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盐酸米贝地尔 /Mibefradil 2HCl {[allProObj[0].p_purity_real_show]}

货号:A186181 同义名: 米贝拉地尔 / Ro 40-5967 dihydrochloride;Mibefradil (hydrochloride) Ambeed 开学季,买赠积分,赢豪礼

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

Mibefradil 2HCl 化学结构 CAS号:116666-63-8
Mibefradil 2HCl 化学结构
CAS号:116666-63-8
Mibefradil 2HCl 3D分子结构
CAS号:116666-63-8
Mibefradil 2HCl 化学结构 CAS号:116666-63-8
Mibefradil 2HCl 3D分子结构 CAS号:116666-63-8
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Mibefradil 2HCl 纯度/质量文件 产品仅供科研

货号:A186181 标准纯度: {[allProObj[0].p_purity_real_show]}
批次查询: 批次纯度:

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产品名称 Ca2+ channel-like protein Calcium Channel Cav 2.2 其他靶点 纯度
CDC25B-IN-2 Akt {[allProObj[0].p_purity_real_show]}
Clevidipine {[allProObj[0].p_purity_real_show]}
Verapamil HCl {[allProObj[0].p_purity_real_show]}
Amlodipine {[allProObj[0].p_purity_real_show]}
Amlodipine maleate {[allProObj[0].p_purity_real_show]}
(+)-cis-Diltiazem HCl {[allProObj[0].p_purity_real_show]}
Zegocractin ++

Orai1/STIM1-mediated Ca2+ currents, IC50: 120 nM

{[allProObj[0].p_purity_real_show]}
Tanshinone IIA sulfonate sodium {[allProObj[0].p_purity_real_show]}
Ulixacaltamide ++

hCaV3.1, IC50: 50 nM

hCaV3.2, IC50: 110 nM

{[allProObj[0].p_purity_real_show]}
Dronedarone Hydrochloride {[allProObj[0].p_purity_real_show]}
Nitrendipine +

Calcium channel, IC50: 95 nM

{[allProObj[0].p_purity_real_show]}
Efonidipine HCl monoethanolate {[allProObj[0].p_purity_real_show]}
Cinnarizine {[allProObj[0].p_purity_real_show]}
SEA0400 ++

NCX, IC50: 33 nM

p38 MAPK,ROS,ERK {[allProObj[0].p_purity_real_show]}
Fasudil HCl Rho,PKA {[allProObj[0].p_purity_real_show]}
ML-9 MLCK,Akt {[allProObj[0].p_purity_real_show]}
Flunarizine 2HCl +

Calcium channel, Ki: 68 nM

{[allProObj[0].p_purity_real_show]}
Lomerizine 2HCl {[allProObj[0].p_purity_real_show]}
Efonidipine {[allProObj[0].p_purity_real_show]}
Levamlodipine {[allProObj[0].p_purity_real_show]}
Nisoldipine ++

L-type Cav1.2, IC50: 10 nM

{[allProObj[0].p_purity_real_show]}
Isradipine {[allProObj[0].p_purity_real_show]}
Lacidipine {[allProObj[0].p_purity_real_show]}
Lercanidipine {[allProObj[0].p_purity_real_show]}
Loureirin B Potassium Channel {[allProObj[0].p_purity_real_show]}
Tetracaine HCl {[allProObj[0].p_purity_real_show]}
Manidipine +++

Calcium channel, IC50: 2.6 nM

{[allProObj[0].p_purity_real_show]}
Manidipine Dihydrochlorid +++

Calcium channel, IC50: 2.6 nM

{[allProObj[0].p_purity_real_show]}
Nicardipine {[allProObj[0].p_purity_real_show]}
Wilforgine {[allProObj[0].p_purity_real_show]}
Econazole {[allProObj[0].p_purity_real_show]}
Ginsenoside Rd NF-κB {[allProObj[0].p_purity_real_show]}
Fendiline HCl {[allProObj[0].p_purity_real_show]}
Mesaconitine {[allProObj[0].p_purity_real_show]}
Tetrandrine {[allProObj[0].p_purity_real_show]}
Nifedipine {[allProObj[0].p_purity_real_show]}
Nilvadipine ++++

Calcium channel, IC50: 0.03 nM

{[allProObj[0].p_purity_real_show]}
Barnidipine ++++

[3H]nitrendipine, Ki: 0.21 nM

{[allProObj[0].p_purity_real_show]}
Azelnidipine {[allProObj[0].p_purity_real_show]}
Levetiracetam {[allProObj[0].p_purity_real_show]}
Nimodipine {[allProObj[0].p_purity_real_show]}
Benidipine HCl {[allProObj[0].p_purity_real_show]}
Pinaverium bromide {[allProObj[0].p_purity_real_show]}
Pranidipine {[allProObj[0].p_purity_real_show]}
NP118809 +

L-type calcium channel, IC50: 12.2 μM

N-type Ca2+ channel, IC50: 0.11 μM

{[allProObj[0].p_purity_real_show]}
Amlodipine Besylate +++

Calcium channel, IC50: 1.9 nM

{[allProObj[0].p_purity_real_show]}
Cilnidipine {[allProObj[0].p_purity_real_show]}
Cinepazide Maleate {[allProObj[0].p_purity_real_show]}
Terfenadine {[allProObj[0].p_purity_real_show]}
YM-58483 {[allProObj[0].p_purity_real_show]}
Ranolazine {[allProObj[0].p_purity_real_show]}
Praeruptorin A p38 MAPK,Akt {[allProObj[0].p_purity_real_show]}
Ranolazine 2HCl {[allProObj[0].p_purity_real_show]}
Felodipine ++++

L-type calcium channel, IC50: 0.15 nM

{[allProObj[0].p_purity_real_show]}
PD173212 +++

N-type Ca2+ channel, IC50: 36 nM

{[allProObj[0].p_purity_real_show]}
Levamlodipine besylate {[allProObj[0].p_purity_real_show]}
Carboxyamidotriazole Orotate {[allProObj[0].p_purity_real_show]}
IGS-1.76 {[allProObj[0].p_purity_real_show]}
WH-4-023 ++++

Cav 2.2, IC50: 0.001 μM

++++

Cav 2.2, IC50: 0.001 μM

{[allProObj[0].p_purity_real_show]}
1. 鼠标悬停在“+”上可以显示相关IC50的具体数值。"+"越多,抑制作用越强。2. "✔"表示该化合物对相应的亚型有抑制作用,但抑制强度暂时没有相关数据。

Mibefradil 2HCl 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].

Mibefradil 2HCl 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 <<

Mibefradil 2HCl 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.

Mibefradil 2HCl 实验方案

计算器
存储液制备 1mg 5mg 10mg

1 mM

5 mM

10 mM

1.76mL

0.35mL

0.18mL

8.79mL

1.76mL

0.88mL

17.59mL

3.52mL

1.76mL

Mibefradil 2HCl 技术信息

CAS号116666-63-8
分子式C29H40Cl2FN3O3
分子量 568.551
别名 米贝拉地尔 ;Ro 40-5967 dihydrochloride;Mibefradil (hydrochloride);Ro 40-5967;Posicor;Mibefradil dihydrochloride
运输蓝冰
存储条件

粉末 Inert atmosphere,2-8°C

液体 -20°C:3-6个月-80°C:12个月

溶解度

H2O: 150 mg/mL(263.83 mM),配合低频超声助溶

动物实验配方
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