Bepridil hydrochloride是一种长效的钙通道阻滞剂。
Cas No.:68099-86-5
Sample solution is provided at 25 µL, 10mM.
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Bepridil hydrochloride is a long-acting calcium channel blocker. Bepridil hydrochloride blocks Ca²⁺, Na⁺, and K⁺ channels and inhibits calmodulin. Bepridil hydrochloride can be used in research related to chronic stable angina and arrhythmias[1-4].
In vitro, Bepridil hydrochloride (25-50μM) was used to treat A2058, A375, and C8161 melanoma cells preloaded with Fluo-4 AM (5μM) for 40 minutes. Bepridil hydrochloride significantly increased cytoplasmic Ca²⁺ signal levels; Bepridil hydrochloride (10-50μM) was used to treat A2058 melanoma cells for 18-24 hours, causing G0/G1 phase cell cycle arrest and enhanced apoptosis[5]. Bepridil hydrochloride (0.78–200μM) was used to treat Vero E6 or A549/ACE2 cells infected with SARS-CoV-2 (MOI=0.5) for 3 days and A549/ACE2 cells for 4 days. Bepridil hydrochloride prevented virus-induced cytopathic effects and inhibited viral replication[6].
In vivo, Bepridil hydrochloride (5mg/kg/day) was intraperitoneally injected into NSG mice intravenously transplanted with CLL cells for 20 days. Bepridil hydrochloride significantly reduced the percentage of leukemic cell infiltration in the spleen by enhancing apoptosis and decreasing NOTCH1 activation[7]. Bepridil hydrochloride (12mg/kg) was intraperitoneally injected once or twice daily into BALB/c mice infected with Marburg virus (195PFU) for 10 days. Bepridil hydrochloride significantly increased the survival rate of infected mice[8].
References:
[1] Pang DC, Sperelakis N. Inhibitory action of bepridil (CERM-1978) on calcium binding to cardiac sarcolemma of guinea pig. Biochem Pharmacol. 1981 Aug 15;30(16):2356-8.
[2] Mras S, Sperelakis N. Bepridil (CERM-1978) an verapamil depression of contractions of rabbit aortic rings. Blood Vessels. 1981;18(4-5):196-205.
[3] Mras S, Sperelakis N. Bepridil (CERM-1978) blockade of action potentials in cultured rat aortic smooth muscle cells. Eur J Pharmacol. 1981 Apr 24;71(1):13-9.
[4] Flaim SF, Stranieri MT, Mathiasen JR. Effects of bepridil hydrochloride on cardiocirculatory dynamics, coronary vascular resistance, and cardiac output distribution in normal, conscious rats. J Cardiovasc Pharmacol. 1988 Mar;11(3):363-72.
[5] Liu Z, Cheng Q, Ma X, et al. Suppressing Effect of Na+/Ca2+ Exchanger (NCX) Inhibitors on the Growth of Melanoma Cells. Int J Mol Sci. 2022 Jan 14;23(2):901.
[6] Vatansever EC, Yang KS, Drelich AK, et al. Bepridil is potent against SARS-CoV-2 in vitro. Proc Natl Acad Sci U S A. 2021 Mar 9;118(10):e2012201118.
[7] Baldoni S, Del Papa B, Dorillo E, et al. Bepridil exhibits anti-leukemic activity associated with NOTCH1 pathway inhibition in chronic lymphocytic leukemia. Int J Cancer. 2018 Aug 15;143(4):958-970.
[8] DeWald LE, Dyall J, Sword JM, et al. The Calcium Channel Blocker Bepridil Demonstrates Efficacy in the Murine Model of Marburg Virus Disease. J Infect Dis. 2018 Nov 22;218(suppl_5):S588-S591.
