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Mibefradil (dihydrochloride)

Mibefradil dihydrochloride (Ro 40-5967 dihydrochloride) is a calcium channel blocker with moderate selectivity for T-type Ca2+ channels (IC50s of 2.7 μM and 18.6 μM for T-type and L-type currents, respectively) [1].

Product Specifications

CAS Number

116666-63-8

Product Name Alternative

Ro 40-5967 (dihydrochloride)

UNSPSC

12352005

Hazard Statement

H302, H315, H319, H335

Target

Calcium Channel

Type

Reference compound

Related Pathways

Membrane Transporter/Ion Channel; Neuronal Signaling

Applications

COVID-19-immunoregulation

Field of Research

Cardiovascular Disease; Cancer

Assay Protocol

https://www.medchemexpress.com/Mibefradil-dihydrochloride.html

Purity

99.71

Solubility

DMSO : 50 mg/mL (ultrasonic) |H2O : 150 mg/mL (ultrasonic)

Smiles

O=C(O[C@@]1(CCN(CCCC2=NC3=CC=CC=C3N2)C)[C@@H](C(C)C)C4=C(C=C(F)C=C4)CC1)COC.[H]Cl.[H]Cl

Molecular Formula

C29H40Cl2FN3O3

Molecular Weight

568.55

Precautions

H302, H315, H319, H335

References & Citations

[1]Mehrke G, et al. The Ca (++) -channel blocker Ro 40-5967 blocks differently T-type and L-type Ca++ channels. J Pharmacol Exp Ther. 1994 Dec;271 (3) :1483-8.|[2]Brain KL, et al. The sources and sequestration of Ca (2+) contributing to neuroeffector Ca (2+) transients in the mouse vas deferens. J Physiol. 2003 Dec 1;553 (Pt 2) :627-35.|[3]Yu YF, et al. Protection of the cochlear hair cells in adult C57BL/6J mice by T-type calcium channel blockers. Exp Ther Med. 2016 Mar;11 (3) :1039-1044.|[4]Shiue SJ, et al. Chronic intrathecal infusion of T-type calcium channel blockers attenuates CaV3.2 upregulation in nerve-ligated rats. Acta Anaesthesiol Taiwan. 2016 Oct 17. pii: S1875-4597 (16) 30071-6.

Shipping Conditions

Blue Ice

Storage Conditions

-20°C (Powder, stored under nitrogen, away from moisture)

Scientific Category

Reference compound1

Clinical Information

Launched

Isoform

L-type calcium channel; T-type calcium channel

Citation 01

ACS Nano. 2024 Nov 12;18 (45) :31451-31465.|Biochem Biophys Res Commun. 2025 Sep 19:785:152676.|Front Pharmacol. 2022 Feb 23;13:816133.|PLoS Biol. 2024 Mar 25;22 (3) :e3002565.|Res Sq. 2024 Jun 11.|Small. 2024 Aug 10:e2403381.|Biochem Biophys Res Commun. 2020 Feb 19;522 (4) :862-868.|Br J Pharmacol. 2021 Jan;178 (2) :346-362.|Eur J Pharmacol. 2021 Feb 5;892:173782.|Front Pharmacol. 2022 Feb 23:13:816133.|J Cell Physiol. 2021 Sep;236 (9) :6548-6558.|Mediators Inflamm. 2020 Nov 10;2020:3691701.|Theriogenology. 2021 Jan 1;159:140-146.

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