1. Membrane Transporter/Ion Channel Neuronal Signaling
  2. Calcium Channel
  3. Mibefradil

Mibefradil (Ro 40-5967) is a calcium channel blocker with moderate selectivity for T-type Ca2+ channels displaying IC50s of 2.7 μM and 18.6 μM for T-type and L-type currents, respectively.

The free form of the compound is prone to instability, it is advisable to consider the stable salt form (Mibefradil dihydrochloride) that retains the same biological activity.

商品は「研究用試薬」です。人や動物の医療用・臨床診断用・食品用の製品ではありません。
研究用途以外に使用した場合、当社は一切の責任を負いかねます。

Mibefradil

Mibefradil 構造式

CAS 番号 : 116644-53-2

容量 価格(税別) 在庫状況
1 mg $140 見積もりとリードタイムを求めるのご確認
5 mg $350 見積もりとリードタイムを求めるのご確認
10 mg $550 見積もりとリードタイムを求めるのご確認
25 mg $1220 見積もりとリードタイムを求めるのご確認
50 mg $1980 見積もりとリードタイムを求めるのご確認

* アイテムを追加する前、数量をご選択ください

This product is a controlled substance and not for sale in your territory.

Other 在庫あり Forms of Mibefradil:

Other Forms of Mibefradil:

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製品説明

Mibefradil (Ro 40-5967) is a calcium channel blocker with moderate selectivity for T-type Ca2+ channels displaying IC50s of 2.7 μM and 18.6 μM for T-type and L-type currents, respectively[1].

IC50 & Target

L-type calcium channel

 

T-type calcium channel

 

