Art. -Nr.: HY-12515

Nicardipine

(Synonyms: YC-93 free base)

6 Cited Publications

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Based on 6 publication(s) in Google Scholar

Nicardipine (YC-93 free base) is a calcium channel blocker with an IC₅₀ of 1 μM for blocking cardiac calcium channels. Nicardipine acts as an agent for chronic stable angina and for controlling blood pressure.

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Reinheit: 99.75%
CAS. Nr.: 55985-32-5
Formel: C₂₆H₂₉N₃O₆
Molecular Weight:479.52

Speicherung:

4°C, protect from light

* In solvent : -80°C, 6 months; -20°C, 1 month (protect from light)

Nicardipine Chemical Structure

CAS. Nr.: 55985-32-5

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Biologische Aktivität
- Beschreibung
- IC₅₀ & Target
- Cellular Effect
- In Vitro
- In Vivo
- Clinical Trial
Chemical Information
Publications (6)
Lösungsmittel & Löslichkeit
- In Vitro
- In Vivo
Reinheit & Dokumentation
Verweise
Help & FAQs
Classifications
Bioz

Biologische Aktivität

Beschreibung

IC₅₀ & Target

IC50: 1 μM (cardiac calcium channels)^[1]

Alle Calcium Channel Isoform-spezifische Produkte anzeigen :

