Nicardipine
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.
For research use only. We do not sell to patients.
- Purity: 99.75%
- CAS No.: 55985-32-5
- Formula: C26H29N3O6
- Molecular Weight:479.52
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Storage:
4°C, protect from light
* In solvent : -80°C, 6 months; -20°C, 1 month (protect from light)
Publications Citing Use of MedChemExpress (MCE) Nicardipine
MoreAll Calcium Channel Isoforms
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Biological Activity
IC50: 1 μM (cardiac calcium channels)[1]
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Cell Line
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Type | Value | Description | References |
|---|---|---|---|---|
| CHO | EC50 |
0.5 μM
Compound: 55
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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
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[PMID: 20356305] |
| HEK293 | IC50 |
0.25 μM
Compound: Nicardipine
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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
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[PMID: 22761000] |
| LLC-MK2 | IC50 |
10.59 μM
Compound: Nicardipine
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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
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[PMID: 20934347] |
| LLC-MK2 | IC50 |
71.59 μM
Compound: Nicardipine
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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
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[PMID: 20934347] |
| LLC-PK1 | IC50 |
17.5 μM
Compound: Nicardipine
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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
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[PMID: 11145223] |
| LLC-PK1 | IC50 |
4.54 μM
Compound: Nicardipine
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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
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[PMID: 12128170] |
| LLC-PK1 | IC50 |
2.3 μM
Compound: Nicardipine
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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
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[PMID: 12699389] |
| LLC-PK1 | IC50 |
2.3 μM
Compound: Nicardipine
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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
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[PMID: 12699389] |
| LLC-PK1 | IC50 |
2.5 μM
Compound: Nicardipine
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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
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[PMID: 12699389] |
| LLC-PK1 | IC50 |
2.5 μM
Compound: Nicardipine
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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
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[PMID: 12699389] |
| LLC-PK1 | IC50 |
8 μM
Compound: Nicardipine
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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
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[PMID: 12699389] |
| LLC-PK1 | IC50 |
8 μM
Compound: Nicardipine
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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
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[PMID: 12699389] |
| NIH-3T3-G185 | IC50 |
>25.8 μM
Compound: Nicardipine
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TP_TRANSPORTER: inhibition of Rhodamine 123 efflux in NIH-3T3-G185 cells
TP_TRANSPORTER: inhibition of Rhodamine 123 efflux in NIH-3T3-G185 cells
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[PMID: 11716514] |
| NIH-3T3-G185 | IC50 |
11.7 μM
Compound: Nicardipine
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TP_TRANSPORTER: inhibition of Tetramethylrosamine efflux in NIH-3T3-G185 cells
TP_TRANSPORTER: inhibition of Tetramethylrosamine efflux in NIH-3T3-G185 cells
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[PMID: 11716514] |
| NIH-3T3-G185 | IC50 |
14.6 μM
Compound: Nicardipine
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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
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[PMID: 11716514] |
| NIH-3T3-G185 | IC50 |
3.2 μM
Compound: Nicardipine
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TP_TRANSPORTER: inhibition of Daunorubicin efflux in NIH-3T3-G185 cells
TP_TRANSPORTER: inhibition of Daunorubicin efflux in NIH-3T3-G185 cells
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[PMID: 11716514] |
| NIH-3T3-G185 | IC50 |
5.6 μM
Compound: Nicardipine
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TP_TRANSPORTER: inhibition of LDS-751 efflux in NIH-3T3-G185 cells
TP_TRANSPORTER: inhibition of LDS-751 efflux in NIH-3T3-G185 cells
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[PMID: 11716514] |
| NIH-3T3-G185 | IC50 |
6.6 μM
Compound: Nicardipine
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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
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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] |
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.
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Cell Line:VSMCs were isolated from New Zealand rabbit aortic preparations
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Concentration:0.1 μM, 1 μM, 3 μM, 10 μM
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Incubation Time:24-48 hours
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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.
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.
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Animal Model:In conscious normotensive rats (NR)[3]
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Dosage:0.3-10 mg/kg
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Administration:P.o.
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Result:Induced a dose-dependent hypotensive response (maximal decrease in mean blood pressure, supine position) without any postural hypotensive response.
| NCT Number | Sponsor | Condition | Start Date |
Phase
|
|---|---|---|---|---|
| NCT01329991 | Plexxikon| | 2011-05 | PHASE1 |
Chemical Information
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CAS No. 55985-32-5
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Appearance Solid
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Molecular Weight 479.52
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Formula C26H29N3O6
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Color Light yellow to yellow
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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
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Synonyms
YC-93 free base
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Shipping
Room temperature in continental US; may vary elsewhere.
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Storage
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
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Most Recent
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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 -
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Solvent & Solubility
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)
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.
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.
Concentration (start) × Volume (start) = Concentration (final) × Volume (final)
Select the appropriate dissolution method based on your experimental animal and administration route.
- 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.
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.
Preparation of Saline: Dissolve 0.9 g sodium chloride in ddH₂O and dilute to 100 mL to obtain a clear Saline solution.
Please enter the basic information of animal experiments:
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Recommended: Prepare an additional quantity of animals to account for potential losses during experiments.
Please enter your animal formula composition:
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%DMSO +
Recommended: Keep the proportion of DMSO in working solution below 2% if your animal is weak.
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%+
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+%Tween-80 + +
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%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
Method for preparing stock solution: mg drug dissolved in μL DMSO. Stock solution concentration: mg/mL. * In solvent : -80°C, 6 months; -20°C, 1 month (protect from light)
1. Take μL DMSO stock solution;
2. Add μL .
μL , mix evenly;
3. Then add μL Tween 80, mix evenly;
4. Then add μL
Please ensure that the stock solution in the first step is dissolved to a clear state, and add co-solvents in sequence. You can use ultrasonic heating (ultrasonic cleaner, recommended frequency 20-40 kHz), vortexing, etc. to assist dissolution.
Purity & Documentation
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Data Sheet (280 KB)
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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)
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Handling Instructions (2659 KB)
References
Complete Stock Solution Preparation Table
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.
| 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 |