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Nicardipine

Name: Nicardipine
Brand: TargetMol
SKU: T21454
Price: 29 USD
Availability: InStock
Rating: 5 (10 reviews)

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Catalog No. T21454Cas No. 55985-32-5

Alias Flusemide, Dagan, Cardene, Antagonil

Nicardipine (Cardene), a calcium channel blockers belonging to the dihydropyridine class, is a drug used to treat angina and high blood pressure.

Nicardipine

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Purity: 99.56%

Catalog No. T21454Alias Flusemide, Dagan, Cardene, AntagonilCas No. 55985-32-5

Nicardipine (Cardene), a calcium channel blockers belonging to the dihydropyridine class, is a drug used to treat angina and high blood pressure.

Pack Size	Price	USA Warehouse	Global Warehouse	Quantity
100 mg	$29	In Stock	In Stock
1 mL x 10 mM (in DMSO)	$29	In Stock	In Stock

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In Stock Estimated shipping dateUSA Warehouse[1-2 days] Global Warehouse[5-7 days]

All TargetMol products are for research purposes only and cannot be used for human consumption. We do not provide products or services to individuals. Please comply with the intended use and do not use TargetMol products for any other purpose.

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Batch Information

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Purity:99.56%

Appearance:Solid

Color:White

Resource Download

COA HPLC LCMS HNMR

Product Introduction

Nicardipine AI Summary

Nicardipine exhibits a wide range of bioactivities and pharmacokinetic properties making it a compound of significant interest in various therapeutic areas. Pharmacokinetic studies in dogs show that Nicardipine has a plasma clearance of 37.0 mL.min^-1.kg^-1, a volume of distribution of 3.5 L.kg^-1, and a plasma half-life of 17.0 hours. It has a high oral bioavailability in humans at 49.0% and demonstrates varied clearance rates across species with the fastest clearance observed in rats and the slowest in humans. Electrophysiological studies indicate its impact on the atrio-His bundle interval in rabbit hearts with an EC30 of 5.2 M. It also affects vascular resistance and atrioventricular conduction in dogs, and inhibits high-potassium depolarization-induced contracture in isolated rat aorta with an IC50 of 1400.0 nM. Nicardipine shows significant enzyme inhibition properties; it inhibits beta-lactamase, chymotrypsinogen, and malate dehydrogenase (MDH) with IC50 values of 20000.0 nM, 175000.0 nM, and 50000.0 nM, respectively. It also inhibits human cytochrome P450 2C9 with a Ki value of 280.0 nM and demonstrates moderate inhibition of other cytochrome P450 enzymes. Inhibition of human liver transporters such as BSEP and MRP4 is notable with IC50 values of 7900.0 nM and 88000.0 nM, respectively. The compound has bioactivity related to adenosine receptors, showing moderate to good affinity for A1, A2A, and A3 receptors. In various models, it demonstrates strong potential for cardiovascular, smooth muscle-related applications, and calcium channel blocking properties. It also exhibits P-glycoprotein inhibitory activity, significant repurposing potential for viral infections such as SARS-CoV-2 and antileishmanial and antitrypanosomal activities, indicating a potential for antiparasitic application. Nicardipine demonstrates potential hepatotoxic effects including increases in liver enzymes and has undergone comprehensive profiling for liver toxicity. It shows promising antiviral, inhibitory activities against several transporters and enzymes, and binding affinity to multiple receptors, suggesting a significant scope for therapeutic applications involving complex biological pathways and diverse targets..

Note: Summary generated by AI. Data source: ChEMBL

Bioactivity

Description	Nicardipine (Cardene), a calcium channel blockers belonging to the dihydropyridine class, is a drug used to treat angina and high blood pressure.
Targets&IC50	Ca2+ channel (Cardiac):1 μM (IC50)
Synonyms	Flusemide, Dagan, Cardene, Antagonil

Chemical Properties

Molecular Weight	479.52
Formula	C₂₆H₂₉N₃O₆
Cas No.	55985-32-5
Smiles	COC(=O)C1=C(C)NC(C)=C(C1c1cccc(c1)[N+]([O-])=O)C(=O)OCCN(C)Cc1ccccc1
Relative Density.	1.230 g/cm3 (Predicted)

Storage & Solubility Information

Storage

Powder: -20°C for 3 years | In solvent: -80°C for 1 year | Shipping with blue ice/Shipping at ambient temperature.

Solubility Information

H2O: Insoluble

DMSO: 250 mg/mL (521.35 mM), Sonication is recommended.

In Vivo Formulation

10% DMSO+40% PEG300+5% Tween 80+45% Saline: 2 mg/mL (4.17 mM), Sonication is recommended.

Please add the solvents sequentially, clarifying the solution as much as possible before adding the next one. Dissolve by heating and/or sonication if necessary. Working solution is recommended to be prepared and used immediately. The formulation provided above is for reference purposes only. In vivo formulations may vary and should be modified based on specific experimental conditions.

Solution Preparation Table

DMSO

	1mg	5mg	10mg	50mg
1 mM	2.0854 mL	10.4271 mL	20.8542 mL	104.2709 mL
5 mM	0.4171 mL	2.0854 mL	4.1708 mL	20.8542 mL
10 mM	0.2085 mL	1.0427 mL	2.0854 mL	10.4271 mL
20 mM	0.1043 mL	0.5214 mL	1.0427 mL	5.2135 mL
50 mM	0.0417 mL	0.2085 mL	0.4171 mL	2.0854 mL
100 mM	0.0209 mL	0.1043 mL	0.2085 mL	1.0427 mL

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In Vivo Formulation Calculator (Clear solution)

Please enter your animal experiment information in the following box and click Calculate to obtain the stock solution preparation method and in vivo formula preparation method:

For example, if the intended dosage is 10 mg/kg for animals weighing 20 g , with a dosing volume of 100 μL per animal, TargetMol | Animal experiments

and a total of 10 animals are to be administered, using a formulation of TargetMol | reagent

10% DMSO+ 40% PEG300+ 5% Tween 80+ 45% Saline/PBS/ddH₂O , the resulting working solution concentration would be 2 mg/mL.

Stock Solution Preparation:

Dissolve 2 mg of the compound in 100 μL DMSO TargetMol | reagent to obtain a stock solution at a concentration of 20 mg/mL . If the required concentration exceeds the compound's known solubility, please contact us for technical support before proceeding.

Preparation of the In Vivo Formulation:

1) Add 100 μL of the DMSO TargetMol | reagent stock solution to 400 μL PEG300 and mix thoroughly until the solution becomes clear.

2) Add 50 μL Tween 80 and mix well until fully clarified.

3) Add 450 μL Saline,PBS or ddH₂O TargetMol | reagent and mix thoroughly until a homogeneous solution is obtained.

This example is provided solely to demonstrate the use of the In Vivo Formulation Calculator and does not constitute a recommended formulation for any specific compound. Please select an appropriate dissolution and formulation strategy based on your experimental model and route of administration.

All co-solvents required for this protocol, includingDMSO, PEG300/PEG400, Tween 80, SBE-β-CD, and Corn oil, are available for purchase on the TargetMol website.

Dose Conversion

You can also refer to dose conversion for different animals. More Dose Conversion

Tech Support

Please see Inhibitor Handling Instructions for more frequently ask questions. Topics include: how to prepare stock solutions, how to store products, and cautions on cell-based assays & animal experiments, etc