Bepridil hydrochloride
Based on 9 publication(s) in Google Scholar
Bepridil hydrochloride (CERM 1978; Org 5730 hydrochloride) is an orally active non-selective calcium channel antagonist with multi-ion channel blocking activity. Bepridil hydrochloride modulates Calmodulin, the 20S proteasome, T-type/L-type calcium channels, cardiac sodium channels, multiple potassium channels, γ-secretase, β-secretase, and mitoKATP/sarcKATP channels. Bepridil hydrochloride acts as a hydroxyl radical scavenger, regulates mitochondrial and intracellular calcium handling, and exerts antiarrhythmic, antianginal, and cardioprotective effects. Bepridil hydrochloride alters amyloid precursor protein processing, reduces β-amyloid and thalamic calcium levels, restores seladin-1/DHCR24 expression, and improves sensorimotor recovery after cerebral ischemia. Bepridil hydrochloride also exhibits potent inhibitory effects on SARS-CoV-2 replication. Bepridil hydrochloride is used in studies related to stable angina, arrhythmias, cerebral ischemia, Alzheimer's disease, and SARS-CoV-2 infection.
For research use only. We do not sell to patients.
- Purity : 99.98%
- CAS No.: 68099-86-5
- Formula: C24H35ClN2O
- Molecular Weight:403.00
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Storage:
-20°C, sealed storage, away from moisture
* In solvent : -80°C, 6 months; -20°C, 1 month (sealed storage, away from moisture)
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Biological Activity
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Chemical Information
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Solvent & Solubility
- Protocols
- Purity & Documentation
- References
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Help & FAQs
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Publications Citing Use of MedChemExpress (MCE) Bepridil hydrochloride
More- Autophagy. 2026 Mar 5. [Abstract]
- Acta Pharmacol Sin. 2025 May;46(5):1190-1204. [Abstract]
- Eur J Pharm Sci. 2023 Aug 1:187:106475. [Abstract]
- Eur J Pharm Sci. 2021 Sep 1:164:105889. [Abstract]
- Virology. 2020 Jan 2:539:38-48. [Abstract]
- Biochem Biophys Res Commun. 2025 Oct 30:786:152756. [Abstract]
- bioRxiv. 2025 Nov 21:2025.11.20.689520. [Abstract]
- Research Square Preprint. 2024 Feb 9.
- Università Vita-Salute San Raffaele. 2022 Apr 08. 34.
All Calcium Channel Isoforms
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Biological Activity
Description
IC50 & Target
[2]|
Nav1.5 |
T-type calcium channel |
L-type calcium channel |
In Vitro
Bepridil hydrochloride accumulates extensively in cat ileal smooth muscle, chick ventricular muscle, rabbit papillary muscle, and rat ventricular myocytes; it inhibits ATP-dependent calcium uptake in isolated rat and rabbit heart mitochondria; and it exhibits potent hydroxyl radical scavenging activity in cell-free in vitro assays[1].
Bepridil hydrochloride exerts bidirectional regulation on sodium currents in neonatal rat cardiomyocytes: short-term exposure inhibits INa (IC50 = 96.3 mM), while long-term exposure (EC50 = 9.5 mM) upregulates Na+ currents by inhibiting 20S proteasome-mediated degradation of Nav1.5 protein[2].
Bepridil hydrochloride directly inhibits purified 20S proteasome activity in a concentration-dependent manner in vitro; HEK‑Nav1.5 cell experiments confirm that its effect of upregulating Na+ current does not depend on the expression of cardiomyocyte-specific Ca2+ channels[2].
Bepridil hydrochloride blocks Kir6.2+SUR2A sarcKATP channel currents in HEK-293 cells and opens mitoKATP channels in a concentration-dependent manner (EC50 = 27.5 nM), leading to flavoprotein oxidation, attenuation of Ouabain (HY-B1457)-induced mitochondrial Ca2+ overload, and improvement of post-ischemic contractile function recovery in guinea pig cardiac preparations[4].
Bepridil hydrochloride reduces myocardial contractility, heart rate, and oxygen consumption in isolated perfused rabbit hearts, and its coronary vasodilatory effect occurs only at low flow rates[1].
