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Home / Biochemicals / Small Molecules

Mibefradil dihydrochloride hydrate

SKU : BHB21300214

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

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Mfr.No.	M-150, M-150_1 mg, M-150_10 mg, M-150_25 mg, M-150_5 mg, M-150_50 mg
Description	Mibefradil dihydrochloride hydrate (#M-150) is a highly pure, synthetic, and biologically active compound.
Molecular Formula	C29H40Cl2FN3O3.
Synonyms	Synthetic
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 uM 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 uM and 18.6 uM 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.
Shipping	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
Concentration	0.01-50 uM.
Reconstitution	Centrifuge the vial before adding solvent (10,000 x g for 5 minutes) to spin down all the powder to the bottom of the vial. The lyophilized product may be difficult to visualize. Add solvent directly to the centrifuged vial. Tap the vial to aid in dissolving the lyophilized product. Tilt and gently roll the liquid over the walls of the vial. Avoid vigorous vortexing. Light vortexing for up to 3 seconds is acceptable if needed. For long-term storage in solution, we recommend preparing a stock solution by dissolving the product in sterile water at a concentration of at least 0.1 mg/mL. Divide the stock solution into small aliquots and store at -20°C. Before use, thaw the relevant vial(s) and dilute to the desired working concentration in your working buffer. It is recommended to prepare fresh solutions in working buffers just before use. Repeat freeze-thawing may result in loss of activity.
Cas Number	116666-63-8
Molecular Weight	568.55
Solubility	35 mM in water, 100 mM in DMSO. Centrifuge all product preparations before use (10 000 x g for 1 min).
Target	CaV3, Orai1-3, KV10.1 channels
Activity	Mibefradil blocks T-type Ca2+ channels with an IC50 of ~1 uM. Orai1-3 and most potent on Orai32. It also modulates the gating properties of KV10.1 channel3.
Country Of Origin	Israel/IL
UNSPSC Code	41116134
Application	FC- Flow cytometry, IFC- Indirect flow cytometry, IHC- Immunohistochemistry,LCI- Live cell imaging, Calcium imaging assay,Cell survival assay, Electrophysiology, Neurite outgrowth assay
Lead Time	1-2 Business Days
Notes	Bioassay Tested: Yes 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.

Purity	>98%
Form	Lyophilized powder.
Storage	Storage After Reconstitution: The reconstituted solution can be stored at 4°C for up to 1 week. For longer periods (up to 6 months), small aliquots should be stored at -20°C. We do not recommend storing the product in working solutions for longer than a few days. Avoid multiple freeze-thaw cycles. Storage of solutions: Up to four weeks at 4°C or three months at -20°C.

Product Manual	SDS

Reference	Martin, R.L. et al. (2000) J. Pharmacol. Exp. Ther. 295, 302. Brogden, R.N. et al. (1997) Drugs 54, 774. Major, T.C. et al. (2008) J. Pharmacol. Exp. Ther. 325, 723. Keir, S.T. et al. (2013) J. Neurooncol. 111, 97. Sheehan, J.P. et al. (2013) J. Neurosurg. 118, 830. Gomez-Lagunas, F. et al. (2017) J. Cell. Physiol. 232, 2019. Li, P. et al. (2019) Br. J. Pharmacol. 176, 3845. Martin, R.L. et al. (2000) J. Pharmacol. Exp. Ther. 295, 302. Li, P. et al. (2019) Br. J. Pharmacol. 176, 3845. Gomez-Lagunas, F. et al. (2017) J. Cell. Physiol. 232, 2019.

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Combination SKU	Supplier No.	Size	Your price	Quantity
BHB21300214-1	M-150_1 mg	1 mg	$132		Add to Cart
BHB21300214-2	M-150_10 mg	10 mg	$266		Add to Cart
BHB21300214-3	M-150_25 mg	25 mg	$634		Add to Cart
BHB21300214-4	M-150_5 mg	5 mg	$151		Add to Cart
BHB21300214-5	M-150_50 mg	50 mg	$1227		Add to Cart

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