Cellular Effect

Cell Line	Type	Value	Description	References
CHO	EC₅₀	0.5 μM Compound: 55	Agonist activity at mouse TRPA1 channel expressed in CHO cells assessed as increase in intracellular calcium influx Agonist activity at mouse TRPA1 channel expressed in CHO cells assessed as increase in intracellular calcium influx	[PMID: 20356305]
HEK293	IC₅₀	0.25 μM Compound: Nicardipine	Inhibition of L-type calcium channel measured using 2-electrode voltage-clamp in human embryonic kidney cells heterologically expressing alpha-1C subunit Inhibition of L-type calcium channel measured using 2-electrode voltage-clamp in human embryonic kidney cells heterologically expressing alpha-1C subunit	[PMID: 22761000]
LLC-MK2	IC₅₀	10.59 μM Compound: Nicardipine	Antitrypanosomal activity against trypomastigotes of Trypanosoma cruzi infected in rhesus monkey LLC-MK2 cells after 48 hrs by MTT assay Antitrypanosomal activity against trypomastigotes of Trypanosoma cruzi infected in rhesus monkey LLC-MK2 cells after 48 hrs by MTT assay	[PMID: 20934347]
LLC-MK2	IC₅₀	71.59 μM Compound: Nicardipine	Cytotoxicity against rhesus monkey LLC-MK2 cells after 48 hrs by MTT assay Cytotoxicity against rhesus monkey LLC-MK2 cells after 48 hrs by MTT assay	[PMID: 20934347]
LLC-PK1	IC₅₀	17.5 μM Compound: Nicardipine	TP_TRANSPORTER: inhibition of Daunorubicin transepithelial transport (basal to apical) (Daunorubicin: 0.035 uM) in MDR1-expressing LLC-PK1 cells TP_TRANSPORTER: inhibition of Daunorubicin transepithelial transport (basal to apical) (Daunorubicin: 0.035 uM) in MDR1-expressing LLC-PK1 cells	[PMID: 11145223]
LLC-PK1	IC₅₀	4.54 μM Compound: Nicardipine	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	2.3 μM Compound: Nicardipine	Inhibition of P-glycoprotein, human L-MDR1 expressed in LLC-PK1 epithelial cells using calcein-AM polarisation assay Inhibition of P-glycoprotein, human L-MDR1 expressed in LLC-PK1 epithelial cells using calcein-AM polarisation assay	[PMID: 12699389]
LLC-PK1	IC₅₀	2.3 μM Compound: Nicardipine	TP_TRANSPORTER: inhibition of Calcein-AM efflux in MDR1-expressing LLC-PK1 cells TP_TRANSPORTER: inhibition of Calcein-AM efflux in MDR1-expressing LLC-PK1 cells	[PMID: 12699389]
LLC-PK1	IC₅₀	2.5 μM Compound: Nicardipine	Inhibition of P-glycoprotein, mouse L-mdr1a expressed in LLC-PK1 epithelial cells using calcein-AM polarisation assay Inhibition of P-glycoprotein, mouse L-mdr1a expressed in LLC-PK1 epithelial cells using calcein-AM polarisation assay	[PMID: 12699389]
LLC-PK1	IC₅₀	2.5 μM Compound: Nicardipine	TP_TRANSPORTER: inhibition of Calcein-AM efflux in Mdr1a-expressing LLC-PK1 cells TP_TRANSPORTER: inhibition of Calcein-AM efflux in Mdr1a-expressing LLC-PK1 cells	[PMID: 12699389]
LLC-PK1	IC₅₀	8 μM Compound: Nicardipine	Inhibition of P-glycoprotein, mouse L-mdr1b expressed in LLC-PK1 epithelial cells using calcein-AM polarisation assay Inhibition of P-glycoprotein, mouse L-mdr1b expressed in LLC-PK1 epithelial cells using calcein-AM polarisation assay	[PMID: 12699389]
LLC-PK1	IC₅₀	8 μM Compound: Nicardipine	TP_TRANSPORTER: inhibition of Calcein-AM efflux in Mdr1b-expressing LLC-PK1 cells TP_TRANSPORTER: inhibition of Calcein-AM efflux in Mdr1b-expressing LLC-PK1 cells	[PMID: 12699389]
NIH-3T3-G185	IC₅₀	>25.8 μM Compound: Nicardipine	TP_TRANSPORTER: inhibition of Rhodamine 123 efflux in NIH-3T3-G185 cells TP_TRANSPORTER: inhibition of Rhodamine 123 efflux in NIH-3T3-G185 cells	[PMID: 11716514]
NIH-3T3-G185	IC₅₀	11.7 μM Compound: Nicardipine	TP_TRANSPORTER: inhibition of Tetramethylrosamine efflux in NIH-3T3-G185 cells TP_TRANSPORTER: inhibition of Tetramethylrosamine efflux in NIH-3T3-G185 cells	[PMID: 11716514]
NIH-3T3-G185	IC₅₀	14.6 μM Compound: Nicardipine	TP_TRANSPORTER: inhibition of Fluo-3-AM efflux in NIH-3T3-G185 cells TP_TRANSPORTER: inhibition of Fluo-3-AM efflux in NIH-3T3-G185 cells	[PMID: 11716514]
NIH-3T3-G185	IC₅₀	3.2 μM Compound: Nicardipine	TP_TRANSPORTER: inhibition of Daunorubicin efflux in NIH-3T3-G185 cells TP_TRANSPORTER: inhibition of Daunorubicin efflux in NIH-3T3-G185 cells	[PMID: 11716514]
NIH-3T3-G185	IC₅₀	5.6 μM Compound: Nicardipine	TP_TRANSPORTER: inhibition of LDS-751 efflux in NIH-3T3-G185 cells TP_TRANSPORTER: inhibition of LDS-751 efflux in NIH-3T3-G185 cells	[PMID: 11716514]
NIH-3T3-G185	IC₅₀	6.6 μM Compound: Nicardipine	TP_TRANSPORTER: inhibition of Calcein-AM efflux in NIH-3T3-G185 cells TP_TRANSPORTER: inhibition of Calcein-AM efflux in NIH-3T3-G185 cells	[PMID: 11716514]
NIH-3T3-G185	IC₅₀	7.1 μM Compound: Nicardipine	TP_TRANSPORTER: inhibition of JC-1 efflux in NIH-3T3-G185 cells TP_TRANSPORTER: inhibition of JC-1 efflux in NIH-3T3-G185 cells	[PMID: 11716514]

In Vitro

Nicardipine (0.1-10 μM; 24-48 h) reduces viability and proliferation of vascular smooth muscle cells (VSMCs) and inhibits their ability to migrate^[2].

