Art. -Nr.: HY-B0232

Dofetilide

Name: Dofetilide
Brand: MedChemExpress
SKU: HY-B0232
Price: 60.00 USD
Availability: InStock
Rating: 5 (6 reviews)

(Synonyms: UK 68789)

6 Cited Publications

Kundenbewertung

Based on 6 publication(s) in Google Scholar

Dofetilide (UK 68789), as a class III antiarrhythmic agent, is an orally active, potent and specific IKr blocker. Dofetilide can be used for the research of cardiovascular disease.

Nur für Forschungszwecke. Wir verkaufen nicht an Patienten.

Reinheit: 98.84%
CAS. Nr.: 115256-11-6
Formel: C₁₉H₂₇N₃O₅S₂
Molecular Weight:441.56

Speicherung:

Powder -20°C, 3 years , 4°C, 2 years ; In solvent -80°C, 2 years , -20°C, 1 year

Dofetilide Chemical Structure

CAS. Nr.: 115256-11-6

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Use of MCE Products

Fluorescent Dye

Strong Fluorescence Signal / Multi-Disciplinary Applications / High Fluorescence Specificity

Biologische Aktivität
- Beschreibung
- IC₅₀ & Target
- Cellular Effect
- In Vivo
- Clinical Trial
Chemical Information
Publications (6)
Lösungsmittel & Löslichkeit
- In Vitro
- In Vivo
Reinheit & Dokumentation
Verweise
Help & FAQs
Classifications
Bioz

Biologische Aktivität

Beschreibung

Dofetilide (UK 68789), as a class III antiarrhythmic agent, is an orally active, potent and specific IKr blocker. Dofetilide can be used for the research of cardiovascular disease^[1]^[2].

IC₅₀ & Target

IKr^[1]

Cellular Effect

Cell Line	Type	Value	Description	References
CHO	IC₅₀	10 nM Compound: dofetilide	Inhibition of K+ channel activity in CHO cells expressing HERG Kv11.1 Inhibition of K+ channel activity in CHO cells expressing HERG Kv11.1	[PMID: 12729675]
CHO	IC₅₀	26.7 μM Compound: dofetilide	Inhibition of Cav1.2 current measured using QPatch automatic path clamp system in CHO cells expressing Cav1.2, beta-2 and alpha-2/delta-1 subunits Inhibition of Cav1.2 current measured using QPatch automatic path clamp system in CHO cells expressing Cav1.2, beta-2 and alpha-2/delta-1 subunits	[PMID: 23812503]
HEK293	IC₅₀	0.015 μM Compound: Dofetilide	Inhibition of human ERG stably expressed in HEK293 cells Inhibition of human ERG stably expressed in HEK293 cells	[PMID: 32453591]
HEK293	IC₅₀	1023 μM Compound: Dofetilide	Inhibition of L-type calcium channel measured using 2-electrode voltage-clamp in human embryonic kidney cells heterologically expressing alpha-1C subunit Inhibition of L-type calcium channel measured using 2-electrode voltage-clamp in human embryonic kidney cells heterologically expressing alpha-1C subunit	[PMID: 22761000]
HEK293	IC₅₀	4.1 nM Compound: 1	Displacement of [3H]astemizole from human ERG K+ channel expressed in HEK293 cells by scintillation spectrophotometric analysis Displacement of [3H]astemizole from human ERG K+ channel expressed in HEK293 cells by scintillation spectrophotometric analysis	[PMID: 23473309]
HEK293	IC₅₀	9.2 nM Compound: 1, dofetilide	Blockade of hERG expressed in HEK293 cells by whole-cell patch clamp method Blockade of hERG expressed in HEK293 cells by whole-cell patch clamp method	[PMID: 17536794]
Oocyte	IC₅₀	>300 μM Compound: Dofetilide	Blockade of Na+ current in frog oocytes expressing human cardiac sodium channel (HH1) Blockade of Na+ current in frog oocytes expressing human cardiac sodium channel (HH1)	[PMID: 7629795]
T-cell line	IC₅₀	1 μM Compound: 5	In vitro inhibition of Rb efflux in human T-cells; 1-10 In vitro inhibition of Rb efflux in human T-cells; 1-10	10.1016/S0960-894X(97)00163-7

In Vivo

Dofetilide (3~100 μg/kg; i.v.) increases repolarisation time via a selective prolongation of activation repolarisation interval, activation time being unchanged^[2].
Dofetilide is metabolized by CYP3A4 to a mixture of inactive polar metabolites that are then excreted by the kidney^[1].

MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.

Animal Model:

Adult beagle dogs (13-15 kg)^[2]
Dosage:

3~100 μg/kg
Administration:

I.v.
Result:

Increased repolarisation time via a selective prolongation of activation repolarisation interval, activation time being unchanged.

