| Size | Price | Stock | Qty |
|---|---|---|---|
| 1mg |
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| 5mg |
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| 10mg |
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| Other Sizes |
| Targets |
KATP channel[1]
KATP channel (directly affects pore-forming Kir6.2 subunit, IC50 = 22.2 microM). |
|---|---|
| ln Vitro |
In vitro, Cibenzoline is a potent KATP channel inhibitor with an IC50 of 22.2 microM, acting directly on the Kir6.2 subunit.
|
| ln Vivo |
Cibenzoline markedly attenuates left ventricular pressure gradient (LVPG) in vivo, a parameter closely related to myocardial contractility, and has potential for the research of hypertrophic obstructive cardiomyopathy.
|
| Cell Assay |
Recombinant Kir6.2 channels can be expressed in HEK293 cells, and whole-cell patch-clamp recordings are performed to measure KATP currents. The test compound is applied at varying concentrations, and the inhibition of potassium current is measured. IC50 values are calculated from dose-response curves.
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| Animal Protocol |
Cibenzoline's antiarrhythmic activity is assessed in animal models, such as rats with coronary artery occlusion. It is formulated in a suitable vehicle and administered intravenously or orally, and its effects on arrhythmia incidence and hemodynamic parameters are evaluated.
|
| ADME/Pharmacokinetics |
Cibenzoline has a half-life of approximately 7-15 hours, is metabolized in the liver by CYP2D6 and CYP3A4, and is excreted in urine and feces. It is well absorbed after oral administration.
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| Toxicity/Toxicokinetics |
Potential side effects include dizziness, dry mouth, nausea, and headache. As a class Ia agent, it may cause QT prolongation and proarrhythmia. Contraindicated in patients with severe heart failure or cardiogenic shock.
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| References |
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| Additional Infomation |
Cebenzazoline is a diarylmethane.
Developed for the treatment of hypertrophic obstructive cardiomyopathy and cardiac arrhythmias. It is available in Japan and other countries. |
| 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
|
| SMILES |
C1CN=C(N1)C2CC2(C3=CC=CC=C3)C4=CC=CC=C4
|
| 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)
|
| 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. View More
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. |
| 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.
Calculation results
Working concentration： mg/mL；
Method for preparing DMSO stock solution： mg drug pre-dissolved in μL DMSO (stock solution concentration mg/mL). Please contact us first if the concentration exceeds the DMSO solubility of the batch of drug.
Method for preparing in vivo formulation:：Take μL DMSO stock solution, next add μL PEG300, mix and clarify, next addμL Tween 80, mix and clarify, next add μL ddH2O，mix and clarify.
(1) Please be sure that the solution is clear before the addition of next solvent. Dissolution methods like vortex, ultrasound or warming and heat may be used to aid dissolving.
(2) Be sure to add the solvent(s) in order.
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