Cat. No.: HY-106577

Cibenzoline

(Synonyms: Cifenline; Ro 22-7796)

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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.

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Pureté: 95.08%
CAS No.: 53267-01-9
Formule: C₁₈H₁₈N₂
Masse moléculaire:262.36

Stockage:

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

Cibenzoline Chemical Structure

CAS No.: 53267-01-9

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Activité biologique
- Description
- IC₅₀ & Target
- Cellular Effect
- In Vitro
- In Vivo
Chemical Information
Solvant et solubilité
- In Vitro
- In Vivo
Pureté et documentation
Références
Help & FAQs
Classifications
Bioz

Activité biologique

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.

Chemical Information

CAS No. 53267-01-9
Appearance Solid
Masse moléculaire 262.36
Formule C₁₈H₁₈N₂
Color White to off-white
SMILES

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

Cifenline; Ro 22-7796
Livraison

Room temperature in continental US; may vary elsewhere.

Stockage

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

Solvant et solubilité

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)

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

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

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.

Calculateur de molarité

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

Mass Mass

Concentration Concentration

Volume Volume

Molecular Weight Molecular Weight

Calculateur de dilution

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

Concentration _(start) Concentration _(start)

Volume _(start) Volume _(start)

Concentration _(final) Concentration _(final)

Volume _(final) Volume _(final)

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: 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.

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.

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 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

Pureté et documentation

Select Batch:

Pureté: 99.98%

Assay: 99.98%

ee.: 99.98%

Fiche technique (292 KB)
SDS (393 KB)
- English - EN (393 KB)
- Français - FR (393 KB)
- Deutsch - DE (393 KB)
- Norwegian - NO (393 KB)
- Español - ES (393 KB)
- Swedish - SV (393 KB)
- Italian - IT (393 KB)
- Korean - KR (393 KB)
- Portuguese - PT (393 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)
Instruction de manipulation (2659 KB)

Références

[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. [Content Brief]

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

[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]

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, 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.

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

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Cibenzoline

Membrane Transporter/Ion Channel Compound Library

Clinical Compound Library

Drug Repurposing Compound Library

Anti-diabetic Compound Library

Anti-Cardiovascular Disease Compound Library

Rare Diseases Drug Library

Protein-protein Interaction Inhibitor Library

Human Metabolite Library

Membrane Protein-targeted Compound Library

Membrane Receptor-targeted Compound Library

Ion Channel Compound Library

Bioactive Compound Library Max

MCE Bioactive Compound Library

Drug Repurposing Compound Library Plus

Clinical Compound Library Plus

Bioactive Compound Library

High-Throughput Bioactive Compound Library

Mass Spectrometry Human Metabolite Library

3D Diverse Fragment Library

Activité biologique

Chemical Information

Solvant et solubilité

Pureté et documentation

Références

Help & FAQs

Complete Stock Solution Preparation Table

Cibenzoline

Membrane Transporter/Ion Channel Compound Library

Clinical Compound Library

Drug Repurposing Compound Library

Anti-diabetic Compound Library

Anti-Cardiovascular Disease Compound Library

Rare Diseases Drug Library

Protein-protein Interaction Inhibitor Library

Human Metabolite Library

Membrane Protein-targeted Compound Library

Membrane Receptor-targeted Compound Library

Ion Channel Compound Library

Bioactive Compound Library Max

MCE Bioactive Compound Library

Drug Repurposing Compound Library Plus

Clinical Compound Library Plus

Bioactive Compound Library

High-Throughput Bioactive Compound Library

Mass Spectrometry Human Metabolite Library

3D Diverse Fragment Library

Activité biologique

Chemical Information

Solvant et solubilité

Pureté et documentation

Références

Help & FAQs

Complete Stock Solution Preparation Table

Cibenzoline Related Classifications

HY-106577 Related Classifications