Bepridil hydrochloride reduces the electrical activity of rabbit sinoatrial node cells by inhibiting the slow inward current, and at concentrations of 4-6 mmol/L, it decreases the automaticity of isolated rabbit sinoatrial node tissue, slows conduction, and prolongs the refractory period[1].
Bepridil hydrochloride exerts differential repolarization effects on myocardial tissues of rabbits and dogs: it shortens the action potential duration of Purkinje fibers while prolonging that of ventricular muscle, and this effect is dose-dependent within the range of 0.1 to 10 mg/L; it also restores ATP content and cell viability in hypoxic rat ventricular myocytes[1].
Bepridil hydrochloride accelerates the recovery of ischemia-induced end-diastolic contracture during reperfusion in isolated perfused rat hearts via coronary vasodilation, an effect independent of its negative inotropic activity[1].
MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only. Further protocols information, click here.
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Cell Line:neonatal rat cardiomyocytes
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Concentration:10 mM
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Incubation Time:24, 48 h
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Result:Did not modify the mRNA levels of Na_v1.5 and all tested Na_v β subunits (β1, β2, β3, β4).
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Cell Line:neonatal rat cardiomyocytes
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Concentration:10 mM (protein expression)
10 mM + 10 μg/mL Cycloheximide (HY-12320) (protein degradation assay; INa with Cycloheximide) -
Incubation Time:24 h (protein expression; INa with Cycloheximide)
3, 6, 12 h (protein degradation assay) -
Result:Increased Na_v1.5 protein expression by 54% after treatment with 10 mM for 24 h.
Did not significantly affect Na_vβ protein expression after treatment with 10 mM for 24 h.
Augmented INa by 64.6% in the presence of Cycloheximide after 24 h.
Significantly slowed the time course of Na_v1.5 protein degradation.
In Vivo
Bepridil hydrochloride (1.25-5 mg/kg; i.v.; single dose) exerts negative chronotropic and negative dromotropic effects in anesthetized and conscious dogs, reducing heart rate in intact or denervated canine hearts, increasing coronary blood flow and oxygenation levels; in conscious dogs with chronic heart block, it produces a biphasic chronotropic response that includes an initial reflex tachycardia, while in anesthetized dogs it induces direct negative chronotropic and transient vasodilatory hemodynamic effects, with sustained reductions in heart rate and myocardial oxygen consumption[1].
Bepridil hydrochloride exhibits potent hydroxyl radical scavenging activity in alloxan-induced diabetic mice[1].
Bepridil hydrochloride (50 mg/kg; p.o.; once daily; for 27 consecutive days) reduces soluble Aβ42 by 57% and calcium levels by 71% in the ipsilateral thalamus of rats after transient middle cerebral artery occlusion, restores seladin-1 expression, and improves forelimb sensorimotor function in rats[3].
MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.
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Animal Model:Wistar (male; 2-3 months old; 295-344 g; transient middle cerebral artery occlusion induced by intraluminal filament technique with 120 min occlusion)[3]
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Dosage:50 mg/kg
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Administration:p.o.; once daily; 27 days (starting 2 days post-MCAO)
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Result:Reduced soluble Aβ40 (by 46 %) and soluble Aβ42 (by 57 %), insoluble guanidine‑soluble Aβ42, and calcium (by 71 %) in the ipsilateral thalamus versus vehicle‑treated MCAO rats, mitigated MCAO‑provoked APP‑processing disturbances, restrained APP C‑terminal fragment elevation and total‑APP decline, and blunted the rise of total soluble APP to ~1.8‑fold.
Restored seladin‑1/DHCR24 mRNA and protein, lowered HMOX1 mRNA by an average of 30 %, improved impaired contralateral‑forelimb performance at postoperative day 28 in the cylinder test.
Showed no significant alterations in limb‑placing and beam‑walking test results.
Failed to reverse the ~10‑fold GFAP protein elevation and ~3.5‑fold TNF‑α mRNA up‑regulation in the ipsilateral thalamus of MCAO rats.
Chemical Information
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CAS No. 68099-86-5
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Appearance Solid
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Molecular Weight 403.00
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Formula C24H35ClN2O
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Color White to light yellow
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SMILES
CC(C)COCC(N1CCCC1)CN(C2=CC=CC=C2)CC3=CC=CC=C3.[H]Cl
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Synonyms
CERM 1978; Org 5730 hydrochloride
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Shipping
Room temperature in continental US; may vary elsewhere.
