nM at +20 mV in atrial tumor myocytes (AT-1) cells[1].
Ibutilide fumarate blocks IKr in cells expressing HERG+MDR1*1 to the same extent as cells expressing HERG alone (IC50: 22.5 nM vs 27.4 nM). However, cells expressing MDR1*7 show a marked resistance to Ibutilide (IC50: 105.3 nM vs 27.4 nM)[2].
MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.
Ibutilide (administered cumulatively in three doses, 0.01, 0.02 and 0.05 mg/kg i.v., each as a 10-min infusion) fumarate results in both polymorphic and monomorphic non-sustained ventricular tachycardia[3].
MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.
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Animal Model:Fifteen adult mongrel dogs of either sex[1]
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Dosage:0.01, 0.02 and 0.05 mg/kg
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Administration:Intravenous injection; each as a 10-min infusion
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Result:The action potential duration at 90% (APD90) prolongation with Ibutilide (0.01 mg/kg) was significantly greater in congestive heart failure (CHF) vs. controls.
An increased dispersion of left-right ventricular APD90 was observed in CHF at 0.01 mg/kg, but not in controls.
| NCT Number | Sponsor | Condition | Start Date |
Phase
|
|---|---|---|---|---|
| NCT01329991 | Plexxikon| | 2011-05 | PHASE1 |
化学情報
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CAS 番号 122647-32-9
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性状 Solid
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分子量 442.61
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分子式 C24H40N2O7S
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Color White to off-white
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SMILES
CS(=O)(NC1=CC=C(C(O)CCCN(CC)CCCCCCC)C=C1)=O.O=C(O)/C=C/C(O)=O
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別名
U70226E
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輸送条件
Room temperature in continental US; may vary elsewhere.
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保管条件
4°C, sealed storage, away from moisture
* In solvent : -80°C, 6 months; -20°C, 1 month (sealed storage, away from moisture)
Publications (1)
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Journal Impact Factor
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Most Recent
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Biochem Biophys Res Commun
Dual-cardiotoxicity evaluation of torsadogenic risk drugs using human iPSC-derived cardiomyocytes. [Abstract]2025 Oct 30:786:152756. PMID: 41043280
溶剤 & 溶解度
DMSO : ≥ 50 mg/mL (112.97 mM; Hygroscopic DMSO has a significant impact on the solubility of product, please use newly opened DMSO)
H2O : 50 mg/mL (112.97 mM; Need ultrasonic)
* "≥" means soluble, but saturation unknown.
Please refer to the solubility information to select the appropriate solvent. Once prepared, please aliquot and store the solution to prevent product inactivation from repeated freeze-thaw cycles.
Storage method and period of stock solution: -80°C, 6 months; -20°C, 1 month (sealed storage, away from moisture). When stored at -80°C, please use it within 6 months. When stored at -20°C, please use it within 1 month.
* Note: If you choose water as the stock solution, please dilute it to the working solution, then filter and sterilize it with a 0.22 μm filter before use.
Please refer to the solubility information to select the appropriate solvent. Once prepared, please aliquot and store the solution to prevent product inactivation from repeated freeze-thaw cycles.
Storage method and period of stock solution: -80°C, 6 months; -20°C, 1 month (sealed storage, away from moisture). When stored at -80°C, please use it within 6 months. When stored at -20°C, please use it within 1 month.
* Note: If you choose water as the stock solution, please dilute it to the working solution, then filter and sterilize it with a 0.22 μm filter before use.
濃度 (開始) × 体積 (開始) = 濃度 (終了) × 体積 (終了)
Select the appropriate dissolution method based on your experimental animal and administration route.
- For the following dissolution methods, please ensure to first prepare a clear stock solution using an In Vitro approach and then sequentially add co-solvents:
- To ensure reliable experimental results, the clarified stock solution can be appropriately stored based on storage conditions. As for the working solution for In Vivo experiments, it is recommended to prepare freshly and use it on the same day.
- The percentages shown for the solvents indicate their volumetric ratio in the final prepared solution. If precipitation or phase separation occurs during preparation, heat and/or sonication can be used to aid dissolution.
Add each solvent one by one: 10% DMSO 40% PEG300 5% Tween-80 45% Saline
Solubility: ≥ 2.5 mg/mL (5.65 mM); Clear solution
This protocol yields a clear solution of ≥ 2.5 mg/mL (saturation unknown).
Taking 1 mL working solution as an example, add 100 μL DMSO stock solution (25.0 mg/mL) to 400 μL PEG300, and mix evenly; then add 50 μL Tween-80 and mix evenly; then add 450 μL Saline to adjust the volume to 1 mL.