Cellular Effect
Cell Line Type Value Description References
A2780 IC50
24.23 3
Compound: Mibefradil
Cytotoxicity against human A2780 cells after 48 hrs by MTT assay
Cytotoxicity against human A2780 cells after 48 hrs by MTT assay
[PMID: 24220170]
A2780 IC50
24.23 3
Compound: Mibefradil
Cytotoxicity against human A2780 cells after 48 hrs by MTT assay
Cytotoxicity against human A2780 cells after 48 hrs by MTT assay
[PMID: 24220170]
A2780 IC50
24.23 3
Compound: Mibefradil
Cytotoxicity against human A2780 cells after 48 hrs by MTT assay
Cytotoxicity against human A2780 cells after 48 hrs by MTT assay
[PMID: 24220170]
A2780/Taxol IC50
35.26 3
Compound: Mibefradil
Cytotoxicity against human paclitaxel-resistant A2780T cells after 48 hrs by MTT assay
Cytotoxicity against human paclitaxel-resistant A2780T cells after 48 hrs by MTT assay
[PMID: 24220170]
A2780/Taxol IC50
35.26 3
Compound: Mibefradil
Cytotoxicity against human paclitaxel-resistant A2780T cells after 48 hrs by MTT assay
Cytotoxicity against human paclitaxel-resistant A2780T cells after 48 hrs by MTT assay
[PMID: 24220170]
A2780/Taxol IC50
35.26 3
Compound: Mibefradil
Cytotoxicity against human paclitaxel-resistant A2780T cells after 48 hrs by MTT assay
Cytotoxicity against human paclitaxel-resistant A2780T cells after 48 hrs by MTT assay
[PMID: 24220170]
A549 IC50
24.8 3
Compound: Mibefradil
Cytotoxicity against human A549 cells after 48 hrs by MTT assay
Cytotoxicity against human A549 cells after 48 hrs by MTT assay
[PMID: 24529871]
A549 IC50
24.8 3
Compound: Mibefradil
Cytotoxicity against human A549 cells after 48 hrs by MTT assay
Cytotoxicity against human A549 cells after 48 hrs by MTT assay
[PMID: 24529871]
A549 IC50
24.9 3
Compound: Mibefradil
Cytotoxicity against human A549 cells assessed as reduction in cell viability after 48 hrs by MTT assay
Cytotoxicity against human A549 cells assessed as reduction in cell viability after 48 hrs by MTT assay
[PMID: 32327350]
A549 IC50
24.9 3
Compound: Mibefradil
Cytotoxicity against human A549 cells assessed as reduction in cell viability after 48 hrs by MTT assay
Cytotoxicity against human A549 cells assessed as reduction in cell viability after 48 hrs by MTT assay
[PMID: 32327350]
A549 IC50
31.4 3
Compound: Mibefradil
Cytotoxicity against human A549 cells assessed as reduction in cell viability by MTT assay
Cytotoxicity against human A549 cells assessed as reduction in cell viability by MTT assay
[PMID: 26739776]
A549 IC50
31.4 3
Compound: Mibefradil
Cytotoxicity against human A549 cells assessed as reduction in cell viability by MTT assay
Cytotoxicity against human A549 cells assessed as reduction in cell viability by MTT assay
[PMID: 26739776]
CHO IC50
0.51 3
Compound: mibefradil
Inhibition of Cav1.2 current measured using QPatch automatic path clamp system in CHO cells expressing Cav1.2, beta-2 and alpha-2/delta-1 subunits
Inhibition of Cav1.2 current measured using QPatch automatic path clamp system in CHO cells expressing Cav1.2, beta-2 and alpha-2/delta-1 subunits
[PMID: 23812503]
Hepatocyte IC50
0.873 1
Compound: Mibefradil
Antimicrobial activity against Plasmodium yoelii 265 liver infected in mammalian hepatocytes after 48 hrs
Antimicrobial activity against Plasmodium yoelii 265 liver infected in mammalian hepatocytes after 48 hrs
[PMID: 18212104]
CHO IC50
3.3 3
Compound: Mibefradil
Inhibition of human ERG expressed in CHO cells by IONWORKS assay
Inhibition of human ERG expressed in CHO cells by IONWORKS assay
[PMID: 23200256]
HEK293 IC50
0.13 3
Compound: 1, Mibefradil
Antagonist activity at human alpha1H T-type calcium channel expressed in HEK293 cells by patch clamp technique
Antagonist activity at human alpha1H T-type calcium channel expressed in HEK293 cells by patch clamp technique
[PMID: 18160281]
CHO IC50
0.51 3
Compound: mibefradil
Inhibition of Cav1.2 current measured using QPatch automatic path clamp system in CHO cells expressing Cav1.2, beta-2 and alpha-2/delta-1 subunits
Inhibition of Cav1.2 current measured using QPatch automatic path clamp system in CHO cells expressing Cav1.2, beta-2 and alpha-2/delta-1 subunits
[PMID: 23812503]
HEK293 IC50
0.2 3
Compound: 1
Inhibition of human Cav3.1 alpha1G expressed in HEK293 cells assessed as inhibition of calcium influx by FLIPR assay
Inhibition of human Cav3.1 alpha1G expressed in HEK293 cells assessed as inhibition of calcium influx by FLIPR assay
[PMID: 21875808]
HEK293 IC50
0.56 3
Compound: Mibefradil
Inhibition of T-type CaV3.1 channel (unknown origin) expressed in HEK293 cells assessed as inhibition of calcium current by whole cell patch-clamp method
Inhibition of T-type CaV3.1 channel (unknown origin) expressed in HEK293 cells assessed as inhibition of calcium current by whole cell patch-clamp method
[PMID: 24529871]
CHO IC50
3.3 3
Compound: Mibefradil
Inhibition of human ERG expressed in CHO cells by IONWORKS assay
Inhibition of human ERG expressed in CHO cells by IONWORKS assay
[PMID: 23200256]
HEK293 IC50
1.34 3
Compound: Mibefradil
Ability to block calcium channel T type 3.1v expressed in HEK293 cells by whole cell patch clamp method
Ability to block calcium channel T type 3.1v expressed in HEK293 cells by whole cell patch clamp method
[PMID: 16876404]
HEK293 IC50
0.56 3
Compound: Mibefradil
Inhibition of t-type Cav3.1 channel (unknown origin) expressed in HEK293 cells assessed as inhibition of 50 ms depolarizing voltage step-induced current by whole cell patch-clamp method
Inhibition of t-type Cav3.1 channel (unknown origin) expressed in HEK293 cells assessed as inhibition of 50 ms depolarizing voltage step-induced current by whole cell patch-clamp method
[PMID: 24220170]
HEK293 IC50
0.13 3
Compound: 1, Mibefradil
Antagonist activity at human alpha1H T-type calcium channel expressed in HEK293 cells by patch clamp technique
Antagonist activity at human alpha1H T-type calcium channel expressed in HEK293 cells by patch clamp technique
[PMID: 18160281]
HEK293 IC50
0.83 3
Compound: Mibefradil
Inhibition of alpha-1G calcium channel in human HEK293 cells by whole-cell patch-clamp method
Inhibition of alpha-1G calcium channel in human HEK293 cells by whole-cell patch-clamp method
[PMID: 23395659]
HEK293 IC50
0.83 3
Compound: Mibefradil
