Efonidipine hydrochloride  (Synonyms: NZ-105 hydrochloride; (±)-Efonidipine hydrochloride)

Efonidipine (NZ-105) hydrochloride is an orally active dual L-type and T-type calcium channel blocker (CCB) with IC₅₀ values of 1.8 and 350 nM, respectively. Efonidipine hydrochloride inhibits SARS-CoV-2 main protease. Efonidipine hydrochloride modulates adrenal steroidogenesis by increasing the expression of steroidogenic acute regulatory protein (StAR), dbcAMP-or angiotensin II-induced StAR mRNA expression and DHEA-S production, while suppressing the biosynthesis of aldosterone and cortisol. Efonidipine hydrochloride reduces plasma aldosterone levels in vivo. Efonidipine hydrochloride improves cardiac function in heart failure models by inhibiting T-type calcium channels (via both tonic and use-dependent blockade), independently of blood pressure reduction. Efonidipine hydrochloride can be used for research in hypertension, heart failure, and disorders involving dysregulated steroid hormone synthesis^{[1][2][3][4][5]}.

Efonidipine (10 μM, 24 h) hydrochloride induces an increase in StAR mRNA that is independent of extracellular Ca²⁺ in NCI-H295R human adrenocortical cells^[2].
Efonidipine (1 μM, 24 h) hydrochloride significantly increases the production of DHEA-S in NCI-H295R human adrenocortical cells^[2].

MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.

Efonidipine (0.1% in diet, p.o., 4 weeks) hydrochloride inhibits T type calcium channels and improves cardiac function during the progression of heart failure in UM-X7.1 hamsters and gold hamsters^[1].

MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.

668.12

C₃₄H₃₉ClN₃O₇P

111011-53-1

CC1=C(P2(OCC(C)(C)CO2)=O)C(C3=CC([N+]([O-])=O)=CC=C3)C(C(OCCN(C4=CC=CC=C4)CC5=CC=CC=C5)=O)=C(C)N1.Cl

Room temperature in continental US; may vary elsewhere.

Please store the product under the recommended conditions in the Certificate of Analysis.

• [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.  [Content Brief]

  [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.  [Content Brief]

  [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.  [Content Brief]

  [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.  [Content Brief]

  [5]. Ghahremanpour MM, et al. Identification of 14 Known Drugs as Inhibitors of the Main Protease of SARS-CoV-2. bioRxiv [Preprint]. 2020 Aug 28:2020.08.28.271957.