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

Cell Viability Assay^[2]

Cell Line:

VSMCs were isolated from New Zealand rabbit aortic preparations
Concentration:

0.1 μM, 1 μM, 3 μM, 10 μM
Incubation Time:

24-48 hours
Result:

Treatment reduced significantly cell viability and inhibited VSMCs proliferation in the presence of 10% FBS in a dose-dependent way, from 205.4±17.5% to 176.6±17%, 160.6±5.7%, 150.4±11.2%, 61.22±7.83% after 0.1 μM, 1 μM, 3 μM, 10 μM treatment, respectively.

In Vivo

Nicardipine (0.3-10 mg/kg; p.o.) shows antihypertensive properties^[3].
LD₅₀s of Nicardipine are 643 mg/kg (oral) and 557 mg/kg (oral); 18.1 mg/kg (intravenous) 25.0 mg/kg (intravenous); 735 mg/kg (subcutaneous) and 683 mg/kg (subcutaneous); 171 mg/kg (intraperitoneally) and 155 mg/kg (intraperitoneally) for male and female Sprague-Dawley rats, respectively^[3].
LD₅₀s of Nicardipine are 187 mg/kg (oral) and 15.5 mg/kg (intravenous) for male Wistar rats, respectively^[3].
LD₅₀s of Nicardipine are 634 mg/kg (oral) and 650 mg/kg (oral); 20.7 mg/kg (intravenous) 19.9 mg/kg (intravenous); 540 mg/kg (subcutaneous) and 710 mg/kg (subcutaneous); 144 mg/kg (intraperitoneally) and 161 mg/kg (intraperitoneally) for male and female mice, respectively^[3].

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

Animal Model:

In conscious normotensive rats (NR)^[3]
Dosage:

0.3-10 mg/kg
Administration:

P.o.
Result:

Induced a dose-dependent hypotensive response (maximal decrease in mean blood pressure, supine position) without any postural hypotensive response.

Clinical Trial

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

Chemical Information

CAS. Nr. 55985-32-5
Appearance Solid
Molecular Weight 479.52
Formel C₂₆H₂₉N₃O₆
Color Light yellow to yellow
SMILES

O=C(C1=C(C)NC(C)=C(C(OCCN(C)CC2=CC=CC=C2)=O)C1C3=CC=CC([N+]([O-])=O)=C3)OC
Synonyms

YC-93 free base
Versand

Room temperature in continental US; may vary elsewhere.
Speicherung

4°C, protect from light

* In solvent : -80°C, 6 months; -20°C, 1 month (protect from light)

Publications (6)

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Journal Impact Factor

Talanta

Direct investigations of the effects of nicardipine on calcium channels of astrocytes by Atomic Force Microscopy. [Abstract]

2024 Jul 1:274:125947. PMID: 38537353
Biosci Rep

CaMKII/proteasome/cytosolic calcium/cathepsin B axis was present in tryspin activation induced by nicardipine. [Abstract]

2019 Jul 2;39(7):BSR20190516. PMID: 31221819
J Dig Dis

DREADDs-Based Chemogenetics Induced Slow Transit Constipation via Inhibition of Enteric Neurons. [Abstract]

2025 Apr 14. PMID: 40223443
J Chromatogr Sci

Method Development and Validation of Liquid Chromatography Tandem Mass Spectrometry for SLP-1A6 in Rat Plasma. [Abstract]

2026 Feb 13;64(3):bmag004. PMID: 41686531
Int J Clin Exp Med

2019;12(5):5184-5190.
Research Square Preprint

2023 Jul 21.

Lösungsmittel & Löslichkeit

In Vitro:

DMSO : 100 mg/mL (208.54 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

2.0854 mL

10.4271 mL

20.8542 mL

5 mM

0.4171 mL

2.0854 mL

4.1708 mL

10 mM

0.2085 mL

1.0427 mL

2.0854 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 (protect from light). 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 (5.21 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.