Inhibition of T-type CaV3.1 channel expressed in HEK293 cells assessed as inhibition of calcium current by automated patch-clamp assay
Inhibition of T-type CaV3.1 channel expressed in HEK293 cells assessed as inhibition of calcium current by automated patch-clamp assay
[PMID: 20621730]
HEK293 IC50
1.34 3
Compound: mibefradil
Antagonist activity at T type calcium channel alpha1G expressed in HEK293 cells assessed as inhibition of peak currents by whole-cell patch-clamp method
Antagonist activity at T type calcium channel alpha1G expressed in HEK293 cells assessed as inhibition of peak currents by whole-cell patch-clamp method
[PMID: 18625556]
HEK293 IC50
0.84 3
Compound: mibefradil
Inhibition of alpha-1G T-type calcium channel expressed in HEK293 cells by electrophysiological method
Inhibition of alpha-1G T-type calcium channel expressed in HEK293 cells by electrophysiological method
[PMID: 17074493]
HEK293 IC50
0.84 3
Compound: Midefradil
Concentration of the compounds required for inhibition of HEK293 cells (alpha1G T-type)
Concentration of the compounds required for inhibition of HEK293 cells (alpha1G T-type)
[PMID: 15177437]
HEK293 IC50
0.86 3
Compound: Mibefradil
Inhibition of T-type CaV3.1 channel expressed in HEK293 cells assessed as inhibition of calcium current by manual patch-clamp assay
Inhibition of T-type CaV3.1 channel expressed in HEK293 cells assessed as inhibition of calcium current by manual patch-clamp assay
[PMID: 20621730]
HEK293 IC50
0.83 3
Compound: Mibefradil
Inhibition of alpha-1G calcium channel in human HEK293 cells by whole-cell patch-clamp method
Inhibition of alpha-1G calcium channel in human HEK293 cells by whole-cell patch-clamp method
[PMID: 23395659]
HEK293 IC50
0.84 3
Compound: mibefradil
Inhibition of alpha-1G T-type calcium channel expressed in HEK293 cells by electrophysiological method
Inhibition of alpha-1G T-type calcium channel expressed in HEK293 cells by electrophysiological method
[PMID: 17074493]
HEK293 IC50
1 3
Compound: Mibefradil
Inhibition of human T-type calcium channel Cav3.2 expressed in T-Rex293 cells by whole cell patch clamp assay
Inhibition of human T-type calcium channel Cav3.2 expressed in T-Rex293 cells by whole cell patch clamp assay
[PMID: 23200256]
HEK293 IC50
1.3 3
Compound: I, Posicor
Inhibition of human ERG expressed in HEK cells by patch clamp assay
Inhibition of human ERG expressed in HEK cells by patch clamp assay
[PMID: 26231163]
HEK293 IC50
0.2 3
Compound: 1
Inhibition of human Cav3.1 alpha1G expressed in HEK293 cells assessed as inhibition of calcium influx by FLIPR assay
Inhibition of human Cav3.1 alpha1G expressed in HEK293 cells assessed as inhibition of calcium influx by FLIPR assay
[PMID: 21875808]
HEK293 IC50
1.3 3
Compound: I, Posicor
Inhibition of human ERG expressed in HEK cells by patch clamp assay
Inhibition of human ERG expressed in HEK cells by patch clamp assay
[PMID: 26231163]
HEK293 IC50
1.34 3
Compound: Mibefradil
Inhibition of T-type alpha1G channel expressed in HEK293 cells by whole-cell patch-clamp method
Inhibition of T-type alpha1G channel expressed in HEK293 cells by whole-cell patch-clamp method
[PMID: 20659804]
HEK293 IC50
1.34 3
Compound: Mibefradil
Inhibition of T-type calcium channel alpha1G expressed in human HEK293 cells assessed as inhibition of peak currents by whole-cell patch-clamp method
Inhibition of T-type calcium channel alpha1G expressed in human HEK293 cells assessed as inhibition of peak currents by whole-cell patch-clamp method
[PMID: 20382529]
HEK293 IC50
1 3
Compound: Mibefradil
Inhibition of human T-type calcium channel Cav3.2 expressed in T-Rex293 cells by whole cell patch clamp assay
Inhibition of human T-type calcium channel Cav3.2 expressed in T-Rex293 cells by whole cell patch clamp assay
[PMID: 23200256]
A549 IC50
24.8 3
Compound: Mibefradil
Cytotoxicity against human A549 cells after 48 hrs by MTT assay
Cytotoxicity against human A549 cells after 48 hrs by MTT assay
[PMID: 24529871]
HEK293 IC50
1.34 3
Compound: mibefradil
Antagonist activity at T type calcium channel alpha1G expressed in HEK293 cells assessed as inhibition of peak currents by whole-cell patch-clamp method
Antagonist activity at T type calcium channel alpha1G expressed in HEK293 cells assessed as inhibition of peak currents by whole-cell patch-clamp method
[PMID: 18625556]
A549 IC50
24.9 3
Compound: Mibefradil
Cytotoxicity against human A549 cells assessed as reduction in cell viability after 48 hrs by MTT assay
Cytotoxicity against human A549 cells assessed as reduction in cell viability after 48 hrs by MTT assay
[PMID: 32327350]
HEK293 IC50
1.34 3
Compound: Mibefradil
Inhibition of T type calcium channel subunit alpha-1G expressed in HEK293 cells assessed as effect on T-type calcium currents by patch clamp method
Inhibition of T type calcium channel subunit alpha-1G expressed in HEK293 cells assessed as effect on T-type calcium currents by patch clamp method
[PMID: 17150365]
HEK293 IC50
1.34 3
Compound: mibefradil
Inhibition of T-type calcium channel Cav3.1 alpha-1G subunit expressed in HEK293 cells assessed as calcium current by patch-clamp assay
Inhibition of T-type calcium channel Cav3.1 alpha-1G subunit expressed in HEK293 cells assessed as calcium current by patch-clamp assay
[PMID: 17869104]
HEK293 IC50
1.34 3
Compound: Mibefradil
Inhibition of T-type [Ca2+] channel (alpha1G) expressed in HEK293 cells
Inhibition of T-type [Ca2+] channel (alpha1G) expressed in HEK293 cells
[PMID: 15603940]
A549 IC50
31.4 3
Compound: Mibefradil
Cytotoxicity against human A549 cells assessed as reduction in cell viability by MTT assay
Cytotoxicity against human A549 cells assessed as reduction in cell viability by MTT assay
[PMID: 26739776]
HEK293 IC50
1.34 3
Compound: Mibefradil
Inhibition of T-type alpha1G calcium channel expressed in HEK293 cells assessed as Kcl-induced depolarization
Inhibition of T-type alpha1G calcium channel expressed in HEK293 cells assessed as Kcl-induced depolarization
[PMID: 21126876]
HEK293 IC50
1.34 3
Compound: Mibefradil
Inhibition of T type calcium channel subunit alpha-1G expressed in HEK293 cells assessed as effect on T-type calcium currents by patch clamp method
Inhibition of T type calcium channel subunit alpha-1G expressed in HEK293 cells assessed as effect on T-type calcium currents by patch clamp method
