Dofetilide (Synonyms: UK 68789)

Name: Dofetilide
Brand: MedChemExpress
SKU: HY-B0232
Rating: 5.0 (6 reviews)

Cat. No.: HY-B0232 Purity: 98.84%: Data Sheet
COA

SDS
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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.

For research use only. We do not sell to patients.

CAS No. : 115256-11-6

Size	Stock	Quantity

Free Sample (0.1 - 0.2 mg)	Apply Now
Solid + Solvent (Highly Recommended)
10 mM * 1 mL in DMSO ready for reconstitution	In-stock	Estimated Time of Arrival: December 31
Solution
10 mM * 1 mL in DMSO	In-stock	Estimated Time of Arrival: December 31
Solid
5 mg	In-stock	Estimated Time of Arrival: December 31
10 mg	In-stock	Estimated Time of Arrival: December 31
25 mg	In-stock	Estimated Time of Arrival: December 31
50 mg	In-stock	Estimated Time of Arrival: December 31
100 mg	In-stock	Estimated Time of Arrival: December 31
200 mg	Get quote
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Customer Review

Based on 6 publication(s) in Google Scholar

Other Forms of Dofetilide:

Dofetilide-d₄ In-stock
Dofetilide (Standard) Get quote

6 Publications Citing Use of MCE Dofetilide

: Dofetilide purchased from MedChemExpress. Usage Cited in: Comput Struct Biotechnol J. 2023 Jul 7:21:3490-3502.; 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.; 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.; Dofetilide (10–40 μM; 24 h) significantly suppressed the expression levels of fibrosis-related proteins in HK-2 cells.

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Biological Activity
Purity & Documentation
References
Customer Review

Description

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

Molecular Weight

441.56

Formula

C₁₉H₂₇N₃O₅S₂

CAS No.

115256-11-6

Appearance

Solid

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

Shipping

Room temperature in continental US; may vary elsewhere.

Storage

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

Solvent & Solubility

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.

Preparing
Stock Solutions

Concentration Solvent Mass	1 mg	5 mg	10 mg

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

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, 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.

Molarity Calculator
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

Concentration _(start)

Volume _(start)

Concentration _(final)

Volume _(final)

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: 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.
Preparation of Saline: Dissolve 0.9 g sodium chloride in ddH₂O and dilute to 100 mL to obtain a clear Saline solution.
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.
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 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

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.

Please enter your animal formula composition:

DMSO +

Tween-80 +

Saline

Recommended: Keep the proportion of DMSO in working solution below 2% if your animal is weak.

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).

Calculation results:

Working solution concentration: mg/mL

Method for preparing stock solution: mg drug dissolved in μL DMSO (Stock solution concentration: mg/mL).

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).

Method for preparing in vivo working solution for animal experiments: Take μL DMSO stock solution, add μL . μL , mix evenly, next add μL Tween 80, mix evenly, then add μL Saline.

If the continuous dosing period exceeds half a month, please choose this protocol carefully.

Please ensure that the stock solution in the first step is dissolved to a clear state, and add co-solvents in sequence. You can use ultrasonic heating (ultrasonic cleaner, recommended frequency 20-40 kHz), vortexing, etc. to assist dissolution.

Purity & Documentation

Purity: 98.84%

Select Batch:

Data Sheet (272 KB) SDS (419 KB)

COA (245 KB) RP-HPLC (256 KB)

Handling Instructions (2659 KB)

References

[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]

Complete Stock Solution Preparation Table

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

Dofetilide Related Classifications

Cardiovascular Disease

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:

Dofetilide115256-11-6UK 68789UK68789UK-68789Potassium ChannelKcsAclassIIIantiarrhythmicagentorallypotentspecificcardiovascularInhibitorinhibitorinhibit

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Dofetilide (Synonyms: UK 68789)

Customer Review

Other Forms of Dofetilide:

Dofetilide Related Antibodies

6 Publications Citing Use of MCE Dofetilide

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Biological Activity

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References

Customer Review

Molarity Calculator

Dilution Calculator

Complete Stock Solution Preparation Table

Dofetilide Related Classifications

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