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Storage
-20°C, sealed storage, away from moisture
* In solvent : -80°C, 6 months; -20°C, 1 month (sealed storage, away from moisture)
Publications (9)
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Journal Impact Factor
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Most Recent
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Autophagy
2026 Mar 5. PMID: 41787744 -
Acta Pharmacol Sin
Electrophysiological characterization of human KCNT1 channel modulators and the therapeutic potential of hydroquinine and tipepidine in KCNT1 mutation-associated epilepsy mouse model. [Abstract]2025 May;46(5):1190-1204. PMID: 39870847 -
Eur J Pharm Sci
Investigating the relevance of CYP2J2 inhibition for drugs known to cause intermediate to high risk torsades de pointes. [Abstract]2023 Aug 1:187:106475. PMID: 37225005 -
Eur J Pharm Sci
Atypical kinetics of cytochrome P450 2J2: Epoxidation of arachidonic acid and reversible inhibition by xenobiotic inhibitors. [Abstract]2021 Sep 1:164:105889. PMID: 34044117 -
Virology
2020 Jan 2:539:38-48. PMID: 31670218 -
Biochem Biophys Res Commun
Dual-cardiotoxicity evaluation of torsadogenic risk drugs using human iPSC-derived cardiomyocytes. [Abstract]2025 Oct 30:786:152756. PMID: 41043280 -
bioRxiv
2025 Nov 21:2025.11.20.689520. PMID: 41332603 -
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Solvent & Solubility
In Vitro:
DMSO : 100 mg/mL (248.14 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)
H2O : 12.5 mg/mL (31.02 mM; Need ultrasonic)
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 (sealed storage, away from moisture). When stored at -80°C, please use it within 6 months. When stored at -20°C, please use it within 1 month.
* Note: If you choose water as the stock solution, please dilute it to the working solution, then filter and sterilize it with a 0.22 μm filter before use.
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 (sealed storage, away from moisture). When stored at -80°C, please use it within 6 months. When stored at -20°C, please use it within 1 month.
* Note: If you choose water as the stock solution, please dilute it to the working solution, then filter and sterilize it with a 0.22 μm filter before use.
Concentration (start) × Volume (start) = Concentration (final) × Volume (final)
In Vivo:
Select the appropriate dissolution method based on your experimental animal and administration route.
- 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.
Add each solvent one by one: 10% DMSO 40% PEG300 5% Tween-80 45% Saline
Solubility: ≥ 2.08 mg/mL (5.16 mM); Clear solution
This protocol yields a clear solution of ≥ 2.08 mg/mL (saturation unknown).
Taking 1 mL working solution as an example, add 100 μL DMSO stock solution (20.8 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.
Preparation of Saline: Dissolve 0.9 g sodium chloride in ddH₂O and dilute to 100 mL to obtain a clear Saline solution.
Add each solvent one by one: 10% DMSO 90% (20% SBE-β-CD in Saline)
Solubility: ≥ 2.08 mg/mL (5.16 mM); Clear solution
This protocol yields a clear solution of ≥ 2.08 mg/mL (saturation unknown).
Taking 1 mL working solution as an example, add 100 μL DMSO stock solution (20.8 mg/mL) to 900 μL 20% SBE-β-CD in Saline, and mix evenly.
Preparation of 20% SBE-β-CD in Saline (4°C, storage for one week): 2 g SBE-β-CD powder is dissolved in 10 mL Saline, completely dissolve until clear.
For the following dissolution methods, please prepare the working solution directly:
It is recommended to prepare fresh solutions and use them promptly within a short period of time.
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.
Add each solvent one by one: PBS
Solubility: 25 mg/mL (62.03 mM); Clear solution; Need ultrasonic
In Vivo Dissolution Calculator
Please enter the basic information of animal experiments:
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Recommended: Prepare an additional quantity of animals to account for potential losses during experiments.
Please enter your animal formula composition:
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%DMSO +
Recommended: Keep the proportion of DMSO in working solution below 2% if your animal is weak.
