Bepridil hydrochloride hydrate
Based on 9 publication(s) in Google Scholar
Bepridil hydrochloride hydrate (CERM 1978 hydrate; Org 5730 hydrochloride hydrate) is an orally active non-selective calcium channel antagonist with multi-ion channel blocking activity. Bepridil hydrochloride hydrate 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 hydrate acts as a hydroxyl radical scavenger, regulates mitochondrial and intracellular calcium handling, and exerts antiarrhythmic, antianginal, and cardioprotective effects. Bepridil hydrochloride hydrate 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 hydrate also exhibits potent inhibitory effects on SARS-CoV-2 replication. Bepridil hydrochloride hydrate 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 : 99.86%
- CAS No.: 74764-40-2
- Formula: C24H37ClN2O2
- Molecular Weight:421.02
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Storage:
4°C, sealed storage, away from moisture
* In solvent : -80°C, 6 months; -20°C, 1 month (sealed storage, away from moisture)
To place orders, for customer services and technical support, please contact: MedChemExpress USA
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Biological Activity
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Chemical Information
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Solvent & Solubility
- Purity & Documentation
- References
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Help & FAQs
Publications Citing Use of MedChemExpress (MCE) Bepridil hydrochloride hydrate
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
More
Biological Activity
Description
IC50 & Target
[2]|
Nav1.5 |
T-type calcium channel |
L-type calcium channel |
In Vitro
Bepridil hydrochloride hydrate 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 hydrate 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 hydrate 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 hydrate 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 hydrate 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 hydrate 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 hydrate 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 hydrate 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.
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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 hydrate (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 hydrate exhibits potent hydroxyl radical scavenging activity in alloxan-induced diabetic mice[1].
Bepridil hydrochloride hydrate (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. 74764-40-2
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Appearance Solid
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Molecular Weight 421.02
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Formula C24H37ClN2O2
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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.[H]O[H]
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Synonyms
CERM 1978 hydrate; Org 5730 hydrochloride hydrate
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Shipping
Room temperature in continental US; may vary elsewhere.
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Storage
4°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 : 125 mg/mL (296.90 mM; Need ultrasonic; Hygroscopic DMSO has a significant impact on the solubility of product, please use newly opened DMSO)
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.
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.
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 (4.94 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 (4.94 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.
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.
Purity & Documentation
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Data Sheet (299 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 |
|---|---|---|---|---|---|
| DMSO | 1 mM | 2.3752 mL | 11.8759 mL | 23.7518 mL | 59.3796 mL |
| 5 mM | 0.4750 mL | 2.3752 mL | 4.7504 mL | 11.8759 mL | |
| 10 mM | 0.2375 mL | 1.1876 mL | 2.3752 mL | 5.9380 mL | |
| 15 mM | 0.1583 mL | 0.7917 mL | 1.5835 mL | 3.9586 mL | |
| 20 mM | 0.1188 mL | 0.5938 mL | 1.1876 mL | 2.9690 mL | |
| 25 mM | 0.0950 mL | 0.4750 mL | 0.9501 mL | 2.3752 mL | |
| 30 mM | 0.0792 mL | 0.3959 mL | 0.7917 mL | 1.9793 mL | |
| 40 mM | 0.0594 mL | 0.2969 mL | 0.5938 mL | 1.4845 mL | |
| 50 mM | 0.0475 mL | 0.2375 mL | 0.4750 mL | 1.1876 mL | |
| 60 mM | 0.0396 mL | 0.1979 mL | 0.3959 mL | 0.9897 mL | |
| 80 mM | 0.0297 mL | 0.1484 mL | 0.2969 mL | 0.7422 mL | |
| 100 mM | 0.0238 mL | 0.1188 mL | 0.2375 mL | 0.5938 mL |
Bepridil hydrochloride hydrate Related Classifications
HY-16952A Related Classifications
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Keywords
- Bepridil hydrochloride
- 74764-40-2
- CERM 1978
- Org 5730 hydrochloride
- CERM1978
- CERM-1978
- 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