| Size | Price | Stock | Qty |
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| 100mg |
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| 250mg |
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| 500mg |
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| 1g |
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| Other Sizes |
| Targets |
Bepridil targets voltage-gated calcium channels as a calcium channel blocker. It blocks calcium entry through membranous calcium channels of coronary and peripheral vascular smooth muscle. Bepridil also activates mitochondrial ATP-sensitive KATP channels. Additionally, it inhibits phosphodiesterase, regulating the breakdown of cyclic nucleotides (cAMP and cGMP). As a class IV anti-arrhythmic agent, it slows cardiac conduction and reduces myocardial contractility.
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| ln Vitro |
Bepridil Hydrochloride is an antianginal calcium channel blocker [1].
In vitro, bepridil is a calcium channel blocker that inhibits calcium influx through voltage-gated calcium channels. It activates mitochondrial ATP-sensitive KATP channels. Bepridil inhibits phosphodiesterase activity, regulating cyclic nucleotide levels. In cell-based assays, bepridil treatment results in reduced calcium influx, vasodilation, and negative inotropic effects on cardiac muscle. The compound's anti-arrhythmic effects are mediated through its actions on calcium channels and phosphodiesterase. |
| ln Vivo |
Rats given 21 mg/kg of bepridil hydrochloride have lower heart rates, mean arterial pressure, decreased mean coronary vascular resistance, and increased stroke volume [1].
In vivo, bepridil hydrochloride was used as a calcium channel blocker and class IV anti-arrhythmic agent for the treatment of angina and atrial fibrillation. It blocks calcium entry through calcium channels, leading to vasodilation and reduced cardiac contractility. Bepridil was approved by the FDA in 1990 for the treatment of chronic/stable angina. However, it is no longer on the market due to safety concerns and the availability of newer agents. |
| Enzyme Assay |
In vitro enzyme assays for bepridil involve measuring its inhibition of phosphodiesterase activity. The enzyme is incubated with varying concentrations of bepridil in the presence of cAMP or cGMP substrate. The hydrolysis of the cyclic nucleotide is measured, and the IC₅₀ is calculated. Calcium channel blocking activity is assessed using patch-clamp electrophysiology in isolated cardiac or vascular smooth muscle cells. These assays confirm the compound's dual mechanism as a calcium channel blocker and phosphodiesterase inhibitor.
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| Cell Assay |
In vitro cell-based assays for bepridil evaluate its effects on calcium signaling and cardiac myocyte function. Cardiac myocytes are cultured and treated with bepridil, and calcium influx is measured using fluorescent calcium indicators. The compound's effects on action potential parameters and contractility are assessed. These assays confirm the compound's functional activity as a calcium channel blocker and anti-arrhythmic agent.
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| Animal Protocol |
In vivo animal experiments for bepridil have been conducted in animal models of angina and arrhythmia. The compound's effects on blood pressure, heart rate, and cardiac contractility are assessed. Bepridil was evaluated in preclinical studies for its efficacy in treating angina and atrial fibrillation. Pharmacokinetic studies were conducted to determine the compound's absorption, distribution, metabolism, and excretion. Comprehensive in vivo studies are available from clinical development.
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| ADME/Pharmacokinetics |
Bepridil is absorbed after oral administration and is metabolized in the liver. It has a molecular weight of 403.00 g/mol. The compound's half-life, bioavailability, and excretion profile have been characterized in clinical studies. Bepridil was approved by the FDA in 1990 for the treatment of chronic/stable angina. However, it is no longer on the market.
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| Toxicity/Toxicokinetics |
The toxicity of bepridil includes pro-arrhythmic effects, including QT prolongation and torsades de pointes. The compound was withdrawn from the market due to safety concerns. Common side effects include gastrointestinal disturbances, headache, and dizziness. Bepridil should be used with caution in patients with cardiac conduction abnormalities. It is no longer available as a prescription medication in many countries.
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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 HCl hydrate is a potent calcium channel blocker and class IV anti-arrhythmic agent once used to treat angina but is no longer on the market. It blocks calcium entry through calcium channels. Bepridil activates mitochondrial KATP channels and inhibits phosphodiesterase. It was FDA-approved in 1990 for chronic/stable angina. Bepridil is no longer marketed due to safety concerns and the availability of newer agents. |
| Molecular Formula |
C24H34N2O.HCL.H2O
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|---|---|
| Molecular Weight |
421.022
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| Exact Mass |
402.244
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| CAS # |
68099-86-5
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| Related CAS # |
Bepridil hydrochloride hydrate;74764-40-2;Bepridil;64706-54-3; 64706-54-3; 68099-86-5 (HCl); 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 |
White to light yellow solid powder
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| Density |
1.054g/cm3
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| Boiling Point |
492.3ºC at 760 mmHg
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| Flash Point |
133.2ºC
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| LogP |
5.57
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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 |
1-Pyrrolideneethanamine, beta-((2-methylpropoxy)methyl)-N-phenyl-N-(phenylmethyl)-, hydrochloride hydrate
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| Synonyms |
CERM 1978; Angopril; Bepadin; Bepridil HCl; CERM1978; CERM-1978; Bepridil hydrochloride
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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 (~310.17 mM)
H2O : ~12.5 mg/mL (~31.02 mM) |
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| Solubility (In Vivo) |
Solubility in Formulation 1: ≥ 2.08 mg/mL (5.16 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 (5.16 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 (5.16 mM) (saturation unknown) in 10% DMSO + 90% Corn Oil (add these co-solvents sequentially from left to right, and one by one), clear solution. Solubility in Formulation 4: 25 mg/mL (62.03 mM) in PBS (add these co-solvents sequentially from left to right, and one by one), clear solution; with ultrasonication. |
| 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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