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Mibefradil dihydrochloride hydrate

Ro 40-5967 hydrate

A Blocker of T-type CaV, Orai1-3, and KV10.1 Channels

Cat #: M-150
Alternative Name Ro 40-5967 hydrate
Lyophilized Powder yes
  • Bioassay Tested
    • Source Synthetic
    MW: 568.55
    Purity: >98%
    Form Lyophilized powder.
    Effective concentration 0.01-50 µM.
    Structure
    Chemical name (1S,2S)-2-[2[[3-(2-Benzimidazolyl)propyl]methylamino]ethyl]-6-fluoro-1,2,3,4-tetrahydro-1-isopropyl-2-naphthyl methoxyacetate dihydrochloride hydrate.
    Molecular formula C29H40Cl2FN3O3.
    CAS No.: 116666-63-8
    Activity Mibefradil blocks T-type Ca2+ channels with an IC50 of ~1 µM. Orai1-3 and most potent on Orai32. It also modulates the gating properties of KV10.1 channel3.
    References-Activity
    1. Martin, R.L. et al. (2000) J. Pharmacol. Exp. Ther. 295, 302.
    2. Li, P. et al. (2019) Br. J. Pharmacol. 176, 3845.
    3. Gomez-Lagunas, F. et al. (2017) J. Cell. Physiol. 232, 2019.
    Shipping and storage Shipped at room temperature. Product as supplied can be stored intact at room temperature for several weeks. For longer periods, it should be stored at -20°C.
    Solubility 35 mM in water, 100 mM in DMSO. Centrifuge all product preparations before use (10 000 x g for 1 min).
    Storage of solutions Up to four weeks at 4°C or three months at -20°C.
    Our bioassay
    • Alomone Labs Mibefradil dihydrochloride hydrate inhibits T-type CaV channels heterologously expressed in Xenopus oocytes.
      Alomone Labs Mibefradil dihydrochloride hydrate inhibits T-type CaV channels heterologously expressed in Xenopus oocytes.
      A. Time course of CaV3.2 peak current amplitude, elicited by 100 ms voltage step from holding potential of -100 mV to -20 mV, delivered every 10 seconds. Application of 10 µM Mibefradil dihydrochloride hydrate (#M-150) inhibits CaV3.2current in a reversible manner (indicated by the horizontal bar).
      B. Representative current traces before and during application of 10 µM Mibefradil dihydrochloride hydrate as indicated.
    References - Scientific background
    1. Martin, R.L. et al. (2000) J. Pharmacol. Exp. Ther. 295, 302.
    2. Brogden, R.N. et al. (1997) Drugs 54, 774.
    3. Major, T.C. et al. (2008) J. Pharmacol. Exp. Ther. 325, 723.
    4. Keir, S.T. et al. (2013) J. Neurooncol. 111, 97.
    5. Sheehan, J.P. et al. (2013) J. Neurosurg. 118, 830.
    6. Gomez-Lagunas, F. et al. (2017) J. Cell. Physiol. 232, 2019.
    7. Li, P. et al. (2019) Br. J. Pharmacol. 176, 3845.
    Scientific background

    Mibefradil dihydrochloride hydrate, a potent T-type calcium antagonist, belongs to a new class of Ca2+ antagonists, the tetralol derivatives. It selectively blocks T-type Ca2+ channels in contrast to other Ca2+ antagonists which block only L-type channels1. Mibefradil also modulates the gating properties of KV10.1 channel6. It also blocks Orai1-3 channels with the following IC50: 52.6, 14.1, and 3.8 μM respectively, in whole-cell and excised-membrane patch clamp7.

    Mibefradil dihydrochloride hydrate has 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 respectively2. Mibefradil relaxes coronary arteries without suppressing myocardial contractility and causes a dose-related decrease in heart rate. Mibefradil demonstrated end organ protection such as preventing neointima formation after vascular injury and myocardial hypertrophy3. In addition, it has been shown that it inhibits human cancer cell proliferation in vitro with several cell lines including glioblastoma (GB), by inhibiting passage beyond the G1/S interphase4,5.

    Target CaV3, Orai1-3, KV10.1 channels
    Lyophilized Powder
    Last update: 06/11/2022

    Mibefradil dihydrochloride hydrate (#M-150) is a highly pure, synthetic, and biologically active compound.

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    For research purposes only, not for human use
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