Bepridil hydrochloride hydrate
(Synonyms: 盐酸苄普地尔,(±)-Bepridil hydrochloride hydrate; Org 5730 hydrochloride hydrate) 目录号 : GC39743
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Bepridil hydrochloride hydrate是一种长效的钙通道阻滞剂。
Cas No.:74764-40-2
Sample solution is provided at 25 µL, 10mM.
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Bepridil hydrochloride hydrate is a long-acting calcium channel blocker. Bepridil hydrochloride hydrate blocks Ca²⁺, Na⁺, and K⁺ channels and inhibits calmodulin. Bepridil hydrochloride hydrate can be used in research related to chronic stable angina and arrhythmias[1-4].
In vitro, Bepridil hydrochloride hydrate (25-50μM) was used to treat A2058, A375, and C8161 melanoma cells preloaded with Fluo-4 AM (5μM) for 40 minutes. Bepridil hydrochloride hydrate significantly increased cytoplasmic Ca²⁺ signal levels; Bepridil hydrochloride hydrate (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 hydrate (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 hydrate prevented virus-induced cytopathic effects and inhibited viral replication[6].
In vivo, Bepridil hydrochloride hydrate (5mg/kg/day) was intraperitoneally injected into NSG mice intravenously transplanted with CLL cells for 20 days. Bepridil hydrochloride hydrate significantly reduced the percentage of leukemic cell infiltration in the spleen by enhancing apoptosis and decreasing NOTCH1 activation[7]. Bepridil hydrochloride hydrate (12mg/kg) was intraperitoneally injected once or twice daily into BALB/c mice infected with Marburg virus (195PFU) for 10 days. Bepridil hydrochloride hydrate 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 hydrate 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 hydrate是一种长效的钙通道阻滞剂。Bepridil hydrochloride hydrate可阻滞Ca²⁺、Na⁺及K⁺通道并抑制钙调蛋白。Bepridil hydrochloride hydrate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 hydrate（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 hydrate显著增加胞质Ca²⁺信号水平；Bepridil hydrochloride hydrate（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 hydrate（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 hydrate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 hydrate（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 hydrate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 hydrate（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 hydrate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 hydrate (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 hydrate 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 hydrate 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 hydrate (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 hydrate significantly reduced the percentage of leukemic cells infiltrating the spleen via enhanced apoptosis and decreased NOTCH1 activation. |
References: | |
| Cas No. | 74764-40-2 | SDF | |
| 别名 | 盐酸苄普地尔,(±)-Bepridil hydrochloride hydrate; Org 5730 hydrochloride hydrate | ||
| Canonical SMILES | CC(C)COCC(N1CCCC1)CN(C2=CC=CC=C2)CC3=CC=CC=C3.[H]Cl.[H]O[H] | ||
| 分子式 | C24H37ClN2O2 | 分子量 | 421.02 |
| 溶解度 | DMSO: ≥ 250 mg/mL (593.80 mM) | 储存条件 | Store at -20°C |
| General tips | 请根据产品在不同溶剂中的溶解度选择合适的溶剂配制储备液；一旦配成溶液，请分装保存，避免反复冻融造成的产品失效。 储备液的保存方式和期限：-80°C 储存时，请在 6 个月内使用，-20°C 储存时，请在 1 个月内使用。 为了提高溶解度，请将管子加热至37℃，然后在超声波浴中震荡一段时间。 |
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| Shipping Condition | 评估样品解决方案：配备蓝冰进行发货。所有其他可用尺寸：配备RT，或根据请求配备蓝冰。 | ||
| 制备储备液 | |||
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1 mg | 5 mg | 10 mg |
| 1 mM | 2.3752 mL | 11.8759 mL | 23.7518 mL |
| 5 mM | 475 μL | 2.3752 mL | 4.7504 mL |
| 10 mM | 237.5 μL | 1.1876 mL | 2.3752 mL |
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| 给药剂量 | mg/kg |  |
动物平均体重 | g | |
每只动物给药体积 | ul | |
动物数量 | 只 |
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| % DMSO % % Tween 80 % saline | ||||||||||
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工作液浓度： mg/ml；
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2.
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Quality Control & SDS
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- Purity: >98.00% Appearance: A solid
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