[PMID: 17150365]
CHO IC50
0.51 3
Compound: mibefradil
Inhibition of Cav1.2 current measured using QPatch automatic path clamp system in CHO cells expressing Cav1.2, beta-2 and alpha-2/delta-1 subunits
Inhibition of Cav1.2 current measured using QPatch automatic path clamp system in CHO cells expressing Cav1.2, beta-2 and alpha-2/delta-1 subunits
[PMID: 23812503]
HEK293 IC50
1.34 3
Compound: Mibefradil
Inhibition of T-type alpha1G channel expressed in HEK293 cells by whole-cell patch-clamp method
Inhibition of T-type alpha1G channel expressed in HEK293 cells by whole-cell patch-clamp method
[PMID: 20659804]
CHO IC50
3.3 3
Compound: Mibefradil
Inhibition of human ERG expressed in CHO cells by IONWORKS assay
Inhibition of human ERG expressed in CHO cells by IONWORKS assay
[PMID: 23200256]
HEK293 IC50
1.34 3
Compound: mibefradil
Inhibition of T-type calcium channel Cav3.1 expressed in HEK293 cells co-expressing alpha1G subunit and Kir2.1 potassium channel by patch-clamp assay
Inhibition of T-type calcium channel Cav3.1 expressed in HEK293 cells co-expressing alpha1G subunit and Kir2.1 potassium channel by patch-clamp assay
[PMID: 17092715]
HEK293 IC50
1.34 3
Compound: mibefradil
Inhibition of T-type calcium channel Cav3.1 expressed in HEK293 cells co-expressing alpha1G subunit by whole-cell patch clamp method
Inhibition of T-type calcium channel Cav3.1 expressed in HEK293 cells co-expressing alpha1G subunit by whole-cell patch clamp method
[PMID: 17064894]
COS-7 IC50
1430 1
Compound: 18 (Mibefradil)
K+ channel blocking activity in COS-7 African green monkey kidney derived cells expressing HERG Kv11.1
K+ channel blocking activity in COS-7 African green monkey kidney derived cells expressing HERG Kv11.1
[PMID: 12190308]
HEK293 IC50
1.34 3
Compound: Mibefradil
Inhibition of T-type calcium channel alpha1G expressed in human HEK293 cells assessed as inhibition of peak currents by whole-cell patch-clamp method
Inhibition of T-type calcium channel alpha1G expressed in human HEK293 cells assessed as inhibition of peak currents by whole-cell patch-clamp method
[PMID: 20382529]
HEK293 IC50
1.34 3
Compound: mibefradil
Inhibition of T-type calcium channel Cav3.1 alpha-1G subunit expressed in HEK293 cells assessed as calcium current by patch-clamp assay
Inhibition of T-type calcium channel Cav3.1 alpha-1G subunit expressed in HEK293 cells assessed as calcium current by patch-clamp assay
[PMID: 17869104]
HEK293 IC50
1.34 3
Compound: Mibefradil
Ability to block calcium channel T type 3.1v expressed in HEK293 cells by whole cell patch clamp method
Ability to block calcium channel T type 3.1v expressed in HEK293 cells by whole cell patch clamp method
[PMID: 16876404]
HEK293 IC50
181 1
Compound: I, Posicor
Inhibition of recombinant Cav3.2 channel (unknown origin) expressed in HEK293 cells assessed as effect on calcium flux incubated for 3 mins by FLIPR assay
Inhibition of recombinant Cav3.2 channel (unknown origin) expressed in HEK293 cells assessed as effect on calcium flux incubated for 3 mins by FLIPR assay
[PMID: 26231163]
Caco-2 IC50
1.2 3
Compound: Mibefradil
TP_TRANSPORTER: inhibition of Digoxin transepithelial transport (basal to apical) (Digoxin: 5 uM) in Caco-2 cells
TP_TRANSPORTER: inhibition of Digoxin transepithelial transport (basal to apical) (Digoxin: 5 uM) in Caco-2 cells
[PMID: 11961113]
HEK293 IC50
1.34 3
Compound: mibefradil
Inhibition of T-type calcium channel Cav3.1 expressed in HEK293 cells co-expressing alpha1G subunit and Kir2.1 potassium channel by patch-clamp assay
Inhibition of T-type calcium channel Cav3.1 expressed in HEK293 cells co-expressing alpha1G subunit and Kir2.1 potassium channel by patch-clamp assay
[PMID: 17092715]
HEK293 IC50
1.34 3
Compound: mibefradil
Inhibition of T-type calcium channel Cav3.1 expressed in HEK293 cells co-expressing alpha1G subunit by whole-cell patch clamp method
Inhibition of T-type calcium channel Cav3.1 expressed in HEK293 cells co-expressing alpha1G subunit by whole-cell patch clamp method
[PMID: 17064894]
HEK293 IC50
202 1
Compound: I, Posicor
Inhibition of recombinant Cav1.2 channel (unknown origin) expressed in HEK293 cells assessed as effect on calcium flux incubated for 3 mins by FLIPR assay
Inhibition of recombinant Cav1.2 channel (unknown origin) expressed in HEK293 cells assessed as effect on calcium flux incubated for 3 mins by FLIPR assay
[PMID: 26231163]
Caco-2 IC50
1.6 3
Compound: Mibefradil
TP_TRANSPORTER: inhibition of Digoxin transepithelial transport (basal to apical) (Digoxin: 5 uM) in Caco-2 cells
TP_TRANSPORTER: inhibition of Digoxin transepithelial transport (basal to apical) (Digoxin: 5 uM) in Caco-2 cells
[PMID: 10901697]
HEK293 IC50
0.56 3
Compound: Mibefradil
Inhibition of t-type Cav3.1 channel (unknown origin) expressed in HEK293 cells assessed as inhibition of 50 ms depolarizing voltage step-induced current by whole cell patch-clamp method
Inhibition of t-type Cav3.1 channel (unknown origin) expressed in HEK293 cells assessed as inhibition of 50 ms depolarizing voltage step-induced current by whole cell patch-clamp method
[PMID: 24220170]
HeLa IC50
4.32 3
Compound: Mibefradil
Inhibition of Ebolavirus glycoprotein/matrix protein VP40 entry in human HeLa cells after 4.5 hrs beta-lactamase reporter assay
Inhibition of Ebolavirus glycoprotein/matrix protein VP40 entry in human HeLa cells after 4.5 hrs beta-lactamase reporter assay
[PMID: 29624387]
HEK293 IC50
0.56 3
Compound: Mibefradil
Inhibition of T-type CaV3.1 channel (unknown origin) expressed in HEK293 cells assessed as inhibition of calcium current by whole cell patch-clamp method
Inhibition of T-type CaV3.1 channel (unknown origin) expressed in HEK293 cells assessed as inhibition of calcium current by whole cell patch-clamp method
[PMID: 24529871]
Hepatocyte IC50
0.873 1
Compound: Mibefradil
Antimicrobial activity against Plasmodium yoelii 265 liver infected in mammalian hepatocytes after 48 hrs
Antimicrobial activity against Plasmodium yoelii 265 liver infected in mammalian hepatocytes after 48 hrs
[PMID: 18212104]
HEK293 IC50
0.83 3
Compound: Mibefradil
Inhibition of T-type CaV3.1 channel expressed in HEK293 cells assessed as inhibition of calcium current by automated patch-clamp assay
