Mibefradil dihydrochloride

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Cat.No. 2198 - Mibefradil dihydrochloride | C29H38FN3O3.2HCl | CAS No. 116666-63-8
Description: Ca2+ channel blocker (T-type)
Alternative Names: Ro 40-5967
Chemical Name: (1S,2S)-2-[2-[[3-(1H-Benzimidazol-2yl)propyl]methylamino]ethyl]-6-fluoro-1,2,3,4-tetrahydro-1-(1-methylethyl)-2-naphthalenyl methoxyacetoacetate dihydrochloride
Purity: ≥97% (HPLC)
Datasheet
Citations (7)
Literature

Biological Activity

Ca2+ channel blocker with moderate selectivity for T-type Ca2+ channels displaying IC50 values of 2.7 μM and 18.6 μM for T-type and L-type channels respectively. Antihypertensive agent.

Compound Libraries

Mibefradil dihydrochloride is also offered as part of the Tocriscreen Plus. Find out more about compound libraries available from Tocris.

Technical Data

M. Wt 568.56
Formula C29H38FN3O3.2HCl
Storage Store at -20°C
Purity ≥97% (HPLC)
CAS Number 116666-63-8
PubChem ID 60662
InChI Key MTJLQTFHJIHXIX-GDUXWEAWSA-N
Smiles Cl.Cl.COCC(=O)O[C@]1(CCN(C)CCCC2=NC3=C(N2)C=CC=C3)CCC2=C(C=CC(F)=C2)[C@@H]1C(C)C

The technical data provided above is for guidance only. For batch specific data refer to the Certificate of Analysis.

All Tocris products are intended for laboratory research use only.

Solubility Data

Solvent Max Conc. mg/mL Max Conc. mM
Solubility
DMSO 56.86 100
water 28.43 50

Preparing Stock Solutions

The following data is based on the product molecular weight 568.56. Batch specific molecular weights may vary from batch to batch due to solvent of hydration, which will affect the solvent volumes required to prepare stock solutions.

Select a batch to recalculate based on the batch molecular weight:
Concentration / Solvent Volume / Mass 1 mg 5 mg 10 mg
1 mM 1.76 mL 8.79 mL 17.59 mL
5 mM 0.35 mL 1.76 mL 3.52 mL
10 mM 0.18 mL 0.88 mL 1.76 mL
50 mM 0.04 mL 0.18 mL 0.35 mL

Molarity Calculator

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Product Datasheets

Certificate of Analysis / Product Datasheet
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Safety Datasheet

References

References are publications that support the products' biological activity.

Osterrieder and Holck (1989) In vitro pharmacologic profile of Ro 40-5967, a novel Ca2+ channel blocker with potent vasodilator but weak inotropic action. J.Cardiovasc.Pharmacol. 13 754 PMID: 2472524

Veniant et al (1991) Hemodynamic profile of Ro 40-5967 in conscious rats: comparison with diltiazem, verapamil, and amlodipine. J.Cardiovasc.Pharmacol. 18 S55 PMID: 1725005

Mehrke et al (1994) The Ca(++)-channel blocker Ro 40-5967 blocks differently T-type and L-type Ca++ channels. J.Pharmacol.Exp.Ther. 271 1483 PMID: 7996461


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View Related Products by Product Action

View all Voltage-gated Calcium Channel (CaV) Blockers

Keywords: Mibefradil dihydrochloride, supplier, Ca2+, channel, blockers, T-type, Calcium, CaV, Channels, L-Type, P-Type, R-Type, Q-Type, T-Type, N-Type, voltage-gated, voltage-dependent, Ro405967, Ro, 40-5967, Voltage-gated, Calcium, Channels, Tocris Bioscience

7 Citations for Mibefradil dihydrochloride

Citations are publications that use Tocris products. Selected citations for Mibefradil dihydrochloride include:

Weick and Demb (2011) Delayed-rectifier K channels contribute to contrast adaptation in mammalian retinal ganglion cells. Neuron 71 166 PMID: 21745646

Higley and Sabatini (2010) Competitive regulation of synaptic Ca2+ influx by D2 dopamine and A2A adenosine receptors. Nat Neurosci 13 958 PMID: 20601948

Grubb and Burrone (2010) Activity-dependent relocation of the axon initial segment fine-tunes neuronal excitability. Neurosci Lett 465 1070 PMID: 20543823

Weber (2017) Activation of odorant receptor in colorectal cancer cells leads to inhibition of cell proliferation and apoptosis. PLoS One 12 e0172491 PMID: 28273117

Prigge et al (2016) M1 ipRGCs Influence Visual Function through Retrograde Signaling in the Retina The Journal of Neuroscience 6 7184 PMID: 27383593

Wang et al (2015) Hydrogen sulfide-induced itch requires activation of Cav3.2 T-type calcium channel in mice. Nature 5 16768 PMID: 26602811

Stone et al (2013) Attenuation of autonomic reflexes by A803467 may not be solely caused by blockade of NaV 1.8 channels. Sci Rep 543 177 PMID: 23523647


Do you know of a great paper that uses Mibefradil dihydrochloride from Tocris? If so please let us know.

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Literature in this Area

Cardiovascular

Cardiovascular Research Product Guide

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Depression

Depression Poster

Major depressive disorder is characterized by depressed mood and a loss of interest and/or pleasure. Updated in 2015 this poster highlights presynaptic and postsynaptic targets for the potential treatment of major depressive disorder, as well as outlining the pharmacology of currently approved antidepressant drugs.

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