Mibefradil dihydrochloride

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Cat.No. 2198 - Mibefradil dihydrochloride | C29H38FN3O3.2HCl | CAS No. 116666-63-8
Description: CaV3.x blocker
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 (9)
Reviews (1)
Literature (3)

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.

Tocris products are intended for laboratory research use only, unless stated otherwise.

Solubility Data

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

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 the degree of hydration, which will affect the solvent volumes required to prepare stock solutions.

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

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Product Datasheets

Certificate of Analysis / Product Datasheet
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References

References are publications that support the biological activity of the product.

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 amlod. 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 CaV3.x Channel (T-type) Blockers

Keywords: Mibefradil dihydrochloride, 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, Cav3.x, 2198, Tocris Bioscience

9 Citations for Mibefradil dihydrochloride

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

Bragança et al (2016) Ion Fluxes through KCa2 (SK) and Cav1 (L-type) Channels Contribute to Chronoselectivity of Adenosine A1 Receptor-Mediated Actions in Spontaneously Beating Rat Atria. Front Pharmacol 7 45 PMID: 27014060

Higley and Sabatini (2010) Competitive regulation of synaptic Ca2+ influx by D2 DA 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


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

Reviews for Mibefradil dihydrochloride

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Mibefradil dihydrochloride used on T type calcium channels.
By Anonymous on 02/13/2019
Species: Human

Mibefradil dihydrochloride used on T type calcium channels that aid in mediating calcium influx into cells after an action potential or depolarizing signal. The entry of calcium into various cells has many different physiological responses associated with it.

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Literature in this Area

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