Ibutilide fumarate (Synonyms: U70226E)

Cat. No.: HY-B0387 Purity: 99.78%: FAQs
Data Sheet SDS COA Handling Instructions

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Ibutilide (U70226E) fumarate, an action potential-prolonging antiarrhythmic, is a potent blocker of the rapidly activating delayed rectifier K⁺ current (I_Kr) in AT-1 cells.

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Ibutilide fumarate Chemical Structure

CAS No. : 122647-32-9

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10 mM * 1 mL in DMSO ready for reconstitution	USD 79	In-stock	Estimated Time of Arrival: December 31
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10 mM * 1 mL in DMSO	USD 79	In-stock	Estimated Time of Arrival: December 31
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10 mg	USD 72	In-stock	Estimated Time of Arrival: December 31
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Other Forms of Ibutilide fumarate:

Ibutilide Get quote
Ibutilide-d₅ fumarate Get quote

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Biological Activity
Purity & Documentation
References
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Description

Ibutilide (U70226E) fumarate, an action potential-prolonging antiarrhythmic, is a potent blocker of the rapidly activating delayed rectifier K⁺ current (I_Kr) in AT-1 cells^[1].

In Vitro

Ibutilide fumarate is a potent I_Kr blocker with an EC₅₀ value of 20 nM at +20 mV in atrial tumor myocytes (AT-1) cells^[1].
Ibutilide fumarate blocks I_Kr 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.

In Vivo

Ibutilide fumarate prolongs cardiac repolarization in vitro and in vivo^[1].
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.

Animal Model:	Fifteen adult mongrel dogs of either sex^[1]
Dosage:	0.01, 0.02 and 0.05 mg/kg
Administration:	Intravenous injection; each as a 10-min infusion
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.

Clinical Trial

Molecular Weight

442.61

Formula

C₂₄H₄₀N₂O₇S

CAS No.

122647-32-9

Appearance

Solid

Color

White to off-white

SMILES

CS(=O)(NC1=CC=C(C(O)CCCN(CC)CCCCCCC)C=C1)=O.O=C(O)/C=C/C(O)=O

Shipping

Room temperature in continental US; may vary elsewhere.

Storage

4°C, sealed storage, away from moisture

*In solvent : -80°C, 6 months; -20°C, 1 month (sealed storage, away from moisture)

Solvent & Solubility

In Vitro:

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.

Preparing
Stock Solutions

Concentration Solvent Mass	1 mg	5 mg	10 mg

1 mM	2.2593 mL	11.2966 mL	22.5933 mL
5 mM	0.4519 mL	2.2593 mL	4.5187 mL
10 mM	0.2259 mL	1.1297 mL	2.2593 mL

View the 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.

* 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.

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Dilution Calculator

Mass (g) = Concentration (mol/L) × Volume (L) × Molecular Weight (g/mol)

Concentration _(start) × Volume _(start) = Concentration _(final) × Volume _(final)

This equation is commonly abbreviated as: C₁V₁ = C₂V₂

In Vivo:

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.

Protocol 1

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.
Protocol 2

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.
Protocol 3

Add each solvent one by one: 10% DMSO 90% Corn Oil
Solubility: ≥ 2.5 mg/mL (5.65 mM); Clear solution

This protocol yields a clear solution of ≥ 2.5 mg/mL (saturation unknown). If the continuous dosing period exceeds half a month, please choose this protocol carefully.
Taking 1 mL working solution as an example, add 100 μL DMSO stock solution (25.0 mg/mL) to 900 μL Corn oil, and mix evenly.

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.

Protocol 1

Add each solvent one by one: PBS
Solubility: 37.5 mg/mL (84.72 mM); Clear solution; Need ultrasonic

In Vivo Dissolution Calculator

Please enter the basic information of animal experiments:

Dosage

mg/kg

Animal weight
(per animal)

Dosing volume
(per animal)

μL

Number of animals

Recommended: Prepare an additional quantity of animals to account for potential losses during experiments.

Calculation results:

Working solution concentration: mg/mL

This product has good water solubility, please refer to the measured solubility data in water/PBS/Saline for details.

The concentration of the stock solution you require exceeds the measured solubility. The following solution is for reference only.If necessary, please contact MedChemExpress (MCE).

Purity & Documentation

Purity: 99.78%

Select Batch:

Data Sheet (273 KB) SDS (398 KB)

COA (247 KB) HNMR (256 KB) LCMS (89 KB)

Handling Instructions (2659 KB)

References

[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

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 Related Classifications

Help & FAQs

Do most proteins show cross-species activity?
Species cross-reactivity must be investigated individually for each product. Many human cytokines will produce a nice response in mouse cell lines, and many mouse proteins will show activity on human cells. Other proteins may have a lower specific activity when used in the opposite species.

Keywords:

Ibutilide122647-32-9U70226EPotassium ChannelKcsApharmacologylong QT syndromeP-glycoproteinATP-binding cassette transportersantiarrhythmia agentK+ currentInhibitorinhibitorinhibit

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