Bepridil HCl hydrate ((±)-Bepridil HCl hydrate) is a non-selective, long-acting calcium ion channel (Ca+ channel) antagonist, sodium ion, potassium ion channel (Na+, K+ channel) inhibitor, with anti-angina and anti-anginal properties. Type I arrhythmic effects. Bepridil HCl hydrate is also a cardiac Na+/Ca2+ exchange (NCX1) inhibitor. Bepridil HCl hydrate may be utilized in cardiovascular disease study.

Physicochemical Properties

Molecular Formula	C24H37CLN2O2
Molecular Weight	421.02
Exact Mass	420.254
CAS #	74764-40-2
Related CAS #	Bepridil hydrochloride;68099-86-5;Bepridil;64706-54-3
PubChem CID	50088
Appearance	Off-white to light yellow solid powder
Melting Point	91 ±2°
LogP	5.505
Hydrogen Bond Donor Count	1
Hydrogen Bond Acceptor Count	3
Rotatable Bond Count	10
Heavy Atom Count	28
Complexity	382
Defined Atom Stereocenter Count	0
InChi Key	JXBBWYGMTNAYNM-UHFFFAOYSA-N
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
Chemical Name	N-benzyl-N-[3-(2-methylpropoxy)-2-pyrrolidin-1-ylpropyl]aniline;hydrochloride
HS Tariff Code	2934.99.9001
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)

Biological Activity

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].
ln Vivo	Bepridil hydrochloride hydrate has an average half-life of 33±15 hours following a single dosage [6].
References	[1]. Pharmacology of Bepridil. Am J Cardiol. 1992 Apr 9;69(11):11D-16D. [2]. Bepridil Blockade of Ca2+-dependent Action Potentials in Vascular Smooth Muscle of Dog Coronary Artery. J Cardiovasc Pharmacol. Jul-Aug 1981;3(4):906-14. [3]. Yasuhide Watanabe. Cardiac Na +/Ca 2+ Exchange Stimulators Among Cardioprotective Drugs. J Physiol Sci. 2019 Nov;69(6):837-849. [4]. Bepridil Block of Cardiac Calcium and Sodium Channels. J Pharmacol Exp Ther. 1986 Apr;237(1):9-17. [5]. Bepridil Differentially Inhibits Two Delayed Rectifier K(+) Currents, I(Kr) and I(Ks), in Guinea-Pig Ventricular Myocytes. Br J Pharmacol. 1999 Dec;128(8):1733-8. [6]. Pharmacokinetics and Metabolism of Bepridil. Am J Cardiol. 1985 Mar 15;55(7):8C-13C.
Additional Infomation	Bepridil Hydrochloride is the hydrochloride salt form of bepridil, a calcium antagonist and class IV anti-arrhythmic agent. Bepridil hydrochloride blocks calcium entry through membranous calcium channels of coronary and peripheral vascular smooth muscle, thereby dilating coronary arteries and peripheral arterioles. This increases oxygen delivery and reduces oxygen requirements. This drug is used to treat chronic stable and variant angina pectoris. A long-acting calcium-blocking agent with significant anti-anginal activity. The drug produces significant coronary vasodilation and modest peripheral effects. It has antihypertensive and selective anti-arrhythmia activities and acts as a calmodulin antagonist.

Solubility Data

Solubility (In Vitro)

DMSO: 125 mg/mL (296.90 mM)

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. 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. 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 corn oil and mix evenly.  (Please use freshly prepared in vivo formulations for optimal results.)

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.