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Submit ReviewMibefradil dihydrochloride
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)
Biological Activity for Mibefradil dihydrochloride
Mibefradil dihydrochloride is a 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 for Mibefradil dihydrochloride
Mibefradil dihydrochloride is also offered as part of the Tocriscreen 2.0 Max. Find out more about compound libraries available from Tocris.
Technical Data for Mibefradil dihydrochloride
| 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 for Mibefradil dihydrochloride
| Solvent | Max Conc. mg/mL | Max Conc. mM | |
|---|---|---|---|
| Solubility | |||
| water | 28.43 | 50 | |
| DMSO | 56.86 | 100 |
Preparing Stock Solutions for Mibefradil dihydrochloride
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 for Mibefradil dihydrochloride
References for Mibefradil dihydrochloride
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
If you know of a relevant reference for Mibefradil dihydrochloride, please let us know.
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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
Cilz et al (2014) DArgic modulation of GABAergic transmission in the entorhinal cortex: concerted roles of α1 adrenoreceptors, inward rectifier K+, and T-type Ca2+ channels. Cereb Cortex 24 3195 PMID: 23843440
Wang et al (2015) Hydrogen sulfide-induced itch requires activation of Cav3.2 T-type calcium channel in mice. Nature 5 16768 PMID: 26602811
Prigge et al (2016) M1 ipRGCs Influence Visual Function through Retrograde Signaling in the Retina The Journal of Neuroscience 6 7184 PMID: 27383593
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
Weick and Demb (2011) Delayed-rectifier K channels contribute to contrast adaptation in mammalian retinal ganglion cells. Neuron 71 166 PMID: 21745646
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
Average Rating: 5 (Based on 1 Review.)
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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.
