Date published: 2026-3-17

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Mibefradil dihydrochloride (CAS 116666-63-8)

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Alternate Names:
Ro 40-5967; Posicor
Application:
Mibefradil dihydrochloride is selectively blocks Ca2+ entry into cells by inhibiting T-type Ca2+ channels
CAS Number:
116666-63-8
Purity:
≥98%
Molecular Weight:
568.55
Molecular Formula:
C29H38FN3O32HCl
For Research Use Only. Not Intended for Diagnostic or Therapeutic Use.
* Refer to Certificate of Analysis for lot specific data.

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Mibefradil dihydrochloride is a nondihydropyridine antagonist and calcium channel protein inhibitor which selectively blocks Ca2+ entry into cells by inhibiting T-type (low-voltage activated) Ca2+ channels. In addition, it has been reported that mibefradil dihydrochloride can partially inhibit L-type (high-voltage activated) Ca2+ channels. Studies show that when this compound is combined with nisoldipine (sc-212396), an L-type Ca2+ antagonist, all calcium channels are completely blocked. Furthermore, in vitro studies indicate that mibefradil dihydrochloride protect CA1 neurons from delayed death after global ischemia in rats.


Mibefradil dihydrochloride (CAS 116666-63-8) References

  1. A post-marketing observational study to assess the safety of mibefradil in the community in England.  |  Riley, J., et al. 2002. Int J Clin Pharmacol Ther. 40: 241-8. PMID: 12078937
  2. Reversal of experimental neuropathic pain by T-type calcium channel blockers.  |  Dogrul, A., et al. 2003. Pain. 105: 159-68. PMID: 14499432
  3. The sources and sequestration of Ca(2+) contributing to neuroeffector Ca(2+) transients in the mouse vas deferens.  |  Brain, KL., et al. 2003. J Physiol. 553: 627-35. PMID: 14500773
  4. Metabolism of calcium antagonist Ro 40-5967: a case history of the use of diode-array u.v. spectroscopy and thermospray-mass spectrometry in the elucidation of a complex metabolic pathway.  |  Wiltshire, HR., et al. 1992. Xenobiotica. 22: 837-57. PMID: 1455903
  5. Induction of apoptosis by the calcium antagonist mibefradil correlates with depolarization of the membrane potential and decreased integrin expression in human lens epithelial cells.  |  Nebe, B., et al. 2004. Graefes Arch Clin Exp Ophthalmol. 242: 597-604. PMID: 15069564
  6. Hemodynamic profile of Ro 40-5967 in conscious rats: comparison with diltiazem, verapamil, and amlodipine.  |  Véniant, M., et al. 1991. J Cardiovasc Pharmacol. 18 Suppl 10: S55-8. PMID: 1725005
  7. In vitro pharmacologic profile of Ro 40-5967, a novel Ca2+ channel blocker with potent vasodilator but weak inotropic action.  |  Osterrieder, W. and Holck, M. 1989. J Cardiovasc Pharmacol. 13: 754-9. PMID: 2472524
  8. Activation of transient receptor potential ankyrin 1 induces CGRP release from spinal cord synaptosomes.  |  Quallo, T., et al. 2015. Pharmacol Res Perspect. 3: e00191. PMID: 27022465
  9. ZD7288 and mibefradil inhibit the myogenic heartbeat in Daphnia magna indicating its dependency on HCN and T-type calcium ion channels.  |  Pirtle, TJ., et al. 2018. Comp Biochem Physiol A Mol Integr Physiol. 222: 36-42. PMID: 29684576
  10. The Ca(++)-channel blocker Ro 40-5967 blocks differently T-type and L-type Ca++ channels.  |  Mehrke, G., et al. 1994. J Pharmacol Exp Ther. 271: 1483-8. PMID: 7996461
  11. Selective inhibition of T-type Ca2+ channels by Ro 40-5967.  |  Mishra, SK. and Hermsmeyer, K. 1994. Circ Res. 75: 144-8. PMID: 8013072
  12. Nonlinear pharmacokinetics of mibefradil in the dog.  |  Skerjanec, A., et al. 1996. J Pharm Sci. 85: 189-92. PMID: 8683447
  13. Pharmacologic and pharmacokinetic profile of mibefradil, a T- and L-type calcium channel antagonist.  |  Abernethy, DR. 1997. Am J Cardiol. 80: 4C-11C. PMID: 9286848
  14. Mibefradil, a T-channel-selective calcium antagonist: clinical trials in hypertension.  |  Oparil, S. 1998. Am J Hypertens. 11: 88S-94S. PMID: 9607372
  15. Inhibition of myogenic tone by mibefradil in rat cerebral arteries.  |  Lam, E., et al. 1998. Eur J Pharmacol. 358: 165-8. PMID: 9808266

Ordering Information

Product NameCatalog #UNITPriceQtyFAVORITES

Mibefradil dihydrochloride, 10 mg

sc-204083
10 mg
$213.00

Mibefradil dihydrochloride, 50 mg

sc-204083A
50 mg
$865.00