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 (280 KB)
SDS (393 KB)
- English - EN (393 KB)
- Français - FR (393 KB)
- Deutsch - DE (393 KB)
- Norwegian - NO (393 KB)
- Español - ES (393 KB)
- Swedish - SV (393 KB)
- Italian - IT (393 KB)
- Korean - KR (393 KB)
- Portuguese - PT (393 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]. Charnet P, et al. Electrophysiological analysis of the action of nifedipine and nicardipine on myocardial fibers. Fundam Clin Pharmacol. 1987;1(6):413-31. [Content Brief]

[2]. R Stamatiou, et al. The dihydropyridine calcium antagonist nicardipine reduces aortic smooth muscle cell viability, proliferation and migration. Cardiovascular Research, 2018 Apr,114(1):S43.

[3]. Sherrin H. Baky. Nic ardipine Hydrochloride.

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

Optional Solvent	Concentration Solvent Mass	1 mg	5 mg	10 mg	25 mg
DMSO	1 mM	2.0854 mL	10.4271 mL	20.8542 mL	52.1355 mL
	5 mM	0.4171 mL	2.0854 mL	4.1708 mL	10.4271 mL
	10 mM	0.2085 mL	1.0427 mL	2.0854 mL	5.2135 mL
	15 mM	0.1390 mL	0.6951 mL	1.3903 mL	3.4757 mL
	20 mM	0.1043 mL	0.5214 mL	1.0427 mL	2.6068 mL
	25 mM	0.0834 mL	0.4171 mL	0.8342 mL	2.0854 mL
	30 mM	0.0695 mL	0.3476 mL	0.6951 mL	1.7378 mL
	40 mM	0.0521 mL	0.2607 mL	0.5214 mL	1.3034 mL
	50 mM	0.0417 mL	0.2085 mL	0.4171 mL	1.0427 mL
	60 mM	0.0348 mL	0.1738 mL	0.3476 mL	0.8689 mL
	80 mM	0.0261 mL	0.1303 mL	0.2607 mL	0.6517 mL
	100 mM	0.0209 mL	0.1043 mL	0.2085 mL	0.5214 mL

Keywords

Nicardipine

6 Cited Publications

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Nicardipine

Membrane Transporter/Ion Channel Compound Library

Neuronal Signaling Compound Library

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Publications Citing Use of MedChemExpress (MCE) Nicardipine

Alle Calcium Channel Isoform-spezifische Produkte anzeigen

Biologische Aktivität

Chemical Information

Publications (6)

Lösungsmittel & Löslichkeit

Reinheit & Dokumentation

Verweise

Help & FAQs

Complete Stock Solution Preparation Table

Nicardipine

Membrane Transporter/Ion Channel Compound Library

Neuronal Signaling Compound Library

FDA-Approved Drug Library

Anti-Cancer Compound Library

Drug Repurposing Compound Library

Anti-Cardiovascular Disease Compound Library

NMPA-Approved Drug Library

Orally Active Compound Library

FDA Approved & Pharmacopeial Drug Library

Neuroprotective Compound Library

Rare Diseases Drug Library

Calcium Channel Blocker Library

FDA-Approved Anticancer Drug Library

Human Metabolite Library

Anti-Aging Natural Product Library

Off-patent Drug Library

Antihypertensive Compound Library

Membrane Protein-targeted Compound Library

Membrane Receptor-targeted Compound Library

Ion Channel Compound Library

Bioactive Compound Library Max

MCE Bioactive Compound Library

Drug Repurposing Compound Library Plus

FDA-Approved Drug Library Plus

FDA-Approved Drug Library Mini

Bioactive Compound Library

High-Throughput Bioactive Compound Library

Mass Spectrometry Human Metabolite Library

Publications Citing Use of MedChemExpress (MCE) Nicardipine

Alle Calcium Channel Isoform-spezifische Produkte anzeigen

Biologische Aktivität

Chemical Information

Publications (6)

Lösungsmittel & Löslichkeit

Reinheit & Dokumentation

Verweise

Help & FAQs

Complete Stock Solution Preparation Table

Nicardipine Related Classifications

HY-12515 Related Classifications