Cibenzoline is a potent KATP channel inhibitor that directly affects the pore-forming Kir6.2 subunit but not the SUR1 subunit. Cibenzoline is a class Ia antiarrhythmic active molecule. Cibenzoline has little anticholinergic activity. Cibenzoline significantly weakens LVPG, which is closely related to the decrease in myocardial contractility. Cibenzoline may be utilized in studies of hypertrophic obstructive cardiomyopathy.

Physicochemical Properties

Molecular Formula	C18H18N2
Molecular Weight	262.35
Exact Mass	262.147
CAS #	53267-01-9
Related CAS #	(-)-(S)-Cibenzoline;103419-18-7
PubChem CID	2747
Appearance	White to off-white solid powder
Density	1.17 g/cm3
Boiling Point	449.2ºC
Melting Point	103-104°
Flash Point	225.5ºC
Index of Refraction	1.655
LogP	2.758
Hydrogen Bond Donor Count	1
Hydrogen Bond Acceptor Count	1
Rotatable Bond Count	3
Heavy Atom Count	20
Complexity	357
Defined Atom Stereocenter Count	0
InChi Key	IPOBOOXFSRWSHL-UHFFFAOYSA-N
InChi Code	InChI=1S/C18H18N2/c1-3-7-14(8-4-1)18(15-9-5-2-6-10-15)13-16(18)17-19-11-12-20-17/h1-10,16H,11-13H2,(H,19,20)
Chemical Name	2-(2,2-diphenylcyclopropyl)-4,5-dihydro-1H-imidazole
HS Tariff Code	2934.99.9001
Storage	Powder-20°C 3 years 4°C 2 years In solvent -80°C 6 months -20°C 1 month
Shipping Condition	Room temperature (This product is stable at ambient temperature for a few days during ordinary shipping and time spent in Customs)

Biological Activity

Targets	KATP channel[1]
References	[1]. The antiarrhythmic agent cibenzoline inhibits KATP channels by binding to Kir6.2. Biochem Biophys Res Commun. 1998;251(2):477-481. [2]. Class Ia antiarrhythmic drug cibenzoline: a new approach to the medical treatment of hypertrophic obstructive cardiomyopathy. Circulation. 1997;96(5):1520-1524.
Additional Infomation	Cibenzoline is a diarylmethane.

Solubility Data

Solubility (In Vitro)

DMSO: 100 mg/mL (381.17 mM)

Solubility (In Vivo)

Solubility in Formulation 1: ≥ 2.5 mg/mL (9.53 mM) (saturation unknown) in 10% DMSO + 40% PEG300 + 5% Tween80 + 45% Saline (add these co-solvents sequentially from left to right, and one by one), clear solution. For example, if 1 mL of working solution is to be prepared, you can add 100 μL of 25.0 mg/mL clear DMSO stock solution to 400 μL PEG300 and mix evenly; then add 50 μL Tween-80 to the above solution and mix evenly; then add 450 μL normal saline to adjust the volume to 1 mL. Preparation of saline: Dissolve 0.9 g of sodium chloride in 100 mL ddH₂ O to obtain a clear solution. Solubility in Formulation 2: ≥ 2.5 mg/mL (9.53 mM) (saturation unknown) in 10% DMSO + 90% (20% SBE-β-CD in Saline) (add these co-solvents sequentially from left to right, and one by one), clear solution. For example, if 1 mL of working solution is to be prepared, you can add 100 μL of 25.0 mg/mL clear DMSO stock solution to 900 μL of 20% SBE-β-CD physiological saline solution and mix evenly. Preparation of 20% SBE-β-CD in Saline (4°C，1 week): Dissolve 2 g SBE-β-CD in 10 mL saline to obtain a clear solution. Solubility in Formulation 3: ≥ 2.5 mg/mL (9.53 mM) (saturation unknown) in 10% DMSO + 90% Corn Oil (add these co-solvents sequentially from left to right, and one by one), clear solution. For example, if 1 mL of working solution is to be prepared, you can add 100 μL of 25.0 mg/mL clear DMSO stock solution to 900 μL of corn oil and mix evenly.  (Please use freshly prepared in vivo formulations for optimal results.)

Preparing Stock Solutions		1 mg	5 mg	10 mg
	1 mM	3.8117 mL	19.0585 mL	38.1170 mL
	5 mM	0.7623 mL	3.8117 mL	7.6234 mL
	10 mM	0.3812 mL	1.9059 mL	3.8117 mL

*Note: Please select an appropriate solvent for the preparation of stock solution based on your experiment needs. For most products, DMSO can be used for preparing stock solutions (e.g. 5 mM, 10 mM, or 20 mM concentration); some products with high aqueous solubility may be dissolved in water directly. Solubility information is available at the above Solubility Data section. Once the stock solution is prepared, aliquot it to routine usage volumes and store at -20°C or -80°C. Avoid repeated freeze and thaw cycles.