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%+
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+%Tween-80 + +
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%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
Method for preparing stock solution: mg drug dissolved in μL DMSO. Stock solution concentration: mg/mL. * In solvent : -80°C, 6 months; -20°C, 1 month (sealed storage, away from moisture)
1. Take μL DMSO stock solution;
2. Add μL .
μL , mix evenly;
3. Then add μL Tween 80, mix evenly;
4. Then add μL
Please ensure that the stock solution in the first step is dissolved to a clear state, and add co-solvents in sequence. You can use ultrasonic heating (ultrasonic cleaner, recommended frequency 20-40 kHz), vortexing, etc. to assist dissolution.
Protocols
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RNA extraction experimental
By lysing cells, releasing RNA, and removing impurities such as proteins and DNA, high-purity RNA products are finally obtained. The commonly used traditional method is the guanidine isothiocyanate/phenol/chloroform method (Trizol), which is suitable for a variety of animal materials including animal tissues, microorganisms, cultured cells, etc., and most plant materials.
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Research Protocol for Infectious Diseases
Infectious-disease experiments test how pathogens interact with host barriers, innate immune receptors, inflammatory signaling, pathogen replication, and tissue injury; pattern-recognition receptors such as TLRs, RIG-I-like receptors, NOD-like receptors, and inflammasomes detect microbial molecules and activate NF-κB, interferon, and cytokine responses. The central hypothesis is that infection severity reflects the balance between pathogen burden and host response: protective inflammation restricts pathogen growth, whereas excessive or mislocalized inflammation contributes to tissue damage and disease phenotype. Unresolved questions include which host pathways are protective versus pathogenic, why some infection models fail to translate to human disease, and which combined readouts best predict clinically relevant infection outcomes.
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Two-electrode voltage clamp in Xenopus oocytes
Two-electrode voltage clamp measures whole-oocyte membrane current from Xenopus oocytes expressing exogenous ion channels, receptors, or transporters; one intracellular microelectrode senses membrane voltage, and the second injects current so the amplifier can hold the membrane at command voltages while recording the compensating current as the functional readout. The method is suited to Xenopus oocytes because their large size supports microinjection and intracellular electrode impalement, but the large membrane area can limit voltage-clamp speed and accuracy, especially for large or fast currents.
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Calcium Spark Assay
Calcium sparks are localized, transient increases in intracellular calcium concentration ([Ca2+]i) that occur in cardiac myocytes and represent elementary events underlying excitation-contraction coupling. These events are generated by the coordinated opening of clusters of ryanodine receptors (RyRs) on the sarcoplasmic reticulum membrane, leading to a brief release of Ca2+ into the cytosol. The detection and analysis of calcium sparks provide insights into the mechanisms of calcium handling and signaling in cardiac cells. Imaging techniques using fluorescent calcium indicators such as Fluo-3 are employed to visualize these subcellular calcium transients with high spatial and temporal resolution. The protocol is based on established methodologies described in primary literature for both experimental measurement and automated analysis of calcium sparks.
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Notch Pathway Solutions
The Notch pathway is a contact-dependent signaling pathway that controls cell-fate decisions, differentiation, proliferation, and tissue patterning through interactions between membrane-bound Notch receptors and membrane-bound ligands on neighboring cells. Canonical Notch signaling is activated when ligand engagement triggers proteolytic release of the Notch intracellular domain, which enters the nucleus and regulates transcription together with DNA-binding transcriptional complexes. In the canonical mechanism, ligand-dependent Notch activation leads to release of the intracellular Notch domain, and presenilin-dependent γ-secretase activity is required for production of the active intracellular signaling fragment. The released intracellular domain functions as a nuclear signal that converts Notch receptor activation at the membrane into transcriptional regulation of target programs such as HES/HEY-family genes and other context-dependent downstream targets. The literature links Notch p
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Ca2+ Staining Technique
Ca2+ staining is an experimental technique that utilizes specific fluorescent probes (such as Fluo-4 AM, Fura-2, etc.) to qualitatively or quantitatively detect dynamic changes in intracellular Ca2+ concentrations; this is achieved by monitoring the changes in fluorescent signals generated when these probes bind to free intracellular calcium ions. The underlying principle relies primarily on the presence of chelating groups within the probe's molecular structure that possess high affinity for calcium ions.