Inhibition of T-type CaV3.1 channel expressed in HEK293 cells assessed as inhibition of calcium current by automated patch-clamp assay
[PMID: 20621730]
LLC-PK1 IC50
1.8 3
Compound: Mibefradil
Inhibition of P-glycoprotein, human L-MDR1 expressed in LLC-PK1 epithelial cells using calcein-AM polarisation assay
Inhibition of P-glycoprotein, human L-MDR1 expressed in LLC-PK1 epithelial cells using calcein-AM polarisation assay
[PMID: 12699389]
HEK293 IC50
0.13 3
Compound: 1, Mibefradil
Antagonist activity at human alpha1H T-type calcium channel expressed in HEK293 cells by patch clamp technique
Antagonist activity at human alpha1H T-type calcium channel expressed in HEK293 cells by patch clamp technique
[PMID: 18160281]
HEK293 IC50
0.86 3
Compound: Mibefradil
Inhibition of T-type CaV3.1 channel expressed in HEK293 cells assessed as inhibition of calcium current by manual patch-clamp assay
Inhibition of T-type CaV3.1 channel expressed in HEK293 cells assessed as inhibition of calcium current by manual patch-clamp assay
[PMID: 20621730]
LLC-PK1 IC50
10 3
Compound: Mibefradil
Inhibition of P-glycoprotein, mouse L-mdr1b expressed in LLC-PK1 epithelial cells using calcein-AM polarisation assay
Inhibition of P-glycoprotein, mouse L-mdr1b expressed in LLC-PK1 epithelial cells using calcein-AM polarisation assay
[PMID: 12699389]
HEK293 IC50
0.2 3
Compound: 1
Inhibition of human Cav3.1 alpha1G expressed in HEK293 cells assessed as inhibition of calcium influx by FLIPR assay
Inhibition of human Cav3.1 alpha1G expressed in HEK293 cells assessed as inhibition of calcium influx by FLIPR assay
[PMID: 21875808]
HeLa IC50
4.32 3
Compound: Mibefradil
Inhibition of Ebolavirus glycoprotein/matrix protein VP40 entry in human HeLa cells after 4.5 hrs beta-lactamase reporter assay
Inhibition of Ebolavirus glycoprotein/matrix protein VP40 entry in human HeLa cells after 4.5 hrs beta-lactamase reporter assay
[PMID: 29624387]
LLC-PK1 IC50
7.4 3
Compound: Mibefradil
Inhibition of P-glycoprotein, mouse L-mdr1a expressed in LLC-PK1 epithelial cells using calcein-AM polarisation assay
Inhibition of P-glycoprotein, mouse L-mdr1a expressed in LLC-PK1 epithelial cells using calcein-AM polarisation assay
[PMID: 12699389]
HEK293 IC50
0.56 3
Compound: Mibefradil
Inhibition of t-type Cav3.1 channel (unknown origin) expressed in HEK293 cells assessed as inhibition of 50 ms depolarizing voltage step-induced current by whole cell patch-clamp method
Inhibition of t-type Cav3.1 channel (unknown origin) expressed in HEK293 cells assessed as inhibition of 50 ms depolarizing voltage step-induced current by whole cell patch-clamp method
[PMID: 24220170]
MDA-MB-231 IC50
> 100 3
Compound: 8
Inhibition of Orai1-mediated store operated Ca2+ entry in human MDA-MB-231 cells assessed as reduction in BAPTA-induced Ca2+ depletion-stimulated SOCE activity preincubated for 15 mins followed by BAPTA addition in presence of extracellular Ca2+ by PBX-ba
Inhibition of Orai1-mediated store operated Ca2+ entry in human MDA-MB-231 cells assessed as reduction in BAPTA-induced Ca2+ depletion-stimulated SOCE activity preincubated for 15 mins followed by BAPTA addition in presence of extracellular Ca2+ by PBX-ba
[PMID: 27856238]
LLC-PK1 IC50
1.8 3
Compound: Mibefradil
Inhibition of P-glycoprotein, human L-MDR1 expressed in LLC-PK1 epithelial cells using calcein-AM polarisation assay
Inhibition of P-glycoprotein, human L-MDR1 expressed in LLC-PK1 epithelial cells using calcein-AM polarisation assay
[PMID: 12699389]
HEK293 IC50
0.56 3
Compound: Mibefradil
Inhibition of T-type CaV3.1 channel (unknown origin) expressed in HEK293 cells assessed as inhibition of calcium current by whole cell patch-clamp method
Inhibition of T-type CaV3.1 channel (unknown origin) expressed in HEK293 cells assessed as inhibition of calcium current by whole cell patch-clamp method
[PMID: 24529871]
MDA-MB-231 IC50
52.1 3
Compound: 8
Inhibition of Orai1-mediated store operated Ca2+ entry in human MDA-MB-231 cells assessed as reduction of SERCA inhibition-induced ER release preincubated for 15 mins followed by CPA addition by PBX-based FLIPR assay
Inhibition of Orai1-mediated store operated Ca2+ entry in human MDA-MB-231 cells assessed as reduction of SERCA inhibition-induced ER release preincubated for 15 mins followed by CPA addition by PBX-based FLIPR assay
[PMID: 27856238]
HEK293 IC50
0.83 3
Compound: Mibefradil
Inhibition of T-type CaV3.1 channel expressed in HEK293 cells assessed as inhibition of calcium current by automated patch-clamp assay
Inhibition of T-type CaV3.1 channel expressed in HEK293 cells assessed as inhibition of calcium current by automated patch-clamp assay
[PMID: 20621730]
LLC-PK1 IC50
7.4 3
Compound: Mibefradil
Inhibition of P-glycoprotein, mouse L-mdr1a expressed in LLC-PK1 epithelial cells using calcein-AM polarisation assay
Inhibition of P-glycoprotein, mouse L-mdr1a expressed in LLC-PK1 epithelial cells using calcein-AM polarisation assay
[PMID: 12699389]
MIA PaCa-2 IC50
18.4 3
Compound: Mibefradil
Cytotoxicity against human MIAPaCa2 cells after 48 hrs by MTT assay
Cytotoxicity against human MIAPaCa2 cells after 48 hrs by MTT assay
[PMID: 24529871]
HEK293 IC50
0.83 3
Compound: Mibefradil
Inhibition of alpha-1G calcium channel in human HEK293 cells by whole-cell patch-clamp method
Inhibition of alpha-1G calcium channel in human HEK293 cells by whole-cell patch-clamp method
[PMID: 23395659]
LLC-PK1 IC50
10 3
Compound: Mibefradil
Inhibition of P-glycoprotein, mouse L-mdr1b expressed in LLC-PK1 epithelial cells using calcein-AM polarisation assay
Inhibition of P-glycoprotein, mouse L-mdr1b expressed in LLC-PK1 epithelial cells using calcein-AM polarisation assay
[PMID: 12699389]
MDA-MB-231 IC50
>100 3
Compound: 8
Inhibition of Orai1-mediated store operated Ca2+ entry in human MDA-MB-231 cells assessed as reduction in BAPTA-induced Ca2+ depletion-stimulated SOCE activity preincubated for 15 mins followed by BAPTA addition in presence of extracellular Ca2+ by PBX-ba
Inhibition of Orai1-mediated store operated Ca2+ entry in human MDA-MB-231 cells assessed as reduction in BAPTA-induced Ca2+ depletion-stimulated SOCE activity preincubated for 15 mins followed by BAPTA addition in presence of extracellular Ca2+ by PBX-ba