Clinical Trial

NCT Number	Sponsor	Condition	Start Date	Phase A549
NCT01329991	Plexxikon\|		2011-05	PHASE1

Chemical Information

CAS. Nr. 115256-11-6
Appearance Solid
Molecular Weight 441.56
Formel C₁₉H₂₇N₃O₅S₂
Color White to off-white
SMILES

CS(=O)(NC1=CC=C(CCN(C)CCOC2=CC=C(NS(=O)(C)=O)C=C2)C=C1)=O
Synonyms

UK 68789
Versand

Room temperature in continental US; may vary elsewhere.

Speicherung

Powder	-20°C	3 years
	4°C	2 years
In solvent	-80°C	2 years
	-20°C	1 year

Publications (6)

All WB

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Journal Impact Factor

Nat Commun

Small molecule in situ resin capture provides a compound first approach to natural product discovery. [Abstract]

2024 Jun 19;15(1):5230. PMID: 38898025
ACS Environ Au

Machine Learning-Assisted Recognition of Environmental Sulfur-Containing Chemicals in Nontargeted Mass Spectrometry Analysis of Inadequate Mass Resolution. [Abstract]

2025 Aug 5;5(6):573-582. PMID: 41277996
Anal Chem

Exposome-Scale Investigation of Cl-/Br-Containing Chemicals Using High-Resolution Mass Spectrometry, Multistage Machine Learning, and Cloud Computing. [Abstract]

2025 Jun 3;97(21):11099-11109. PMID: 40401576
Eur J Pharm Sci

Investigating the relevance of CYP2J2 inhibition for drugs known to cause intermediate to high risk torsades de pointes. [Abstract]

2023 Aug 1:187:106475. PMID: 37225005
Comput Struct Biotechnol J

Drug repurposing screens to identify potential drugs for chronic kidney disease by targeting prostaglandin E2 receptor. [Abstract]

2023 Jul 7:21:3490-3502. PMID: 37484490

Dofetilide purchased from MedChemExpress. Usage Cited in: Comput Struct Biotechnol J. 2023 Jul 7:21:3490-3502. [Abstract]

Dofetilide (10-40 μM; 24 h) increased the autophagy-related protein levels of LC3-I, LC3-II, Beclin 1, and p62 in HK-2 cells.

Dofetilide purchased from MedChemExpress. Usage Cited in: Comput Struct Biotechnol J. 2023 Jul 7:21:3490-3502. [Abstract]

Dofetilide (10-40 μM; 24 h) decreased NLRP3 inflammasome-related protein expression in HK-2 cells.

Dofetilide purchased from MedChemExpress. Usage Cited in: Comput Struct Biotechnol J. 2023 Jul 7:21:3490-3502. [Abstract]

Dofetilide (10–40 μM; 24 h) significantly suppressed the expression levels of fibrosis-related proteins in HK-2 cells.
J Physiol

Deciphering pro-arrhythmogenic mechanisms of EPAC in human atrial cardiomyocytes. [Abstract]

2025 Oct 9. PMID: 41066225

Lösungsmittel & Löslichkeit

In Vitro:

DMSO : ≥ 100 mg/mL (226.47 mM; Hygroscopic DMSO has a significant impact on the solubility of product, please use newly opened DMSO)

* "≥" means soluble, but saturation unknown.

View the Complete Stock Solution Preparation Table

Preparing Stock Solutions

View the Complete Stock Solution Preparation Table

Concentration Solvent Mass

1 mg

5 mg

10 mg

Concentration

Solvent

Mass

1 mM

2.2647 mL

11.3235 mL

22.6470 mL

5 mM

0.4529 mL

2.2647 mL

4.5294 mL

10 mM

0.2265 mL

1.1323 mL

2.2647 mL

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, 2 years; -20°C, 1 year. When stored at -80°C, please use it within 2 years. When stored at -20°C, please use it within 1 year.

Molaritätsrechner

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

Mass Mass

Konzentration Konzentration

Volumen Volumen

Molecular Weight Molecular Weight

Verdünnungsrechner

Konzentration _{(Stammlösung)} × Volumen _{(Stammlösung)} = Konzentration _{(Ziellösung)} × Volumen _{(Ziellösung)}

Konzentration _{(Stammlösung)} Konzentration _{(Stammlösung)}

Volumen _{(Stammlösung)} Volumen _{(Stammlösung)}

Konzentration _{(Ziellösung)} Konzentration _{(Ziellösung)}

Volumen _{(Ziellösung)} Volumen _{(Ziellösung)}

In Vivo:

Select the appropriate dissolution method based on your experimental animal and administration route.

