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Mibefradil dihydrochloride

Catalog No. T12032 CAS 116666-63-8

Synonyms: Ro 40-5967 (dihydrochloride)

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

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Mibefradil dihydrochloride Chemical Structure

Mibefradil dihydrochloride, CAS 116666-63-8

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1 mg	In stock	$ 40.00
5 mg	In stock	$ 92.00

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Purity: 99.72%

Purity: 99.45%

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Description	Mibefradil dihydrochloride (Ro 40-5967 (dihydrochloride)) is an blocker of calcium channel with moderate selectivity for T-type Ca2+ channels (T-type and L-type currents with IC50s of 2.7 μM and 18.6 μM, respectively).
Targets&IC50	Ca2+ channel, L-type:18.6 μM , Ca2+ channel, T-type:2.7 μM
In vitro	Mibefradil dihydrochloride inhibits reversibly the T- and L-type currents with IC50 values of 2.7 and 18.6 μM, respectively.[1].Mibefradil inhibited Orai1, Orai2, and Orai3 currents dose-dependently. The IC50 for Orai1, Orai2, and Orai3 channels was 52.6, 14.1, and 3.8 μM respectively. Outside-out patch demonstrated that perfusion of 10-μM mibefradil to the extracellular surface completely blocked Orai3 currents and single channel activity evoked by 2-APB. Intracellular application of mibefradil did not alter Orai3 channel activity. Mibefradil at higher concentrations (>50 μM) inhibited Ca2+ release but had no effect on cytosolic STIM1 translocation evoked by thapsigargin. Inhibition on Orai channels by mibefradil was structure-related, as other T-type Ca2+ channel blockers with different structures, such as ethosuximide and ML218, had no or minimal effects on Orai channels. Moreover, mibefradil inhibited cell proliferation, induced apoptosis, and arrested cell cycle progression[3].
In vivo	Compared with the saline-treated group, rats receiving Mibefradil or Ethosuximide show significant lower CaV3.2 expression in the spinal cord and DRG.
Cell Research	Human Orai1-3 cDNAs in tetracycline-regulated pcDNA4/TO vectors were transfected into HEK293 T-REx cells with stromal interaction molecule 1 (STIM1) stable expression. The Orai currents were recorded by whole-cell and excised-membrane patch clamp. Ca2+?influx or release was measured by Fura-PE3/AM. Cell growth and death were monitored by WST-1, LDH assays and flow cytometry[3].

Synonyms	Ro 40-5967 (dihydrochloride)
Molecular Weight	568.55
Formula	C29H40Cl2FN3O3
CAS No.	116666-63-8

Storage

Powder: -20°C for 3 years | In solvent: -80°C for 1 year

Solubility Information

H2O: 122 mg/mL (214.58mM)

References and Literature

1. Brain KL, 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. Yu YF, et al. Protection of the cochlear hair cells in adult C57BL/6J mice by T-type calcium channel blockers. Exp Ther Med. 2016 Mar;11(3):1039-1044. 3. Li P , Rubaiy H N , Gui‐Lan Chen, et al. Mibefradil, a T‐type Ca2+ channel blocker also blocks Orai channels by action at the extracellular surface[J]. British Journal of Pharmacology, 2019, 176. 4. Shiue SJ, et al. Chronic intrathecal infusion of T-type calcium channel blockers attenuates CaV3.2 upregulation in nerve-ligated rats. Acta Anaesthesiol Taiwan. 2016 Oct 17. pii: S1875-4597(16)30071-6.

Related compound libraries

This product is contained In the following compound libraries：

Drug Repurposing Compound Library Anti-Cancer Clinical Compound Library Anti-Cancer Drug Library Inhibitor Library Membrane Protein-targeted Compound Library Anti-Cardiovascular Disease Compound Library Bioactive Compound Library NO PAINS Compound Library Anti-Hypertension Compound Library Clinical Compound Library

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Ranolazine dihydrochloride Cav 3.2 inhibitor 4 Thapsigargin McN5691 Gallopamil hydrochloride CDN1163 Cromolyn sodium ZSET1446

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Keywords

Mibefradil dihydrochloride 116666-63-8 Membrane transporter/Ion channel Metabolism Calcium Channel inhibit Mibefradil Dihydrochloride Ro 40-5967 (dihydrochloride) Inhibitor Ca channels Ca2+ channels Mibefradil Ro 40-5967 inhibitor

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