[PMID: 27856238]
HEK293 IC50
0.84 3
Compound: Midefradil
Concentration of the compounds required for inhibition of HEK293 cells (alpha1G T-type)
Concentration of the compounds required for inhibition of HEK293 cells (alpha1G T-type)
[PMID: 15177437]
Oocyte IC50
108 3
Compound: Mibefradil
Inhibition of L-type calcium channel measured using 2-electrode voltage-clamp in Xenopus oocyte heterologically expressing alpha-1C subunit
Inhibition of L-type calcium channel measured using 2-electrode voltage-clamp in Xenopus oocyte heterologically expressing alpha-1C subunit
[PMID: 22761000]
HEK293 IC50
0.84 3
Compound: mibefradil
Inhibition of alpha-1G T-type calcium channel expressed in HEK293 cells by electrophysiological method
Inhibition of alpha-1G T-type calcium channel expressed in HEK293 cells by electrophysiological method
[PMID: 17074493]
Oocyte IC50
288 3
Compound: Mibefradil
Inhibition of L-type calcium channel measured using 2-electrode voltage-clamp in Xenopus oocyte heterologically expressing alpha-1C subunit
Inhibition of L-type calcium channel measured using 2-electrode voltage-clamp in Xenopus oocyte heterologically expressing alpha-1C subunit
[PMID: 22761000]
MDA-MB-231 IC50
52.1 3
Compound: 8
Inhibition of Orai1-mediated store operated Ca2+ entry in human MDA-MB-231 cells assessed as reduction of SERCA inhibition-induced ER release preincubated for 15 mins followed by CPA addition by PBX-based FLIPR assay
Inhibition of Orai1-mediated store operated Ca2+ entry in human MDA-MB-231 cells assessed as reduction of SERCA inhibition-induced ER release preincubated for 15 mins followed by CPA addition by PBX-based FLIPR assay
[PMID: 27856238]
HEK293 IC50
0.86 3
Compound: Mibefradil
Inhibition of T-type CaV3.1 channel expressed in HEK293 cells assessed as inhibition of calcium current by manual patch-clamp assay
Inhibition of T-type CaV3.1 channel expressed in HEK293 cells assessed as inhibition of calcium current by manual patch-clamp assay
[PMID: 20621730]
MIA PaCa-2 IC50
18.4 3
Compound: Mibefradil
Cytotoxicity against human MIAPaCa2 cells after 48 hrs by MTT assay
Cytotoxicity against human MIAPaCa2 cells after 48 hrs by MTT assay
[PMID: 24529871]
SK-OV-3 IC50
20.54 3
Compound: Mibefradil
Cytotoxicity against human SKOV3 cells after 48 hrs by MTT assay
Cytotoxicity against human SKOV3 cells after 48 hrs by MTT assay
[PMID: 24220170]
HEK293 IC50
1 3
Compound: Mibefradil
Inhibition of human T-type calcium channel Cav3.2 expressed in T-Rex293 cells by whole cell patch clamp assay
Inhibition of human T-type calcium channel Cav3.2 expressed in T-Rex293 cells by whole cell patch clamp assay
[PMID: 23200256]
HEK293 IC50
181 1
Compound: I, Posicor
Inhibition of recombinant Cav3.2 channel (unknown origin) expressed in HEK293 cells assessed as effect on calcium flux incubated for 3 mins by FLIPR assay
Inhibition of recombinant Cav3.2 channel (unknown origin) expressed in HEK293 cells assessed as effect on calcium flux incubated for 3 mins by FLIPR assay
[PMID: 26231163]
HEK293 IC50
202 1
Compound: I, Posicor
Inhibition of recombinant Cav1.2 channel (unknown origin) expressed in HEK293 cells assessed as effect on calcium flux incubated for 3 mins by FLIPR assay
Inhibition of recombinant Cav1.2 channel (unknown origin) expressed in HEK293 cells assessed as effect on calcium flux incubated for 3 mins by FLIPR assay
[PMID: 26231163]
HEK293 IC50
1.3 3
Compound: I, Posicor
Inhibition of human ERG expressed in HEK cells by patch clamp assay
Inhibition of human ERG expressed in HEK cells by patch clamp assay
[PMID: 26231163]
HEK293 IC50
1.34 3
Compound: Mibefradil
Inhibition of T-type [Ca2+] channel (alpha1G) expressed in HEK293 cells
Inhibition of T-type [Ca2+] channel (alpha1G) expressed in HEK293 cells
[PMID: 15603940]
Oocyte IC50
108 3
Compound: Mibefradil
Inhibition of L-type calcium channel measured using 2-electrode voltage-clamp in Xenopus oocyte heterologically expressing alpha-1C subunit
Inhibition of L-type calcium channel measured using 2-electrode voltage-clamp in Xenopus oocyte heterologically expressing alpha-1C subunit
[PMID: 22761000]
HEK293 IC50
1.34 3
Compound: Mibefradil
Ability to block calcium channel T type 3.1v expressed in HEK293 cells by whole cell patch clamp method
Ability to block calcium channel T type 3.1v expressed in HEK293 cells by whole cell patch clamp method
[PMID: 16876404]
Oocyte IC50
288 3
Compound: Mibefradil
Inhibition of L-type calcium channel measured using 2-electrode voltage-clamp in Xenopus oocyte heterologically expressing alpha-1C subunit
Inhibition of L-type calcium channel measured using 2-electrode voltage-clamp in Xenopus oocyte heterologically expressing alpha-1C subunit
[PMID: 22761000]
HEK293 IC50
1.34 3
Compound: Mibefradil
Inhibition of T type calcium channel subunit alpha-1G expressed in HEK293 cells assessed as effect on T-type calcium currents by patch clamp method
Inhibition of T type calcium channel subunit alpha-1G expressed in HEK293 cells assessed as effect on T-type calcium currents by patch clamp method
[PMID: 17150365]
HEK293 IC50
1.34 3
Compound: Mibefradil
Inhibition of T-type calcium channel alpha1G expressed in human HEK293 cells assessed as inhibition of peak currents by whole-cell patch-clamp method
Inhibition of T-type calcium channel alpha1G expressed in human HEK293 cells assessed as inhibition of peak currents by whole-cell patch-clamp method
[PMID: 20382529]
SK-OV-3 IC50
20.54 3
Compound: Mibefradil
Cytotoxicity against human SKOV3 cells after 48 hrs by MTT assay
Cytotoxicity against human SKOV3 cells after 48 hrs by MTT assay
[PMID: 24220170]
HEK293 IC50
1.34 3
Compound: Mibefradil
Inhibition of T-type alpha1G channel expressed in HEK293 cells by whole-cell patch-clamp method
Inhibition of T-type alpha1G channel expressed in HEK293 cells by whole-cell patch-clamp method
[PMID: 20659804]
HEK293 IC50
1.34 3
Compound: Mibefradil
Inhibition of T-type alpha1G calcium channel expressed in HEK293 cells assessed as Kcl-induced depolarization
Inhibition of T-type alpha1G calcium channel expressed in HEK293 cells assessed as Kcl-induced depolarization
[PMID: 21126876]
HEK293 IC50
1.34 3
Compound: mibefradil