Preparation of Saline: Dissolve 0.9 g sodium chloride in ddH₂O and dilute to 100 mL to obtain a clear Saline solution.
Add each solvent one by one: 10% DMSO 90% (20% SBE-β-CD in Saline)
Solubility: ≥ 2.5 mg/mL (5.65 mM); Clear solution
This protocol yields a clear solution of ≥ 2.5 mg/mL (saturation unknown).
Taking 1 mL working solution as an example, add 100 μL DMSO stock solution (25.0 mg/mL) to 900 μL 20% SBE-β-CD in Saline, and mix evenly.
Preparation of 20% SBE-β-CD in Saline (4°C, storage for one week): 2 g SBE-β-CD powder is dissolved in 10 mL Saline, completely dissolve until clear.
For the following dissolution methods, please prepare the working solution directly:
It is recommended to prepare fresh solutions and use them promptly within a short period of time.
The percentages shown for the solvents indicate their volumetric ratio in the final prepared solution. If precipitation or phase separation occurs during preparation, heat and/or sonication can be used to aid dissolution.
Add each solvent one by one: PBS
Solubility: 37.5 mg/mL (84.72 mM); Clear solution; Need ultrasonic
Please enter the basic information of animal experiments:
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Recommended: Prepare an additional quantity of animals to account for potential losses during experiments.
Working solution concentration: 0.22 mg/mL
This product has good water solubility, please refer to the measured solubility data in water/PBS/Saline for details.
純度とドキュメンテーション
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データシート (273 KB)
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取扱説明書 (2659 KB)
参考文献
[1]. Ibutilide, a methanesulfonanilide antiarrhythmic, is a potent blocker of the rapidly activating delayed rectifier K+ current (IKr) in AT-1 cells. Concentration-, time-, voltage-, and use-dependent effects. Circulation. 1995 Mar 15;91(6):1799-806. [Content Brief]
[2]. B F McBride, et al. Influence of the G2677T/C3435T haplotype of MDR1 on P-glycoprotein trafficking and Ibutilide-induced block of HERG. Pharmacogenomics J. 2009 Jun;9(3):194-201. [Content Brief]
[3]. S S Chugh, et al. Altered response to Ibutilide in a heart failure model. Cardiovasc Res. 2001 Jan;49(1):94-102. [Content Brief]
Complete Stock Solution Preparation Table
Please refer to the solubility information to select the appropriate solvent. Once prepared, please aliquot and store the solution to prevent product inactivation from repeated freeze-thaw cycles.
Storage method and period of stock solution: -80°C, 6 months; -20°C, 1 month (sealed storage, away from moisture). When stored at -80°C, please use it within 6 months. When stored at -20°C, please use it within 1 month.
| Optional Solvent | Concentration Solvent Mass | 1 mg | 5 mg | 10 mg | 25 mg |
|---|---|---|---|---|---|
| DMSO / H2O | 1 mM | 2.2593 mL | 11.2966 mL | 22.5933 mL | 56.4831 mL |
| 5 mM | 0.4519 mL | 2.2593 mL | 4.5187 mL | 11.2966 mL | |
| 10 mM | 0.2259 mL | 1.1297 mL | 2.2593 mL | 5.6483 mL | |
| 15 mM | 0.1506 mL | 0.7531 mL | 1.5062 mL | 3.7655 mL | |
| 20 mM | 0.1130 mL | 0.5648 mL | 1.1297 mL | 2.8242 mL | |
| 25 mM | 0.0904 mL | 0.4519 mL | 0.9037 mL | 2.2593 mL | |
| 30 mM | 0.0753 mL | 0.3766 mL | 0.7531 mL | 1.8828 mL | |
| 40 mM | 0.0565 mL | 0.2824 mL | 0.5648 mL | 1.4121 mL | |
| 50 mM | 0.0452 mL | 0.2259 mL | 0.4519 mL | 1.1297 mL | |
| 60 mM | 0.0377 mL | 0.1883 mL | 0.3766 mL | 0.9414 mL | |
| 80 mM | 0.0282 mL | 0.1412 mL | 0.2824 mL | 0.7060 mL | |
| 100 mM | 0.0226 mL | 0.1130 mL | 0.2259 mL | 0.5648 mL |
* Note: If you choose water as the stock solution, please dilute it to the working solution, then filter and sterilize it with a 0.22 μm filter before use.
Ibutilide fumarate 関連分類
HY-B0387 関連分類
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