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Efonidipine Hydrochloride

Product ID E2258
Cas No. 111011-53-1
Purity ≥98%
Product Unit SizeCostQuantityStock
5 mg $81.90 In stock
10 mg $135.90 In stock
50 mg $465.10 In stock
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Description

Efonidipine is a mixture of R(-) and S(+) isomers that exerts long acting blocking actions on both T-type and L-type calcium channels. It has no blocking effects on N-, P/Q- and R-type Ca(2+) channels. While the S(+) isomer is an active blocker of both the T-type and L-type calcium channels, the action of which is similar to the racemic mixture, its R(-) isomer selectively blocks the T-type channel only. In the prevention of cardiovascular disease efonidipine inhibits in a dose dependent manner the Ang II- and K+-induced aldosterone secretion. It suppresses Ang-II and K+-induced mRNA expression of 11-beta-hydroxylase and aldosterone synthase and induces the production of DHEA sulfate, which has anti-atherosclerotic actions.

Product Info

Cas No.

111011-53-1

Purity

≥98%

Formula

C34H38N3O7P ・HCl

Chemical Name

2-(N-benzylanilino)ethyl 5-(5,5-dimethyl-2-oxo-1,3,2λ5-dioxaphosphinan-2-yl)-2,6-dimethyl-4-(3-nitrophenyl)-1,4-dihydropyridine-3-carboxylate;hydrochloride

IUPAC Name

2-[Benzyl(phenyl)amino]ethyl 5-(5,5-dimethyl-2-oxido-1,3,2-dioxaphosphinan-2-yl)-2,6-dimethyl-4-(3-nitrophenyl)-1,4-dihydro-3-pyridinecarboxylate hydrochloride (1:1)

Synonym

NZ-105

Solubility

Soluble in DMSO (5 mg/ml), and ethanol.

Shipping and Storage

Store Temp

4°C

Ship Temp

Ambient

Downloads

MSDS

E2258 MSDS PDF

Info Sheet

E2258 Info Sheet PDF

References

Furukawa T.,Miura R,Honda M, et al. Idenfication of R(-)-isomer of efonidipine as a selective blocker of T-type Ca2+ channels. Br. J Pharmacol. 2004 Dec; 143(8):1050-7. PIMD:15545287, PMCID:PMC1575949.

Tanaka H, Shigenobu K. Efonidipine hydrochloride: a dual blocker of L- and T-type ca(2+) channels. Cardiovascv Drug Rev. 2002 Winter; 20(1):81-92. PMID:12070536.

Imafawa K, Okayama S, Takaoka M, et al Inhibitory effect of efonidipine on aldosterone synthesis and secretion on human adrenocarcinoma (H195R) cells. J Cardiovasc Pharmacol. 2006 Jan; 47(1):133-8. PMID:16424797.

Ikeda K, Saito T, Tojo K. Efonidipine, a Ca(2+)-channel blocker, enhances the production of dehydroepiandrosterone sulfate in NCI-H195 R human adrenocortical carcinoma cells. Tohoku J Exp Med. 2011; 224(4):263-71. PMID:21757861.

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