Bepridil hydrochloride是一种长效的钙通道阻滞剂。Bepridil hydrochloride可阻滞Ca²⁺、Na⁺及K⁺通道并抑制钙调蛋白。Bepridil hydrochloride可用于慢性稳定型心绞痛和心律失常的相关研究[1-4]。
在体外，Bepridil hydrochloride（25-50μM）处理预加载Fluo-4 AM（5μM）的A2058、A375和C8161黑色素瘤细胞40分钟。Bepridil hydrochloride显著增加胞质Ca²⁺信号水平；Bepridil hydrochloride（10-50μM）处理A2058黑色素瘤细胞18-24小时，引起G0/G1期细胞周期阻滞和增强凋亡[5]。Bepridil hydrochloride（0.78–200μM）处理SARS-CoV-2（MOI=0.5）感染的Vero E6或A549/ACE2细胞3天及A549/ACE2细胞4天。Bepridil hydrochloride可预防病毒诱导的细胞病变效应，同时抑制病毒复制[6]。
在体内，Bepridil hydrochloride（5mg/kg/day）腹腔注射于静脉移植CLL细胞的NSG小鼠，持续20天。Bepridil hydrochloride显著减少了脾脏中白血病细胞浸润的百分比，通过增强凋亡和降低NOTCH1激活[7]。Bepridil hydrochloride（12mg/kg）每天一次或两次腹腔注射于感染马尔堡病毒（195PFU）的BALB/c小鼠，持续10天。Bepridil hydrochloride显著提高了感染小鼠的存活率[8]。
| Cell experiment [1]: | |
Cell lines | Vero E6 (kidney epithelial cell line from African green monkey) and A549/ACE2 (human alveolar basal epithelial adenocarcinoma cells stably transduced with human ACE2 viral receptor) |
Preparation Method | Vero E6 and A549/ACE2 cells were treated with Bepridil hydrochloride (0.78–200μM) and infected with SARS-CoV-2 at a multiplicity of infection (MOI) of 0.5. Infected cells were then cultured for 3 days (Vero E6) or 4 days (A549/ACE2) before assessing the yields of infectious progeny virus. |
Reaction Conditions | 0.78–200μM; 3-4 days |
Applications | Bepridil hydrochloride completely prevented SARS-CoV-2-induced cytopathogenic effect (CPE) in both Vero E6 and A549/ACE2 cells at concentrations reaching 6.25μM, with no observed cytotoxicity under microscopy. The EC50 values for inhibiting SARS-CoV-2 infection were estimated to be 0.86μM in Vero E6 cells and 0.46μM in A549/ACE2 cells. Bepridil hydrochloride showed no toxicity to Vero E6 and A549/ACE2 cells until its concentration reached above 25μM and 50μM, respectively. |
| Animal experiment [2]: | |
Animal models | NSG (NOD scid gamma) mice |
Preparation Method | A total of 1.0×10⁸ CLL cells were intravenously transplanted into 8-week-old NSG mice after sublethal irradiation (3.5Gy). Mice were treated with Bepridil hydrochloride (5mg/kg) daily over a 20-day period. Mice were killed 4 weeks after transplant for analysis of the percentage of human CD45+ CD5+ CD19+ CLL cells infiltrating the spleen. |
Dosage form | 5mg/kg; i.p.; daily for 20 days |
Applications | Bepridil hydrochloride significantly reduced the percentage of leukemic cells infiltrating the spleen via enhanced apoptosis and decreased NOTCH1 activation. |
References: | |
| Cas No. | 68099-86-5 | SDF | |
| 别名 | 1-异丁氧基-2-吡咯烷基-3-(N-苄基苯胺基)丙烷盐酸盐,CERM 1978 | ||
| 化学名 | (R)-N-benzyl-N-(3-isobutoxy-2-(pyrrolidin-1-yl)propyl)aniline hydrochloride | ||
| Canonical SMILES | CC(C)COC[C@@H](CN(C1=CC=CC=C1)CC2=CC=CC=C2)N3CCCC3.Cl | ||
| 分子式 | C24H34N2O.HCl | 分子量 | 403 |
| 溶解度 | DMF: 20 mg/mL,DMSO: 5 mg/mL,Ethanol: 25 mg/mL,Ethanol:PBS (pH 7.2)(1:2): 0.3 mg/mL | 储存条件 | Desiccate at RT |
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| 制备储备液 | |||
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1 mg | 5 mg | 10 mg |
| 1 mM | 2.4814 mL | 12.4069 mL | 24.8139 mL |
| 5 mM | 496.3 μL | 2.4814 mL | 4.9628 mL |
| 10 mM | 248.1 μL | 1.2407 mL | 2.4814 mL |
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