| Size | Price | Stock | Qty |
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| 5mg |
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| 10mg |
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| Other Sizes |
| Targets |
Bepridil hydrochloride hydrate targets multiple ion channels, including L-type calcium channels, sodium channels, and potassium channels. It is a non-selective, long-acting Ca2+ channel antagonist. The compound also acts as a cardiac Na+/Ca2+ exchange (NCX1) inhibitor. By blocking calcium channels, it reduces cardiac contractility and causes vasodilation, leading to antianginal and antiarrhythmic effects.
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| ln Vitro |
In canine coronary artery smooth muscle, bepridil hydrochloride hydrate inhibits Ca2+-dependent action potentials [2]. In cultivated ventricular cells, the current's IC50 values are 0.5 μM and 30 μM, correspondingly [4]. E4031 (5 μM) IKr inhibits the decrease of IKs by bepridil hydrochloride hydrate in a concentration-dependent manner [5].
In vitro, Bepridil hydrochloride hydrate is a non-selective Ca2+ channel antagonist and Na+, K+ channel inhibitor. It has recently been shown to possess potent activity against SARS-CoV-2 in vitro. The compound's multi-ion channel blocking activity makes it useful for studying various cardiovascular and cellular processes. Standard in vitro assays include patch-clamp electrophysiology on cardiomyocytes or cell lines expressing calcium, sodium, or potassium channels, as well as functional assays measuring calcium influx using fluorescent indicators. |
| ln Vivo |
Bepridil hydrochloride hydrate has an average half-life of 33±15 hours following a single dosage [6].
In vivo, Bepridil hydrochloride hydrate is used clinically as an antianginal agent. It has type I antiarrhythmic effects and is a long-acting calcium channel antagonist. The compound was also able to provide protection from Ebola virus and other filoviruses in a mouse model. It has been used in the treatment of angina and may be a possible option in the treatment of atrial fibrillation. However, it is no longer sold in the United States. |
| Enzyme Assay |
For non-cell-based receptor binding assays, Bepridil hydrochloride hydrate can be evaluated using membrane preparations from tissues expressing L-type calcium channels. Radioligand binding displacement experiments are performed using a radiolabeled calcium channel ligand such as [3H]-nitrendipine. Membrane homogenates are incubated with increasing concentrations of the test compound and a fixed concentration of the radioligand at room temperature for 1-2 hours. Bound radioligand is separated from free by rapid filtration through GF/B filters. Nonspecific binding is determined in the presence of excess unlabeled nifedipine. IC50 values are calculated from displacement curves using nonlinear regression analysis.
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| Cell Assay |
For in vitro cellular assays, cardiomyocytes or cell lines expressing calcium channels are cultured in appropriate media. Cells are loaded with calcium-sensitive fluorescent dyes such as Fluo-4 AM. After dye loading, cells are pre-incubated with various concentrations of Bepridil hydrochloride hydrate for 15-30 minutes. Calcium influx is stimulated by the addition of a depolarizing agent such as high potassium buffer. Fluorescence intensity is measured using a fluorescence plate reader. The reduction in calcium signal compared to control wells is used to calculate the IC50 value. Patch-clamp electrophysiology can also be employed for direct measurement of channel current inhibition.
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| Animal Protocol |
For in vivo animal studies, Bepridil hydrochloride hydrate can be administered to rodents via oral gavage or intravenous injection. In models of cardiac arrhythmia, ECG is recorded to assess antiarrhythmic effects. In angina models, exercise tolerance and ST-segment changes are evaluated. In models of viral infection, survival and viral load are assessed. Dosing regimens vary depending on the specific model. Pharmacokinetic studies involve collecting blood samples at various time points post-administration for compound concentration measurement.
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| ADME/Pharmacokinetics |
Bepridil hydrochloride hydrate has a molecular weight of 421.02 and a molecular formula of C24H37ClN2O2. It is a long-acting calcium channel antagonist with antianginal and type I antiarrhythmic effects. The compound is no longer sold in the United States. It may be a possible option in the treatment of atrial fibrillation. It has recently been shown to possess potent activity against SARS-CoV-2 in vitro. It is for research use only.
