Efonidipine hydrochloride monoethanolate

• CAT Number: I000446
• CAS Number: 111011-76-8
• Molecular Formula: C34H38N3O7P.HCl.C2H5OH
• Molecular Weight: 714.18
• Purity: ≥95%
• Synonyms: NZ-105
• Target: Calcium Channel
• Solubility: DMSO: ≤ 8.5 mg/mL
• Storage: 2-8°C
• IUPAC 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;ethanol;hydrochloride
• InChI: InChI=1S/C34H38N3O7P.C2H6O.ClH/c1-24-30(33(38)42-19-18-36(28-15-9-6-10-16-28)21-26-12-7-5-8-13-26)31(27-14-11-17-29(20-27)37(39)40)32(25(2)35-24)45(41)43-22-34(3,4)23-44-45;1-2-3;/h5-17,20,31,35H,18-19,21-23H2,1-4H3;3H,2H2,1H3;1H
• InChIKey: IKBJGZQVVVXCEQ-UHFFFAOYSA-N
• SMILES: CCO.CC1=C(C(C(=C(N1)C)P2(=O)OCC(CO2)(C)C)C3=CC(=CC=C3)[N+](=O)[O-])C(=O)OCCN(CC4=CC=CC=C4)C5=CC=CC=C5.Cl

Efonidipine (NZ-105) HCl monoethanolamine （Cat No.:I000446） is a calcium channel blocker (CCB) that exhibits dual activity, targeting both T-type and L-type calcium channels. By blocking these channels, efonidipine inhibits the influx of calcium ions into cells, thereby reducing calcium-dependent signaling and smooth muscle contraction. This dual inhibition of T-type and L-type calcium channels contributes to its therapeutic effects, including vasodilation, blood pressure reduction, and potential benefits in the treatment of cardiovascular conditions such as hypertension and angina pectoris.

Reference

[1]. Ikeda K, et al. Efonidipine, a Ca(2+)-channel blocker, enhances the production of dehydroepiandrosterone sulfate in NCI-H295R human adrenocortical carcinoma cells. Tohoku J Exp Med. 2011;224(4):263-71. 


[2]. Nakano N, et al. Effects of efonidipine, an L- and T-type calcium channel blocker, on the renin-angiotensin-aldosterone system in chronic hemodialysis patients. Int Heart J. 2010 May;51(3):188-92. 


[3]. Suzuki S, et al. Beneficial effects of the dual L- and T-type Ca2+ channel blocker efonidipine on cardiomyopathic hamsters. Circ J. 2007 Dec;71(12):1970-6. 


[4]. Lee TS, et al. Actions of mibefradil, efonidipine and nifedipine block of recombinant T- and L-type Ca channels with distinct inhibitory mechanisms. Pharmacology. 2006;78(1):11-20.