Efonidipine hydrochloride
Based on 1 publication(s) in Google Scholar
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.
For research use only. We do not sell to patients.
- CAS No.: 111011-53-1
- Formula: C34H39ClN3O7P
- Molecular Weight:668.12
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Storage:
Please store the product under the recommended conditions in the Certificate of Analysis.
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Biological Activity
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Chemical Information
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Solvent & Solubility
- Purity & Documentation
- References
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Help & FAQs
Publications Citing Use of MedChemExpress (MCE) Efonidipine hydrochloride
MoreAll Calcium Channel Isoforms
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Biological Activity
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L-type calcium channel 1.8 nM (IC50) |
T-type calcium channel 350 nM (IC50) |
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.
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Cell Line:NCI-H295R human adrenocortical cells
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Concentration:10 μM
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Incubation Time:24 h
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Result:Dose-dependently and significantly enhanced the dbcAMP-induced expression of StAR mRNA.
Enhanced the angiotensin II-induced expression of StAR mRNA.
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Cell Line:NCI-H295R human adrenocortical cells
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Concentration:10 μM
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Incubation Time:24 h
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Result:Significantly and dose-dependently enhanced the dbcAMP-induced expression of StAR protein.
MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.
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Animal Model:UM-X7.1 hamsters and gold hamsters[1]
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Dosage:0.1% in diet
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Administration:p.o. 4 weeks
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Result:Showed an increase in body weight with no remarkable increase in the biventricular-to-body weight ratio in UM-X7.1 hamsters but not affected the ratio of gold hamsters.
Did not affect the expression of TCCa1G mRNA in either the golden and UM-X7.1 hamster.
Increased left ventricular ejection fraction (LVEF) in UM-X7.1 hamster.
Did not significantly affect blood pressure in either UM X7.1 hamsters or golden hamsters.
Reduced heart rate by approximately 10%.
Significantly lowered the BNP level in UM X7.1 hamsters (from 35.2 pg/ml to 30.5 pg/ml), and the BNP level did not differ significantly in golden hamster group.
Chemical Information
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CAS No. 111011-53-1
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Molecular Weight 668.12
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Formula C34H39ClN3O7P
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SMILES
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
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Synonyms
NZ-105 hydrochloride; (±)-Efonidipine hydrochloride
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Shipping
Room temperature in continental US; may vary elsewhere.
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Storage
Please store the product under the recommended conditions in the Certificate of Analysis.
Publications (1)
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Journal Impact Factor
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Most Recent
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Basic Clin Pharmacol Toxicol
A New Method for Antispastic Effect in Coronary Artery Bypass Grafts by Using a L- and T-Type Calcium Channel Blocker Efonidipine. [Abstract]2025 Aug;137(2):e70077. PMID: 40624735
Solvent & Solubility
DMSO : 8.5 mg/mL (12.72 mM; Need ultrasonic and warming; Hygroscopic DMSO has a significant impact on the solubility of product, please use newly opened DMSO)
Concentration (start) × Volume (start) = Concentration (final) × Volume (final)
Purity & Documentation
References
[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]
Complete Stock Solution Preparation Table
| Optional Solvent | Concentration Solvent Mass | 1 mg | 5 mg | 10 mg | 25 mg |
|---|---|---|---|---|---|
| DMSO | 1 mM | 1.4967 mL | 7.4837 mL | 14.9674 mL | 37.4184 mL |
| 5 mM | 0.2993 mL | 1.4967 mL | 2.9935 mL | 7.4837 mL | |
| 10 mM | 0.1497 mL | 0.7484 mL | 1.4967 mL | 3.7418 mL |
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