Absorption, Distribution and Excretion
Rapid and complete absorption after oral administration. Metabolism/Metabolites Hepatic metabolism. Biological Half-Life 24-50 hours.

Protein Binding

99%

: The relationship between the plasma concentration of bepridil and its efficacy in the treatment of atrial fibrillation in Japanese patients. Biol Pharm Bull. 2012;35(5):672-6.

Bepodil is a tertiary amine with benzyl, phenyl, and 3-(2-methylpropoxy)-2-(pyrrolidine-1-yl)propyl substituents on its nitrogen atom. It has vasodilatory, antiarrhythmic, hypotensive, and calcium channel blocking effects. It is a tertiary amine belonging to the pyrrolidine class of compounds. Bepodil is a long-acting, non-selective calcium channel blocker with significant antianginal activity. It significantly dilates coronary arteries and produces mild peripheral effects. It has hypotensive and selective antiarrhythmic effects and acts as a calmodulin antagonist. This drug has been discontinued in the United States due to its association with ventricular arrhythmias, such as torsades de pointes. This is a long-acting calcium channel blocker with significant antianginal activity. It significantly dilates coronary arteries and produces mild peripheral effects. It has hypotensive and selective antiarrhythmic effects and acts as a calmodulin antagonist. Indications Bepredil is used to treat hypertension and chronic stable angina (classical exertional angina). Mechanism of Action Bepredil inhibits slow (L-type) calcium influx and fast sodium influx in myocardial and vascular smooth muscle, interferes with calcium binding to calmodulin, and blocks voltage-gated and receptor-gated calcium channels. Bepredil inhibits transmembrane influx of calcium ions into myocardial and vascular smooth muscle. In isolated myocardial and vascular smooth muscle preparations, bepredil has been shown to significantly reduce the slope of the calcium dose-response curve and the maximum calcium-induced positive inotropic response. In cultured cardiomyocytes, bepredil binds tightly to actin. Bepredil stably reduces heart rate and arterial blood pressure at rest and specific exercise levels by dilating peripheral arterioles and reducing the total peripheral resistance (afterload) overcome by cardiac work.

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Pharmacodynamics
Bepredil is a calcium channel blocker with well-established antianginal properties, as well as known but not fully elucidated type I antiarrhythmic and antihypertensive properties. Its chemical structure is independent of other calcium channel blockers such as diltiazem hydrochloride, nifedipine, and verapamil hydrochloride.

C24H34N2O

366.53956

366.267

64706-54-3

Bepridil hydrochloride;68099-86-5;Bepridil hydrochloride hydrate;74764-40-2

2351

Typically exists as solid at room temperature

1.054 g/cm3

492.3ºC at 760 mmHg

133.2ºC

1.572

4.768

0

3

10

27

382

0

CC(C)COCC(N1CCCC1)CN(CC2=CC=CC=C2)C3=CC=CC=C3

UIEATEWHFDRYRU-UHFFFAOYSA-N

InChI=1S/C24H34N2O/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

N-Benzyl-N-[3-(2-methylpropoxy)-2-pyrrolidin-1-ylpropyl]aniline

CERM1978CERM 1978 AngoprilCERM-1978 Bepadin.

2934.99.9001

Powder      -20°C    3 years

                     4°C     2 years

In solvent   -80°C    6 months

                  -20°C    1 month

Room temperature (This product is stable at ambient temperature for a few days during ordinary shipping and time spent in Customs)

May dissolve in DMSO (in most cases), if not, try other solvents such as H2O, Ethanol, or DMF with a minute amount of products to avoid loss of samples

Note: Listed below are some common formulations that may be used to formulate products with low water solubility (e.g. < 1 mg/mL), you may test these formulations using a minute amount of products to avoid loss of samples.

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Injection Formulation 1: DMSO : Tween 80： Saline = 10 : 5 : 85 (i.e. 100 μL DMSO stock solution → 50 μL Tween 80 → 850 μL Saline)
*Preparation of saline: Dissolve 0.9 g of sodium chloride in 100 mL ddH ₂ O to obtain a clear solution.
Injection Formulation 2: DMSO : PEG300 ：Tween 80 : Saline = 10 : 40 : 5 : 45 (i.e. 100 μL DMSO → 400 μLPEG300 → 50 μL Tween 80 → 450 μL Saline)
Injection Formulation 3: DMSO : Corn oil = 10 : 90 (i.e. 100 μL DMSO → 900 μL Corn oil)
Example: Take the Injection Formulation 3 (DMSO : Corn oil = 10 : 90) as an example, if 1 mL of 2.5 mg/mL working solution is to be prepared, you can take 100 μL 25 mg/mL DMSO stock solution and add to 900 μL corn oil, mix well to obtain a clear or suspension solution (2.5 mg/mL, ready for use in animals).

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Injection Formulation 4: DMSO : 20% SBE-β-CD in saline = 10 : 90 [i.e. 100 μL DMSO → 900 μL (20% SBE-β-CD in saline)]
*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.
Injection Formulation 5: 2-Hydroxypropyl-β-cyclodextrin : Saline = 50 : 50 (i.e. 500 μL 2-Hydroxypropyl-β-cyclodextrin → 500 μL Saline)
Injection Formulation 6: DMSO : PEG300 : castor oil : Saline = 5 : 10 : 20 : 65 (i.e. 50 μL DMSO → 100 μLPEG300 → 200 μL castor oil → 650 μL Saline)
Injection Formulation 7: Ethanol : Cremophor : Saline = 10： 10 : 80 (i.e. 100 μL Ethanol → 100 μL Cremophor → 800 μL Saline)
Injection Formulation 8: Dissolve in Cremophor/Ethanol (50 : 50), then diluted by Saline
Injection Formulation 9: EtOH : Corn oil = 10 : 90 (i.e. 100 μL EtOH → 900 μL Corn oil)
Injection Formulation 10: EtOH : PEG300：Tween 80 : Saline = 10 : 40 : 5 : 45 (i.e. 100 μL EtOH → 400 μLPEG300 → 50 μL Tween 80 → 450 μL Saline)

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Oral Formulation 1: Suspend in 0.5% CMC Na (carboxymethylcellulose sodium)
Oral Formulation 2: Suspend in 0.5% Carboxymethyl cellulose
Example: Take the Oral Formulation 1 (Suspend in 0.5% CMC Na) as an example, if 100 mL of 2.5 mg/mL working solution is to be prepared, you can first prepare 0.5% CMC Na solution by measuring 0.5 g CMC Na and dissolve it in 100 mL ddH2O to obtain a clear solution; then add 250 mg of the product to 100 mL 0.5% CMC Na solution, to make the suspension solution (2.5 mg/mL, ready for use in animals).

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Oral Formulation 3: Dissolved in PEG400
Oral Formulation 4: Suspend in 0.2% Carboxymethyl cellulose
Oral Formulation 5: Dissolve in 0.25% Tween 80 and 0.5% Carboxymethyl cellulose
Oral Formulation 6: Mixing with food powders

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Note: Please be aware that the above formulations are for reference only. InvivoChem strongly recommends customers to read literature methods/protocols carefully before determining which formulation you should use for in vivo studies, as different compounds have different solubility properties and have to be formulated differently.

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 (Please use freshly prepared in vivo formulations for optimal results.)