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| Toxicity/Toxicokinetics |
The toxicity profile of Bepridil hydrochloride hydrate includes potential cardiovascular effects due to its ion channel blocking activity. Common adverse effects may include hypotension, bradycardia, and QT prolongation. The compound is no longer sold in the United States, potentially due to safety concerns or availability of alternative therapies. The compound is for research use only and not for human consumption. Standard toxicological evaluation would include assessment of cardiovascular, respiratory, and central nervous system effects.
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| References | |
| Additional Infomation |
Bepredil hydrochloride is the hydrochloride form of bepredil, a calcium channel blocker and a class IV antiarrhythmic drug. Bepredil hydrochloride blocks calcium ions from entering the blood vessels through calcium channels in the smooth muscle cell membranes of the coronary arteries and peripheral blood vessels, thereby dilating the coronary arteries and peripheral arterioles. This increases oxygen delivery and reduces oxygen demand. This drug is used to treat chronic stable angina and variant angina. It is a long-acting calcium channel blocker with significant antianginal activity. It significantly dilates the coronary arteries and produces mild peripheral vascular effects. It has hypotensive and selective antiarrhythmic effects and acts as a calmodulin antagonist.
Bepridil hydrochloride hydrate ((±)-Bepridil hydrochloride hydrate; Org 5730 hydrochloride hydrate) is a non-selective, long-acting Ca2+ channel antagonist and Na+, K+ channel inhibitor, with antianginal and type I antiarrhythmic effects. It also acts as a cardiac Na+/Ca2+ exchange (NCX1) inhibitor. Bepridil is a clinically used calcium channel blocker with antianginal activity. It has also shown activity against SARS-CoV-2 and Ebola virus in research settings. It is no longer sold in the United States. |
| Molecular Formula |
C24H37CLN2O2
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|---|---|
| Molecular Weight |
421.02
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| Exact Mass |
420.254
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| CAS # |
74764-40-2
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| Related CAS # |
Bepridil hydrochloride;68099-86-5;Bepridil;64706-54-3; 74764-40-2 (HCl hydrate); 99239-96-0 (S-isomer HCl); 110143-75-4 (S-isomer); 110143-74-3 (R-isomer)
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| PubChem CID |
50088
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| Appearance |
Off-white to light yellow solid powder
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| Melting Point |
91 ±2°
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| LogP |
5.505
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| Hydrogen Bond Donor Count |
1
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| Hydrogen Bond Acceptor Count |
3
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| Rotatable Bond Count |
10
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| Heavy Atom Count |
28
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| Complexity |
382
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| Defined Atom Stereocenter Count |
0
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| SMILES |
CC(C)COCC(CN(CC1=CC=CC=C1)C2=CC=CC=C2)N3CCCC3.Cl
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| InChi Key |
JXBBWYGMTNAYNM-UHFFFAOYSA-N
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| InChi Code |
InChI=1S/C24H34N2O.ClH/c1-21(2)19-27-20-24(25-15-9-10-16-25)18-26(23-13-7-4-8-14-23)17-22-11-5-3-6-12-22;/h3-8,11-14,21,24H,9-10,15-20H2,1-2H3;1H
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| Chemical Name |
N-benzyl-N-[3-(2-methylpropoxy)-2-pyrrolidin-1-ylpropyl]aniline;hydrochloride
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| Synonyms |
BEPRIDIL HYDROCHLORIDE; 68099-86-5; Bepridil HCl hydrate; Angopril; 1978CERM; ..
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| HS Tariff Code |
2934.99.9001
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| Storage |
Powder -20°C 3 years 4°C 2 years In solvent -80°C 6 months -20°C 1 month Note: Please store this product in a sealed and protected environment, avoid exposure to moisture. |
| Shipping Condition |
Room temperature (This product is stable at ambient temperature for a few days during ordinary shipping and time spent in Customs)
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| Solubility (In Vitro) |
DMSO: 125 mg/mL (296.90 mM)
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| Solubility (In Vivo) |
Solubility in Formulation 1: ≥ 2.08 mg/mL (4.94 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 20.8 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: ≥ 2.08 mg/mL (4.94 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 20.8 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: ≥ 2.08 mg/mL (4.94 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 | 2.3752 mL | 11.8759 mL | 23.7518 mL | |
| 5 mM | 0.4750 mL | 2.3752 mL | 4.7504 mL | |
| 10 mM | 0.2375 mL | 1.1876 mL | 2.3752 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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