Art. -Nr.: HY-12502

Efonidipine

(Synonyms: NZ-105; (±)-Efonidipine)

1 Cited Publications

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Based on 1 publication(s) in Google Scholar

Efonidipine (NZ-105) 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 inhibits SARS-CoV-2 main protease. Efonidipine 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 reduces plasma aldosterone levels in vivo. Efonidipine 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 can be used for research in hypertension, heart failure, and disorders involving dysregulated steroid hormone synthesis.

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Reinheit: 99.88%
CAS. Nr.: 111011-63-3
Formel: C₃₄H₃₈N₃O₇P
Molecular Weight:631.66

Speicherung:

Powder -20°C, 3 years , 4°C, 2 years ; In solvent -80°C, 6 months , -20°C, 1 month

Efonidipine Chemical Structure

CAS. Nr.: 111011-63-3

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Biologische Aktivität
- Beschreibung
- IC₅₀ & Target
- Cellular Effect
- In Vitro
- In Vivo
- Clinical Trial
Chemical Information
Publications (1)
Lösungsmittel & Löslichkeit
- In Vitro
- In Vivo
Reinheit & Dokumentation
Verweise
Help & FAQs
Classifications
Bioz

Biologische Aktivität

Beschreibung

IC₅₀ & Target

L-type calcium channel

1.8 nM (IC₅₀)

T-type calcium channel

350 nM (IC₅₀)

Alle Calcium Channel Isoform-spezifische Produkte anzeigen :

Cellular Effect

Cell Line	Type	Value	Description	References
LLC-PK1	IC₅₀	13 μM Compound: Efonidipine	TP_TRANSPORTER: inhibition of Digoxin transepithelial transport (basal to apical) (Digoxin: 0.1 uM) in MDR1-expressing LLC-PK1 cells TP_TRANSPORTER: inhibition of Digoxin transepithelial transport (basal to apical) (Digoxin: 0.1 uM) in MDR1-expressing LLC-PK1 cells	[PMID: 12128170]
LLC-PK1	IC₅₀	17.3 μM Compound: Efonidipine	TP_TRANSPORTER: inhibition of Daunorubicin transepithelial transport (basal to apical), (-)-efonidipine (Daunorubicin: 0.035 uM) in MDR1-expressing LLC-PK1 cells TP_TRANSPORTER: inhibition of Daunorubicin transepithelial transport (basal to apical), (-)-efonidipine (Daunorubicin: 0.035 uM) in MDR1-expressing LLC-PK1 cells	[PMID: 11145223]
LLC-PK1	IC₅₀	20.6 μM Compound: Efonidipine	TP_TRANSPORTER: inhibition of Daunorubicin transepithelial transport (basal to apical), (+)-efonidipine (Daunorubicin: 0.035 uM) in MDR1-expressing LLC-PK1 cells TP_TRANSPORTER: inhibition of Daunorubicin transepithelial transport (basal to apical), (+)-efonidipine (Daunorubicin: 0.035 uM) in MDR1-expressing LLC-PK1 cells	[PMID: 11145223]

In Vitro

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

RT-PCR^[1]

Cell Line:

NCI-H295R human adrenocortical cells
Concentration:

10 μM
Incubation Time:

24 h
Result:

Dose-dependently and significantly enhanced the dbcAMP-induced expression of StAR mRNA.
Enhanced the angiotensin II-induced expression of StAR mRNA.

Western Blot Analysis^[1]

Cell Line:

NCI-H295R human adrenocortical cells
Concentration:

10 μM
Incubation Time:

24 h
Result:

Significantly and dose-dependently enhanced the dbcAMP-induced expression of StAR protein.

In Vivo

Efonidipine (0.1% in diet, p.o., 4 weeks) 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.

Animal Model:

UM-X7.1 hamsters and gold hamsters^[1]
Dosage:

0.1% in diet
Administration:

p.o. 4 weeks
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.