Stock Solution Working Solution

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: 50% PEG400 50% Saline

Solubility: 10 mg/mL (22.65 mM); Clear solution; Need ultrasonic

Protocol 2

Add each solvent one by one: 10% DMSO 40% PEG300 5% Tween-80 45% Saline

Solubility: ≥ 2.5 mg/mL (5.66 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.

Protocol 3

Add each solvent one by one: 10% DMSO 90% (20% SBE-β-CD in Saline)

Solubility: ≥ 2.5 mg/mL (5.66 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.

Protocol 4

Add each solvent one by one: 10% DMSO 90% Corn Oil

Solubility: ≥ 2.5 mg/mL (5.66 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.

In Vivo Dissolution Calculator

Please enter the basic information of animal experiments:

Dosage Dosage
mg/kg
Animal Weight (Per Animal) Animal Weight (Per Animal)
g
Dosing Volume (Per Animal) Dosing Volume (Per Animal)
μL
Number of Animals Number of Animals

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

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

Please enter your animal formula composition:

%
DMSO +

Recommended: Keep the proportion of DMSO in working solution below 2% if your animal is weak.
%
+
+
%
Tween-80 + +
%
Saline +

The co-solvents required include: DMSO, . All of co-solvents are available by MedChemExpress (MCE). , Tween 80. All of co-solvents are available by MedChemExpress (MCE).

Working solution concentration: 0.22 mg/mL

Reinheit & Dokumentation

Select Batch:

Reinheit: 99.98%

Assay: 99.98%

ee.: 99.98%

Data Sheet (272 KB)
SDS (419 KB)
- English - EN (419 KB)
- Français - FR (419 KB)
- Deutsch - DE (419 KB)
- Norwegian - NO (419 KB)
- Español - ES (419 KB)
- Swedish - SV (419 KB)
- Italian - IT (419 KB)
- Korean - KR (419 KB)
- Portuguese - PT (419 KB)
COA (2659 KB)
Elemental Analysis Report (2659 KB)
HNMR (2659 KB)
CNMR (2659 KB)
RP-HPLC (2659 KB)
NP-HPLC (2659 KB)
MS (2659 KB)
LCMS (2659 KB)
IR (2659 KB)
GC (2659 KB)
OR (2659 KB)
SDS-PAGE (2659 KB)
SEC-HPLC (2659 KB)
Other Report (2659 KB)
Handling Instructions (2659 KB)

Verweise

[1]. Mounsey JP, et al. Cardiovascular drugs. Dofetilide. Circulation. 2000;102(21):2665-2670. [Content Brief]

[2]. Gwilt M, et al. Dofetilide, a new class III antiarrhythmic agent, reduces pacing induced heterogeneity of repolarisation in vivo. Cardiovasc Res. 1992;26(11):1102-1108. [Content Brief]

Help & FAQs

How should lyophilized recombinant proteins be reconstituted and stored?

1. Before opening the cap, centrifuge the vial at 13000 rpm for 20-30 seconds. This step will ensure that any lyophilized powder that may have adhered to the cap or walls is collected at the bottom of the vial, minimizing the risk of product loss.

Complete Stock Solution Preparation Table

Storage method and period of stock solution: -80°C, 2 years; -20°C, 1 year. When stored at -80°C, please use it within 2 years. When stored at -20°C, please use it within 1 year.

Optional Solvent	Concentration Solvent Mass	1 mg	5 mg	10 mg	25 mg
DMSO	1 mM	2.2647 mL	11.3235 mL	22.6470 mL	56.6174 mL
	5 mM	0.4529 mL	2.2647 mL	4.5294 mL	11.3235 mL
	10 mM	0.2265 mL	1.1323 mL	2.2647 mL	5.6617 mL
	15 mM	0.1510 mL	0.7549 mL	1.5098 mL	3.7745 mL
	20 mM	0.1132 mL	0.5662 mL	1.1323 mL	2.8309 mL
	25 mM	0.0906 mL	0.4529 mL	0.9059 mL	2.2647 mL
	30 mM	0.0755 mL	0.3774 mL	0.7549 mL	1.8872 mL
	40 mM	0.0566 mL	0.2831 mL	0.5662 mL	1.4154 mL
	50 mM	0.0453 mL	0.2265 mL	0.4529 mL	1.1323 mL
	60 mM	0.0377 mL	0.1887 mL	0.3774 mL	0.9436 mL
	80 mM	0.0283 mL	0.1415 mL	0.2831 mL	0.7077 mL
	100 mM	0.0226 mL	0.1132 mL	0.2265 mL	0.5662 mL

Bioz

Keywords

Dofetilide

6 Cited Publications

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Complete Stock Solution Preparation Table

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Biologische Aktivität

Chemical Information

Publications (6)

Lösungsmittel & Löslichkeit

Reinheit & Dokumentation

Verweise

Help & FAQs

Complete Stock Solution Preparation Table

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