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Amyloid: Congo Red Amyloid Staining
Congo red amyloid staining is a histochemical method used to detect extracellular amyloid deposits in tissue sections based on the affinity of Congo red dye for β-pleated sheet-rich protein aggregates. When bound to amyloid, Congo red produces characteristic apple-green birefringence under polarized light microscopy, which is widely regarded as a diagnostic feature of amyloid deposition in histopathology. The diagnostic principle relies on the combination of dye binding (congophilia) and optical anisotropy under polarized illumination, which distinguishes amyloid from most non-amyloid eosinophilic extracellular deposits in routine histological evaluation. Amyloid identification by Congo red staining remains a cornerstone in diagnostic pathology despite the availability of adjunct methods such as immunohistochemistry and mass spectrometry, particularly because of its ability to localize deposits directly within tissue architecture. The specificity of Congo red-positive deposits is incre
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Alzheimer’s Disease Modeling
Alzheimer’s Disease (AD) is a neurodegenerative disorder characterized by a progressive decline in cognitive functions and loss of specific types of neurons and synapses. Alzheimer's symptoms can be simulated in mice by injecting drugs (such as Aβ) or genetically modified.
Purity & Documentation
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Data Sheet (297 KB)
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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)
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Handling Instructions (2659 KB)
References
[2]. Kang L, et al. Bepridil up-regulates cardiac Na+ channels as a long-term effect by blunting proteasome signals through inhibition of calmodulin activity. British journal of pharmacology. 2009 Jun;157(3):404-14. [Content Brief]
[4]. Sato T, et al. Bepridil, an antiarrhythmic drug, opens mitochondrial KATP channels, blocks sarcolemmal KATP channels, and confers cardioprotection. The Journal of pharmacology and experimental therapeutics. 2006 Jan;316(1):182-8. [Content Brief]
Complete Stock Solution Preparation Table
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 (sealed storage, away from moisture). 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 |
|---|---|---|---|---|---|
| H2O / DMSO | 1 mM | 2.4814 mL | 12.4069 mL | 24.8139 mL | 62.0347 mL |
| 5 mM | 0.4963 mL | 2.4814 mL | 4.9628 mL | 12.4069 mL | |
| 10 mM | 0.2481 mL | 1.2407 mL | 2.4814 mL | 6.2035 mL | |
| 15 mM | 0.1654 mL | 0.8271 mL | 1.6543 mL | 4.1356 mL | |
| 20 mM | 0.1241 mL | 0.6203 mL | 1.2407 mL | 3.1017 mL | |
| 25 mM | 0.0993 mL | 0.4963 mL | 0.9926 mL | 2.4814 mL | |
| 30 mM | 0.0827 mL | 0.4136 mL | 0.8271 mL | 2.0678 mL | |
| DMSO | 40 mM | 0.0620 mL | 0.3102 mL | 0.6203 mL | 1.5509 mL |
| 50 mM | 0.0496 mL | 0.2481 mL | 0.4963 mL | 1.2407 mL | |
| 60 mM | 0.0414 mL | 0.2068 mL | 0.4136 mL | 1.0339 mL | |
| 80 mM | 0.0310 mL | 0.1551 mL | 0.3102 mL | 0.7754 mL | |
| 100 mM | 0.0248 mL | 0.1241 mL | 0.2481 mL | 0.6203 mL |
* Note: If you choose water as the stock solution, please dilute it to the working solution, then filter and sterilize it with a 0.22 μm filter before use.
Bepridil hydrochloride Related Classifications
HY-103315 Related Classifications
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Keywords
- Bepridil
- 68099-86-5
- CERM 1978
- Org 5730
- CERM1978
- CERM-1978
- Org5730
- Org-5730
- Calcium Channel
- Sodium Channel
- Potassium Channel
- SARS-CoV
- Beta-secretase
- Amyloid-β
- Proteasome
- γ-secretase
- Calmodulin
- T-type/L-type calcium channels
- sodium-calcium exchanger
- β-secretase
- Na_v1.5
- cardiac sodium channels
- 20S proteasome
- mitoKATP/sarcKATP channels
- calcium channel modulator
- calmodulin
- Inhibitor
- inhibitor
- inhibit