产品说明书
Mibefradil 2HCl
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同义名 : | 米贝拉地尔 ;Ro 40-5967 dihydrochloride;Mibefradil (hydrochloride);Ro 40-5967;Posicor;Mibefradil dihydrochloride |
| CAS号 : | 116666-63-8 | |
| 货号 : | A186181 | |
| 分子式 : | C29H40Cl2FN3O3 | |
| 纯度 : | 98%+ | |
| 分子量 : | 568.551 | |
| MDL号 : | MFCD00881804 | |
| 存储条件： |
粉末 Inert atmosphere,2-8°C 液体 -20°C:3-6个月-80°C:12个月 |
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| 溶解度 : |
H2O: 150 mg/mL(263.83 mM)，配合低频超声助溶 |
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| 动物实验配方： |
| 生物活性 | |||
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| 描述 | Mibefradil Dihydrochloride, a potent T‐type voltage‐gated calcium channel (VGCC) blocker , has been investigated for treating solid tumours. It blocks all three subtypes of T‐type channel, that is, Cav3.1, Cav3.2, and Cav3.3 channels, with an IC50 of 5.8-7.2 μM[3]. In vitro research suggests that Mibefradil potently inhibited the proliferation of vascular endothelial cells. Mibefradil treatment increased the HK‐2 cell numbers at G0/G1 phase and decreased the cell numbers in G2/M, suggesting the cell cycle progressing from G1 to S, and G2 to M phase is arrested. However, high concentrations of mibefradil (i.e., more than 25 μM) could show nonspecific cytotoxicity by stimulating apoptosis and reducing the cell population at G0/G1 phase[3]. | ||
| 临床研究 | |||||
|---|---|---|---|---|---|
| NCT号 | 适应症或疾病 | 临床期 | 招募状态 | 预计完成时间 | 地点 |
| NCT02024919 | Coronary Artery Ectasia | Not Applicable | Completed | - | Turkey ... 展开 >> Ankara University School Of Medicine, Department of Cardiology Ankara, Turkey, 06230 收起 << |
| NCT01480050 | Brain and Central Nervous Syst... 展开 >>em Tumors 收起 << | Phase 1 | Completed | - | United States, Alabama ... 展开 >> UAB Comprehensive Cancer Center Birmingham, Alabama, United States, 35294-3410 United States, Georgia Winship Cancer Institute of Emory University Atlanta, Georgia, United States, 30322 United States, Maryland Johns Hopkins University Baltimore, Maryland, United States, 21205 United States, Michigan Henry Ford Hospital Detroit, Michigan, United States, 48202 United States, North Carolina Wake Forest University Comprehensive Cancer Center Winston-Salem, North Carolina, United States, 27157-1096 United States, Pennsylvania Abramson Cancer Center of the University of Pennsylvania Philadelphia, Pennsylvania, United States, 19104-4283 Hillman Cancer Center at University of Pittsburgh Cancer Institute Pittsburgh, Pennsylvania, United States, 15232 收起 << |
| NCT02202993 | Glioblastoma Multiforme (GBM) | Phase 1 | Completed | - | United States, Connecticut ... 展开 >> Yale University New Haven, Connecticut, United States, 06520 收起 << |
| 实验方案 | |||
|---|---|---|---|
| 1mg | 5mg | 10mg | |
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1 mM 5 mM 10 mM |
1.76mL 0.35mL 0.18mL |
8.79mL 1.76mL 0.88mL |
17.59mL 3.52mL 1.76mL |
| 参考文献 |
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