Inhibition of T-type calcium channel Cav3.1 expressed in HEK293 cells co-expressing alpha1G subunit by whole-cell patch clamp method
Inhibition of T-type calcium channel Cav3.1 expressed in HEK293 cells co-expressing alpha1G subunit by whole-cell patch clamp method
[PMID: 17064894]
HEK293 IC50
1.34 3
Compound: mibefradil
Inhibition of T-type calcium channel Cav3.1 expressed in HEK293 cells co-expressing alpha1G subunit and Kir2.1 potassium channel by patch-clamp assay
Inhibition of T-type calcium channel Cav3.1 expressed in HEK293 cells co-expressing alpha1G subunit and Kir2.1 potassium channel by patch-clamp assay
[PMID: 17092715]
HEK293 IC50
1.34 3
Compound: mibefradil
Inhibition of T-type calcium channel Cav3.1 alpha-1G subunit expressed in HEK293 cells assessed as calcium current by patch-clamp assay
Inhibition of T-type calcium channel Cav3.1 alpha-1G subunit expressed in HEK293 cells assessed as calcium current by patch-clamp assay
[PMID: 17869104]
HEK293 IC50
1.34 3
Compound: mibefradil
Antagonist activity at T type calcium channel alpha1G expressed in HEK293 cells assessed as inhibition of peak currents by whole-cell patch-clamp method
Antagonist activity at T type calcium channel alpha1G expressed in HEK293 cells assessed as inhibition of peak currents by whole-cell patch-clamp method
[PMID: 18625556]
HEK293 IC50
181 1
Compound: I, Posicor
Inhibition of recombinant Cav3.2 channel (unknown origin) expressed in HEK293 cells assessed as effect on calcium flux incubated for 3 mins by FLIPR assay
Inhibition of recombinant Cav3.2 channel (unknown origin) expressed in HEK293 cells assessed as effect on calcium flux incubated for 3 mins by FLIPR assay
[PMID: 26231163]
HEK293 IC50
202 1
Compound: I, Posicor
Inhibition of recombinant Cav1.2 channel (unknown origin) expressed in HEK293 cells assessed as effect on calcium flux incubated for 3 mins by FLIPR assay
Inhibition of recombinant Cav1.2 channel (unknown origin) expressed in HEK293 cells assessed as effect on calcium flux incubated for 3 mins by FLIPR assay
[PMID: 26231163]
HeLa IC50
4.32 3
Compound: Mibefradil
Inhibition of Ebolavirus glycoprotein/matrix protein VP40 entry in human HeLa cells after 4.5 hrs beta-lactamase reporter assay
Inhibition of Ebolavirus glycoprotein/matrix protein VP40 entry in human HeLa cells after 4.5 hrs beta-lactamase reporter assay
[PMID: 29624387]
Hepatocyte IC50
0.873 1
Compound: Mibefradil
Antimicrobial activity against Plasmodium yoelii 265 liver infected in mammalian hepatocytes after 48 hrs
Antimicrobial activity against Plasmodium yoelii 265 liver infected in mammalian hepatocytes after 48 hrs
[PMID: 18212104]
LLC-PK1 IC50
1.8 3
Compound: Mibefradil
Inhibition of P-glycoprotein, human L-MDR1 expressed in LLC-PK1 epithelial cells using calcein-AM polarisation assay
Inhibition of P-glycoprotein, human L-MDR1 expressed in LLC-PK1 epithelial cells using calcein-AM polarisation assay
[PMID: 12699389]
LLC-PK1 IC50
1.8 3
Compound: Mibefradil
TP_TRANSPORTER: inhibition of Calcein-AM efflux in MDR1-expressing LLC-PK1 cells
TP_TRANSPORTER: inhibition of Calcein-AM efflux in MDR1-expressing LLC-PK1 cells
[PMID: 12699389]
LLC-PK1 IC50
10 3
Compound: Mibefradil
Inhibition of P-glycoprotein, mouse L-mdr1b expressed in LLC-PK1 epithelial cells using calcein-AM polarisation assay
Inhibition of P-glycoprotein, mouse L-mdr1b expressed in LLC-PK1 epithelial cells using calcein-AM polarisation assay
[PMID: 12699389]
LLC-PK1 IC50
10 3
Compound: Mibefradil
TP_TRANSPORTER: inhibition of Calcein-AM efflux in Mdr1b-expressing LLC-PK1 cells
TP_TRANSPORTER: inhibition of Calcein-AM efflux in Mdr1b-expressing LLC-PK1 cells
[PMID: 12699389]
LLC-PK1 IC50
7.4 3
Compound: Mibefradil
Inhibition of P-glycoprotein, mouse L-mdr1a expressed in LLC-PK1 epithelial cells using calcein-AM polarisation assay
Inhibition of P-glycoprotein, mouse L-mdr1a expressed in LLC-PK1 epithelial cells using calcein-AM polarisation assay
[PMID: 12699389]
LLC-PK1 IC50
7.4 3
Compound: Mibefradil
TP_TRANSPORTER: inhibition of Calcein-AM efflux in Mdr1a-expressing LLC-PK1 cells
TP_TRANSPORTER: inhibition of Calcein-AM efflux in Mdr1a-expressing LLC-PK1 cells
[PMID: 12699389]
MDA-MB-231 IC50
52.1 3
Compound: 8
Inhibition of Orai1-mediated store operated Ca2+ entry in human MDA-MB-231 cells assessed as reduction of SERCA inhibition-induced ER release preincubated for 15 mins followed by CPA addition by PBX-based FLIPR assay
Inhibition of Orai1-mediated store operated Ca2+ entry in human MDA-MB-231 cells assessed as reduction of SERCA inhibition-induced ER release preincubated for 15 mins followed by CPA addition by PBX-based FLIPR assay
[PMID: 27856238]
MDA-MB-231 IC50
> 100 3
Compound: 8
Inhibition of Orai1-mediated store operated Ca2+ entry in human MDA-MB-231 cells assessed as reduction in BAPTA-induced Ca2+ depletion-stimulated SOCE activity preincubated for 15 mins followed by BAPTA addition in presence of extracellular Ca2+ by PBX-ba
Inhibition of Orai1-mediated store operated Ca2+ entry in human MDA-MB-231 cells assessed as reduction in BAPTA-induced Ca2+ depletion-stimulated SOCE activity preincubated for 15 mins followed by BAPTA addition in presence of extracellular Ca2+ by PBX-ba
[PMID: 27856238]
MIA PaCa-2 IC50
18.4 3
Compound: Mibefradil
Cytotoxicity against human MIAPaCa2 cells after 48 hrs by MTT assay
Cytotoxicity against human MIAPaCa2 cells after 48 hrs by MTT assay
[PMID: 24529871]
Oocyte IC50
108 3
Compound: Mibefradil
Inhibition of L-type calcium channel measured using 2-electrode voltage-clamp in Xenopus oocyte heterologically expressing alpha-1C subunit
Inhibition of L-type calcium channel measured using 2-electrode voltage-clamp in Xenopus oocyte heterologically expressing alpha-1C subunit
[PMID: 22761000]
Oocyte IC50
288 3
Compound: Mibefradil
Inhibition of L-type calcium channel measured using 2-electrode voltage-clamp in Xenopus oocyte heterologically expressing alpha-1C subunit
Inhibition of L-type calcium channel measured using 2-electrode voltage-clamp in Xenopus oocyte heterologically expressing alpha-1C subunit
[PMID: 22761000]
SK-OV-3 IC50
20.54 3
Compound: Mibefradil
Cytotoxicity against human SKOV3 cells after 48 hrs by MTT assay
Cytotoxicity against human SKOV3 cells after 48 hrs by MTT assay
[PMID: 24220170]
体外実験

