Cibenzoline (Synonyms: Cifenline; Ro 22-7796)

Name: Cibenzoline
Brand: MedChemExpress
SKU: HY-106577
Rating: 4.5 (1 reviews)

Cat. No.: HY-106577 Purity: 99.96%: FAQs
Data Sheet SDS COA Handling Instructions

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Cibenzoline is a class Ia antiarrhythmic active molecule with low anticholinergic activity. Cibenzoline is a K_ATP channel inhibitor, acting through the pore forming subunit Kir6.2, with an IC₅₀ of 22.2 μM. Cibenzoline inhibits I_Kr and I_Ks currents with IC₅₀ values of 8.8 μM and 12.3 μM, respectively. Cibenzoline is used in the study of cardiac diseases. In addition, Cibenzoline can induce hypoglycemia.

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

Cibenzoline Chemical Structure

CAS No. : 53267-01-9

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Solid + Solvent (Highly Recommended)
10 mM * 1 mL in DMSO ready for reconstitution	USD 138	In-stock	Estimated Time of Arrival: December 31
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10 mM * 1 mL in DMSO	USD 138	In-stock	Estimated Time of Arrival: December 31
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5 mg	USD 125	In-stock	Estimated Time of Arrival: December 31
10 mg	USD 200	In-stock	Estimated Time of Arrival: December 31
25 mg	USD 400	In-stock	Estimated Time of Arrival: December 31
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Based on 1 publication(s) in Google Scholar

Other Forms of Cibenzoline:

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References
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Description

IC₅₀ & Target

KATP channel^[1]

Cellular Effect

Cell Line	Type	Value	Description	References
Ventricular myocyte	IC₅₀	14 μM Compound: Cibenzoline	Inhibition of L-type calcium channel measured using whole-cell patch clamp in guinea pig ventricular myocytes Inhibition of L-type calcium channel measured using whole-cell patch clamp in guinea pig ventricular myocytes	[PMID: 22761000]
Ventricular myocyte	IC₅₀	14.4 μM Compound: Cibenzoline	Inhibition of L-type calcium channel measured using whole-cell patch clamp in guinea pig ventricular myocytes Inhibition of L-type calcium channel measured using whole-cell patch clamp in guinea pig ventricular myocytes	[PMID: 22761000]
Ventricular myocyte	IC₅₀	30 μM Compound: Cibenzoline	Inhibition of L-type calcium channel measured using whole-cell patch clamp in guinea pig ventricular myocytes Inhibition of L-type calcium channel measured using whole-cell patch clamp in guinea pig ventricular myocytes	[PMID: 22761000]

In Vitro

Cibenzoline (1-100 μM; 3-5 min) inhibits the spontaneous activity and leads to sinus arrest in rat sino-atrial nodal cells^[1].
Cibenzoline (3-300 μM; 15 minutes) inhibits I_Kr and I_Ks currents with IC₅₀ values of 8.8 μM and 12.3 μM in rat sino-atrial nodal cells^[1].

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

In Vivo

Cibenzoline (5-20 mg/kg; intravenous injection; single dose) has hypoglycemic effect in rats^[2].
Pharmacokinetic Analysis in Rats^[2]

Route	Dose (mg/kg)	k₁₂ (h^-1)	k₂₁ (h^-1)	Vc (L/kg)	V_{max, CBZ} (μg/h)	K_{m, CBZ} (μg/L)
i.v.	5, 10 and 20	1.93	1.01	4.70	32391	3554

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

Animal Model:	Male Wistar rats (210-280 g) ^[2]
Dosage:	5, 10 and 20 mg/kg
Administration:	Intravenous injection (i.v.); single dose
Result:	Induced a rapid increase in the serum concentration of insulin. Had a greater hypoglycemic effect.

Molecular Weight

262.36

Formula

C₁₈H₁₈N₂

CAS No.