Clinical Trial

NCT Number	Sponsor	Condition	Start Date	Phase A549
NCT01329991	Plexxikon\|		2011-05	PHASE1

Chemical Information

CAS. Nr. 111011-63-3
Appearance Solid
Molecular Weight 631.66
Formel C₃₄H₃₈N₃O₇P
Color Off-white to yellow
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
Synonyms

NZ-105; (±)-Efonidipine
Versand

Room temperature in continental US; may vary elsewhere.

Speicherung

Powder	-20°C	3 years
	4°C	2 years
In solvent	-80°C	6 months
	-20°C	1 month

Publications (1)

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Journal Impact Factor

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

Lösungsmittel & Löslichkeit

In Vitro:

DMSO : 100 mg/mL (158.31 mM; Need ultrasonic; Hygroscopic DMSO has a significant impact on the solubility of product, please use newly opened DMSO)

View the Complete Stock Solution Preparation Table

Preparing Stock Solutions

View the Complete Stock Solution Preparation Table

Concentration Solvent Mass

1 mg

5 mg

10 mg

Concentration

Solvent

Mass

1 mM

1.5831 mL

7.9157 mL

15.8313 mL

5 mM

0.3166 mL

1.5831 mL

3.1663 mL

10 mM

0.1583 mL

0.7916 mL

1.5831 mL

Please refer to the solubility information to select the appropriate solvent. Once prepared, please aliquot and store the solution to prevent product inactivation from repeated freeze-thaw cycles.

Storage method and period of stock solution: -80°C, 6 months; -20°C, 1 month. When stored at -80°C, please use it within 6 months. When stored at -20°C, please use it within 1 month.

Molaritätsrechner

Mass (g) = Concentration (mol/L) × Volume (L) × Molecular Weight (g/mol)

Mass Mass

Konzentration Konzentration

Volumen Volumen

Molecular Weight Molecular Weight

Verdünnungsrechner

Konzentration _{(Stammlösung)} × Volumen _{(Stammlösung)} = Konzentration _{(Ziellösung)} × Volumen _{(Ziellösung)}

Konzentration _{(Stammlösung)} Konzentration _{(Stammlösung)}

Volumen _{(Stammlösung)} Volumen _{(Stammlösung)}

Konzentration _{(Ziellösung)} Konzentration _{(Ziellösung)}

Volumen _{(Ziellösung)} Volumen _{(Ziellösung)}

In Vivo:

Select the appropriate dissolution method based on your experimental animal and administration route.

Stock Solution Working Solution

For the following dissolution methods, please ensure to first prepare a clear stock solution using an In Vitro approach and then sequentially add co-solvents:
To ensure reliable experimental results, the clarified stock solution can be appropriately stored based on storage conditions. As for the working solution for In Vivo experiments, it is recommended to prepare freshly and use it on the same day.
The percentages shown for the solvents indicate their volumetric ratio in the final prepared solution. If precipitation or phase separation occurs during preparation, heat and/or sonication can be used to aid dissolution.

Protocol 1

Add each solvent one by one: 10% DMSO 40% PEG300 5% Tween-80 45% Saline

Solubility: ≥ 2.5 mg/mL (3.96 mM); Clear solution

This protocol yields a clear solution of ≥ 2.5 mg/mL (saturation unknown).

Taking 1 mL working solution as an example, add 100 μL DMSO stock solution (25.0 mg/mL) to 400 μL PEG300, and mix evenly; then add 50 μL Tween-80 and mix evenly; then add 450 μL Saline to adjust the volume to 1 mL.

Protocol 2

Add each solvent one by one: 10% DMSO 90% Corn Oil

Solubility: 2.5 mg/mL (3.96 mM); Clear solution; Need ultrasonic

This protocol yields a clear solution of 2.5 mg/mL. If the continuous dosing period exceeds half a month, please choose this protocol carefully.

Taking 1 mL working solution as an example, add 100 μL DMSO stock solution (25.0 mg/mL) to 900 μL Corn oil, and mix evenly.