Mibefradil inhibits reversibly the T- and L-type currents with IC50 values of 2.7 and 18.6 μM, respectively. The inhibition of the L-type current is voltage-dependent, whereas that of the T-type current is not. Ro 40-5967 blocks T-type current already at a holding potential of -100 mV[1] At a higher concentration (20 μM), Mibefradil reduces the amplitude of excitatory junction potentials (by 37±10 %), slows the rate of repolarisation (by 44±16 %) and causes a significant membrane potential depolarisation (from 83±1 mV to 71±5 mV). At a higher Mibefradil concentration (20 μM) there is significant membrane potential depolarisation and a slowing of repolarisation. These actions of Mibefradil are consistent with K+ channel inhibition, which has been shown to occur in human myoblasts and other cells[2].

MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.

体内実験

The hearing thresholds of the 24-26 week old C57BL/6J mice differed following the 4-week treatment period. The hearing threshold at 24 kHz is significantly decreased in the Mibefradil-treated and benidipine-treated groups compared with the saline-treated group (P<0.05)[3]. Compared with the saline-treated group, rats receiving Mibefradil or Ethosuximide show significant lower CaV3.2 expression in the spinal cord and DRG[4].

MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.

臨床実験
分子量

495.63

分子式

C29H38FN3O3

CAS 番号
Appearance

Solid

Color

White to off-white

SMILES

O=C(O[C@@]1(CCN(CCCC2=NC3=CC=CC=C3N2)C)[C@@H](C(C)C)C4=C(C=C(F)C=C4)CC1)COC

輸送条件

Room temperature in continental US; may vary elsewhere.

保管条件

-20°C, sealed storage, away from moisture and light

*In solvent : -80°C, 6 months; -20°C, 1 month (sealed storage, away from moisture and light)

純度とドキュメンテーション
参考文献
動物実験
[3][4]

Mice[3]
A total of 30 male C57BL/6J mice (age, 6-8 weeks) are randomized into three groups for the detection of three calcium channel receptor subunits α1G, α1H and α1I, using reverse transcription-quantitative polymerase chain reaction (RT-qPCR). In addition, a further 30 C57BL/6J male mice (age, 24-26 weeks) are allocated at random into three treatment groups: Saline, Mibefradil and benidipine. Each group is subjected to auditory brainstem recording (ABR) and distortion product otoacoustic emission (DPOAE) tests following treatment. Mibefradil and benidipine are dissolved in physiological saline solution. A preliminary experiment led to the selection of dosages of 30 mg/kg/day Mibefradil and 10 mg/kg/day Benidipine. The drugs are administered to the mice by gavage for four consecutive weeks.
Rats[4]
Male Sprague-Dawley rats (200-250 g) are used for right L5/6 SNL to induce neuropathic pain. Intrathecal infusion of saline or TCC blockers [Mibefradil (0.7 μg/h) or Ethosuximide (60 μg/h)] is started after surgery for 7 days. Fluorescent immunohistochemistry and Western blotting are used to determine the expression pattern and protein level of CaV3.2. Hematoxylin-eosin and toluidine blue staining are used to evaluate the neurotoxicity of tested agents.

MedChemExpress (MCE) はこれらの方法の精度を確認していません。 こちらは参照専用です。

参考文献
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製品名:
Mibefradil
製品番号:
HY-15553
数量:
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