53267-01-9

Appearance

Solid

Color

White to off-white

SMILES

C1(C2CC2(C3=CC=CC=C3)C4=CC=CC=C4)=NCCN1

Shipping

Room temperature in continental US; may vary elsewhere.

Storage

Powder	-20°C	3 years
	4°C	2 years
In solvent	-80°C	6 months
	-20°C	1 month

Solvent & Solubility

In Vitro:

DMSO : 100 mg/mL (381.16 mM; ultrasonic and warming and heat to 60°C; Hygroscopic DMSO has a significant impact on the solubility of product, please use newly opened DMSO)

Preparing
Stock Solutions

Concentration Solvent Mass	1 mg	5 mg	10 mg

1 mM	3.8116 mL	19.0581 mL	38.1161 mL
5 mM	0.7623 mL	3.8116 mL	7.6232 mL
10 mM	0.3812 mL	1.9058 mL	3.8116 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. When stored at -80°C, please use it within 6 months. When stored at -20°C, please use it within 1 month.

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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

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: 10% DMSO 40% PEG300 5% Tween-80 45% Saline
Solubility: ≥ 2.5 mg/mL (9.53 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 (9.53 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 (9.53 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: 99.96%

Select Batch:

Data Sheet (292 KB) SDS (251 KB)

COA (256 KB) HNMR (261 KB) LCMS (261 KB)

Handling Instructions (2659 KB)

References

[1]. Satoh H. Comparative actions of cibenzoline and disopyramide on I(Kr) and I(Ks) currents in rat sino-atrial nodal cells. Eur J Pharmacol. 2000 Oct 27;407(1-2):123-9.

[2]. Takahashi Y, et al. Pharmacodynamics of cibenzoline-induced hypoglycemia in rats. Drug Metab Pharmacokinet. 2011 Jun;26(3):242-7.

[3]. Mukai E, et al. The antiarrhythmic agent cibenzoline inhibits KATP channels by binding to Kir6.2. Biochem Biophys Res Commun. 1998;251(2):477-481. [Content Brief]

[4]. Hamada M, et al. Class Ia antiarrhythmic drug cibenzoline: a new approach to the medical treatment of hypertrophic obstructive cardiomyopathy. Circulation. 1997;96(5):1520-1524. [Content Brief]

Complete Stock Solution Preparation Table

Optional Solvent	Concentration Solvent Mass	1 mg	5 mg	10 mg	25 mg

DMSO	1 mM	3.8116 mL	19.0581 mL	38.1161 mL	95.2904 mL
	5 mM	0.7623 mL	3.8116 mL	7.6232 mL	19.0581 mL
	10 mM	0.3812 mL	1.9058 mL	3.8116 mL	9.5290 mL
	15 mM	0.2541 mL	1.2705 mL	2.5411 mL	6.3527 mL
	20 mM	0.1906 mL	0.9529 mL	1.9058 mL	4.7645 mL
	25 mM	0.1525 mL	0.7623 mL	1.5246 mL	3.8116 mL
	30 mM	0.1271 mL	0.6353 mL	1.2705 mL	3.1763 mL
	40 mM	0.0953 mL	0.4765 mL	0.9529 mL	2.3823 mL
	50 mM	0.0762 mL	0.3812 mL	0.7623 mL	1.9058 mL
	60 mM	0.0635 mL	0.3176 mL	0.6353 mL	1.5882 mL
	80 mM	0.0476 mL	0.2382 mL	0.4765 mL	1.1911 mL
	100 mM	0.0381 mL	0.1906 mL	0.3812 mL	0.9529 mL

Cibenzoline Related Classifications

Metabolic Disease 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:

Cibenzoline53267-01-9Cifenline Ro 22-7796Potassium ChannelKcsAsino-atrial nodal cellsInhibitorinhibitorinhibit

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Cibenzoline (Synonyms: Cifenline; Ro 22-7796)

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Other Forms of Cibenzoline:

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Cibenzoline Related Antibodies

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Complete Stock Solution Preparation Table

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