In Vivo Dissolution Calculator

Please enter the basic information of animal experiments:

Dosage Dosage
mg/kg
Animal Weight (Per Animal) Animal Weight (Per Animal)
g
Dosing Volume (Per Animal) Dosing Volume (Per Animal)
μL
Number of Animals Number of Animals

Recommended: Prepare an additional quantity of animals to account for potential losses during experiments.

Recommended: Prepare an additional quantity of animals to account for potential losses during experiments.

Please enter your animal formula composition:

%
DMSO +

Recommended: Keep the proportion of DMSO in working solution below 2% if your animal is weak.
%
+
+
%
Tween-80 + +
%
Saline +

The co-solvents required include: DMSO, . All of co-solvents are available by MedChemExpress (MCE). , Tween 80. All of co-solvents are available by MedChemExpress (MCE).

Working solution concentration: 0.22 mg/mL

Reinheit & Dokumentation

Select Batch:

Reinheit: 99.98%

Assay: 99.98%

ee.: 99.98%

Data Sheet (281 KB)
SDS (644 KB)
- English - EN (644 KB)
- Français - FR (644 KB)
- Deutsch - DE (644 KB)
- Norwegian - NO (644 KB)
- Español - ES (644 KB)
- Swedish - SV (644 KB)
- Italian - IT (644 KB)
- Korean - KR (644 KB)
- Portuguese - PT (644 KB)
COA (2659 KB)
Elemental Analysis Report (2659 KB)
HNMR (2659 KB)
CNMR (2659 KB)
RP-HPLC (2659 KB)
NP-HPLC (2659 KB)
MS (2659 KB)
LCMS (2659 KB)
IR (2659 KB)
GC (2659 KB)
OR (2659 KB)
SDS-PAGE (2659 KB)
SEC-HPLC (2659 KB)
Other Report (2659 KB)
Handling Instructions (2659 KB)

Verweise

[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.

Help & FAQs

How should lyophilized recombinant proteins be reconstituted and stored?

1. Before opening the cap, centrifuge the vial at 13000 rpm for 20-30 seconds. This step will ensure that any lyophilized powder that may have adhered to the cap or walls is collected at the bottom of the vial, minimizing the risk of product loss.

Complete Stock Solution Preparation Table

Storage method and period of stock solution: -80°C, 6 months; -20°C, 1 month. When stored at -80°C, please use it within 6 months. When stored at -20°C, please use it within 1 month.

Optional Solvent	Concentration Solvent Mass	1 mg	5 mg	10 mg	25 mg
DMSO	1 mM	1.5831 mL	7.9157 mL	15.8313 mL	39.5783 mL
	5 mM	0.3166 mL	1.5831 mL	3.1663 mL	7.9157 mL
	10 mM	0.1583 mL	0.7916 mL	1.5831 mL	3.9578 mL
	15 mM	0.1055 mL	0.5277 mL	1.0554 mL	2.6386 mL
	20 mM	0.0792 mL	0.3958 mL	0.7916 mL	1.9789 mL
	25 mM	0.0633 mL	0.3166 mL	0.6333 mL	1.5831 mL
	30 mM	0.0528 mL	0.2639 mL	0.5277 mL	1.3193 mL
	40 mM	0.0396 mL	0.1979 mL	0.3958 mL	0.9895 mL
	50 mM	0.0317 mL	0.1583 mL	0.3166 mL	0.7916 mL
	60 mM	0.0264 mL	0.1319 mL	0.2639 mL	0.6596 mL
	80 mM	0.0198 mL	0.0989 mL	0.1979 mL	0.4947 mL
	100 mM	0.0158 mL	0.0792 mL	0.1583 mL	0.3958 mL

Keywords

Efonidipine

1 Cited Publications

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Efonidipine

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Publications Citing Use of MedChemExpress (MCE) Efonidipine

Alle Calcium Channel Isoform-spezifische Produkte anzeigen

Biologische Aktivität

Chemical Information

Publications (1)

Lösungsmittel & Löslichkeit

Reinheit & Dokumentation

Verweise

Help & FAQs

Complete Stock Solution Preparation Table

Efonidipine Related Classifications

HY-12502 Related Classifications