货号:A186181 同义名: 米贝拉地尔 / Ro 40-5967 dihydrochloride;Mibefradil (hydrochloride)
Mibefradil 2HCl is calcium channel blocker with moderate selectivity for T-type Ca2+ channels displaying
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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。 |
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]. |
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 << |
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 |
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 |