Efonidipine

• CAT Number: I000445
• CAS Number: 111011-63-3
• Molecular Formula: C34H38N3O7P
• Molecular Weight: 631.66
• Purity: ≥95%
• Target: calcium channel blocker
• Solubility: 10 mM in DMSO
• Storage: Store at -20°C
• IUPAC Name: 2-(N-benzylanilino)ethyl 5-(5,5-dimethyl-2-oxo-1,3,2lambda5-dioxaphosphinan-2-yl)-2,6-dimethyl-4-(3-nitrophenyl)-1,4-dihydropyridine-3-carboxylate
• InChI: InChI=1S/C34H38N3O7P/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/h5-17,20,31,35H,18-19,21-23H2,1-4H3
• InChIKey: NSVFSAJIGAJDMR-UHFFFAOYSA-N
• SMILES: 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

Efonidipine (Cat.No:I000445) is a calcium channel blocker used in the treatment of hypertension (high blood pressure). It blocks calcium channels in smooth muscles, leading to relaxation and dilation of blood vessels, resulting in reduced blood pressure. Efonidipine may also have additional cardioprotective effects. 

Reference

1:Solid dispersions of efonidipine hydrochloride ethanolate with improved physicochemical and pharmacokinetic properties prepared with microwave treatment. Otsuka M, Maeno Y, Fukami T, Inoue M, Tagami T, Ozeki T.Eur J Pharm Biopharm. 2016 Nov;108:25-31. doi: 10.1016/j.ejpb.2016.08.008. Epub 2016 Aug 20. PMID: 27553261 2:A chiral LC-MS/MS method for the stereospecific determination of efonidipine in human plasma. Liu M, Deng M, Zhang D, Wang X, Ma J, Zhao H, Zhang L, Tong Y, Liu H.J Pharm Biomed Anal. 2016 Apr 15;122:35-41. doi: 10.1016/j.jpba.2016.01.039. Epub 2016 Jan 19. PMID: 26845200 3:Determination of efonidipine in human plasma by LC-MS/MS for pharmacokinetic applications. Liu M, Zhao H, Tong Y, Zhang D, Wang X, Zhang L, Han J, Liu H.J Pharm Biomed Anal. 2015 Jan 25;103:1-6. doi: 10.1016/j.jpba.2014.11.001. Epub 2014 Nov 11. PMID: 25462114 4:The Ca(2+) channel inhibitor efonidipine decreases voltage-dependent K(+) channel activity in rabbit coronary arterial smooth muscle cells. Park MH, Son YK, Hong DH, Choi IW, Kim DJ, Lee H, Bang H, Na SH, Li H, Jo SH, Park WS.Vascul Pharmacol. 2013 Sep-Oct;59(3-4):90-5. doi: 10.1016/j.vph.2013.07.005. Epub 2013 Jul 19. PMID: 23876554 5:Role of specific T-type calcium channel blocker R(-) efonidipine in the regulation of renal medullary circulation. Hu C, Mori T, Lu Y, Guo Q, Sun Y, Yoneki Y, Ohsaki Y, Nakamichi T, Oba I, Sato E, Ogawa S, Dickinson BC, Chang CJ, Miyata T, Sato H, Ito S.J Hypertens. 2012 Aug;30(8):1620-31. doi: 10.1097/HJH.0b013e3283550e9f. PMID: 22688264 6:Efonidipine, another beauty relieving the pressure. Shin J.Korean Circ J. 2012 Apr;42(4):229-30. doi: 10.4070/kcj.2012.42.4.229. Epub 2012 Apr 26. No abstract available. PMID: 22563334 Free PMC Article7:Effects of efonidipine on the pharmacokinetics and pharmacodynamics of repaglinide: possible role of CYP3A4 and P-glycoprotein inhibition by efonidipine. Li C, Choi DH, Choi JS.J Pharmacokinet Pharmacodyn. 2012 Feb;39(1):99-108. doi: 10.1007/s10928-011-9234-0. Epub 2012 Jan 1. PMID: 22210483 8:Effect of efonidipine on TGF-β1-induced cardiac fibrosis through Smad2-dependent pathway in rat cardiac fibroblasts. Lei B, Hitomi H, Mori T, Nagai Y, Deguchi K, Mori H, Masaki T, Nakano D, Kobori H, Kitaura Y, Nishiyama A.J Pharmacol Sci. 2011;117(2):98-105. Epub 2011 Sep 7. PMID: 21897055 Free PMC Article9:Efonidipine, a Ca(2+)-channel blocker, enhances the production of dehydroepiandrosterone sulfate in NCI-H295R human adrenocortical carcinoma cells. Ikeda K, Saito T, Tojo K.Tohoku J Exp Med. 2011 Aug;224(4):263-71. PMID: 21757861 Free Article10:Beneficial Effect of Efonidipine, an L- and T-Type Dual Calcium Channel Blocker, on Heart Rate and Blood Pressure in Patients With Mild-to-Moderate Essential Hypertension. Oh IY, Seo MK, Lee HY, Kim SG, Kim KS, Kim WH, Hyon MS, Han KR, Lim SJ, Kim CH.Korean Circ J. 2010 Oct;40(10):514-9. doi: 10.4070/kcj.2010.40.10.514. Epub 2010 Oct 31. PMID: 21088755 Free PMC Article