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Home / Biochemicals / Small Molecules

Lomerizine dihydrochloride

SKU : BHB21300197

A Blocker of L-Type Voltage-Gated Ca2+ Channels

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Mfr.No.	L-125, L-125_1 g, L-125_100 mg, L-125_50 mg, L-125_500 mg
Description	Lomerizine dihydrochloride (#L-125) is a highly pure, synthetic, and biologically active compound.
Molecular Formula	C27H32N2F2O3Cl2.
Background	Voltage-dependent L-type Ca2+ channels play an important role Ca2+ influx. L-type calcium currents typically require a strong depolarization for activation and are long-lasting1.The common pharmacological profile of L-type channels is determined by the alpha1 subunit, which forms the Ca2+ selective pore, and is encoded by one of the CaV1 (alpha 1S) channel genes2. Cav1.2 (CACNA1C) in humans is widely expressed in cardiac myocytes, smooth muscle myocytes, endocrine cells, neuronal cell bodies and proximal dendrites1.Lomerizine dihydrochloride is a Ca2+ channel blocker with relatively selective CNS effects. Lomerizine was developed as a potential agent for the selective improvement of the ocular or cerebrovascular circulation with minimal adverse cardiovascular effects3, and it is used as an anti migraine drug4. Lomerizine selectively relaxes smooth muscle cells by inhibiting L-type Ca2+ influx, thereby reducing tone and increasing blood flow in cerebral vessels4.Lomerizine blocked Ba2+ current through the voltage-gated Ca2+ channel in rat pheochromocytoma (PC12) cells5, and it is suggested to bind to the 1,4-dihydropyridine binding site, as obtained by a (3H)nitrendipine binding study6.
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	0.5-100 uM.
Reconstitution	DMSO. Centrifuge all product preparations before use (10000 x g 5 min).
Cas Number	101477-54-7
Molecular Weight	541.5
Solubility	DMSO. Centrifuge all product preparations before use (10000 x g 5 min).
Target	L-type Ca2+ channels
Source	Synthetic
Activity	Lomerizine dihydrochloride inhibited CaV currents in PC12 cells with IC50 of 1.9 uM1. It inhibits L-type Ca2+ channels2.
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: 1-(Bis(4-fluorophenyl)methyl)-4-((2,3,4-trimethoxyphenyl)methyl)piperazine dihydrochloride.

Purity	>99%
Form	Lyophilized Powder
Storage	Storage After Reconstitution: Store the reconstituted solution for the shortest time possible at -20°C. We do not recommend storing the product in working solution for longer than one day. 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	Catterall, W.A. et al. (2003) Pharmacol. Rev. 55, 579. Streissnig, J. et al. (1998) Trends. Pharmacol Sci. 19, 108. Hara, T. et al. (1995) CNS Drug Rev. 1, 204. Ito, Y. et al. (2010) CNS Neurosci. Ther. 16, 103. Watano, T. et al. (1997) Jpn. J. Pharmacol. 75, 209. Iwamoto, T. et al. (1988) Jpn J Pharmacol 48, 241. Watano, T. et al. (1997) Jpn. J. Pharmacol. 75, 209. Iwamoto, T. et al. (1988) Jpn J Pharmacol 48, 241.

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Combination SKU	Supplier No.	Size	Your price	Quantity
BHB21300197-1	L-125_1 g	1 g	$188		Add to Cart
BHB21300197-2	L-125_100 mg	100 mg	$75		Add to Cart
BHB21300197-3	L-125_50 mg	50 mg	$55		Add to Cart
BHB21300197-4	L-125_500 mg	500 mg	$129		Add to Cart

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