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CAS No.: 116666-63-8

Mibefradil 2HCl/盐酸米贝地尔 Catalog No. CSN11439

Synonyms: Ro 40-5967 dihydrochloride;Ro-40-5967 2HCl;Mibefradil (hydrochloride)

Mibefradil 2HCl is calcium channel blocker with moderate selectivity for T-type Ca2+ channels displaying

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技术信息

生物活性

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 ... more >> Ankara University School Of Medicine, Department of Cardiology Ankara, Turkey, 06230 Collapse <<
NCT01480050	Brain and Central Nervous Syst... more >>em Tumors Collapse <<	Phase 1	Completed	-	United States, Alabama ... more >> 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 Collapse <<
NCT02202993	Glioblastoma Multiforme (GBM)	Phase 1	Completed	-	United States, Connecticut ... more >> Yale University New Haven, Connecticut, United States, 06520 Collapse <<

更多
参考文献

[1] Brain KL, Cuprian AM, et al. The sources and sequestration of Ca(2+) contributing to neuroeffector Ca(2+) transients in the mouse vas deferens. J Physiol. 2003 Dec 1;553(Pt 2):627-35.
[2] Mehrke G, Zong XG, et al. The Ca(++)-channel blocker Ro 40-5967 blocks differently T-type and L-type Ca++ channels. J Pharmacol Exp Ther. 1994 Dec;271(3):1483-8.
[3] Li P, Rubaiy HN, Chen GL, Hallett T, Zaibi N, Zeng B, Saurabh R, Xu SZ. Mibefradil, a T-type Ca2+ channel blocker also blocks Orai channels by action at the extracellular surface. Br J Pharmacol. 2019 Oct;176(19):3845-3856. doi: 10.1111/bph.14788. Epub 2019 Aug 19. PMID: 31271653; PMCID: PMC6780027.

实验方案

计算器摩尔计算器总药量计算器工作液计算器
储存液制备
- 1 mg
- 5 mg
- 10 mg
- 1 mM
- 1.7589 mL
- 8.7943 mL
- 17.5886 mL
- 5 mM
- 0.3518 mL
- 1.7589 mL
- 3.5177 mL
- 10 mM
- 0.1759 mL
- 0.8794 mL
- 1.7589 mL

技术信息

CAS号	116666-63-8	储存条件	粉末 Inert atmosphere,2-8°C 液体 -20°C:3-6 月 -80°C:12月
分子式	C29H40Cl2FN3O3	运输	蓝冰
分子量	568.55	别名	Ro 40-5967 dihydrochloride;Ro-40-5967 2HCl;Mibefradil (hydrochloride);Posicor;Ro 40-5967;Mibefradil 2HCl;盐酸米贝地尔

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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 ... more >> Ankara University School Of Medicine, Department of Cardiology Ankara, Turkey, 06230 Collapse <<
NCT01480050	Brain and Central Nervous Syst... more >>em Tumors Collapse <<	Phase 1	Completed	-	United States, Alabama ... more >> 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 Collapse <<
NCT02202993	Glioblastoma Multiforme (GBM)	Phase 1	Completed	-	United States, Connecticut ... more >> Yale University New Haven, Connecticut, United States, 06520 Collapse <<
NCT01550458	Healthy	Phase 1	Completed	-	United States, Nebraska ... more >> Celerion, Inc. Lincoln, Nebraska, United States, 68502 Collapse <<
NCT01480050	Brain and Central Nervous Syst... more >>em Tumors Collapse <<	Phase 1	Completed	-	United States, Alabama ... more >> 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 Collapse <<
NCT02024919	Coronary Artery Ectasia	Not Applicable	Completed	-	Turkey ... more >> Ankara University School Of Medicine, Department of Cardiology Ankara, Turkey, 06230 Collapse <<
NCT02202993	Glioblastoma Multiforme (GBM)	Phase 1	Completed	-	United States, Connecticut ... more >> Yale University New Haven, Connecticut, United States, 06520 Collapse <<
NCT01550458	Healthy	Phase 1	Completed	-	United States, Nebraska ... more >> Celerion, Inc. Lincoln, Nebraska, United States, 68502 Collapse <<

Mibefradil 2HCl/盐酸米贝地尔 Catalog No. CSN11439

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