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Nitrendipine

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Catalog No. T0119Cas No. 39562-70-4
Alias Bayotensin, BAY-E-5009

Nitrendipine (BAY-E-5009) is a calcium channel blocker with marked vasodilator action. It is an effective antihypertensive agent and differs from other calcium channel blockers in that it does not reduce glomerular filtration rate and is mildly natriuretic, rather than sodium retentive.

Nitrendipine

Nitrendipine

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🥰Excellent
Purity: 99.55%
Catalog No. T0119Alias Bayotensin, BAY-E-5009Cas No. 39562-70-4
Nitrendipine (BAY-E-5009) is a calcium channel blocker with marked vasodilator action. It is an effective antihypertensive agent and differs from other calcium channel blockers in that it does not reduce glomerular filtration rate and is mildly natriuretic, rather than sodium retentive.
Pack SizePriceUSA WarehouseGlobal WarehouseQuantity
10 mg$32In StockIn Stock
25 mg$50In StockIn Stock
50 mg$65In StockIn Stock
100 mg$122In StockIn Stock
200 mg$185In StockIn Stock
500 mg$297In StockIn Stock
1 g$459In StockIn Stock
1 mL x 10 mM (in DMSO)$50In StockIn 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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Purity:99.55%
Appearance:Solid
Color:White
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Product Introduction

Nitrendipine AI Summary
Nitrendipine exhibits a wide range of bioactivities across multiple biological systems and potential therapeutic areas. It demonstrates significant inhibitory effects on calcium channels, particularly the L-type calcium channels with extremely low IC50 values (as low as 0.35 nM). This suggests potent activity as a calcium channel blocker, which translates to potential vasorelaxant properties in vascular tissues, evidenced by a reported IC50 of 1.0 nM in rabbit thoracic aorta and EC50 of 30.0 nM in rat endothelium-denuded thoracic aortic rings. Additionally, Nitrendipine shows significant antihypertensive effects in SHR rats, reducing both systolic and diastolic blood pressure. In hepatic metabolism, Nitrendipine inhibits cytochrome P-450 enzymes, with substantial inhibition rates reported, such as 83.0% inhibition on human liver microsomes. This suggests potential interactions affecting drug metabolism. The compound also exhibits notable partition characteristics (CLogP of 3.16 and logD of 0.97), indicating moderate lipophilicity and ability to permeate cellular membranes, though it has low permeability across Caco-2 cells. While Nitrendipine effectively inhibits sodium channels and shows an antifungal effect, it also exhibits moderate to weak activity against adenosine receptors and displays diverse bioactivity against Plasmodium falciparum, suggesting antimalarial potential. The compound shows a broad range of inhibitory effects on other targets, including the SARS-CoV-2 virus and various transporters and enzymes within cellular systems, highlighted by high clearance rates in hepatic metabolism and significant protein binding properties. However, observations of moderate liver toxicity and potential nephrotoxic effects highlight the need for further safety evaluations. Additionally, the compound's low oral bioavailability suggests limitations in its systemic availability when administered orally. Overall, Nitrendipine demonstrates a rich pharmacological profile with significant activities in modulating calcium channels, cytochrome P-450 enzymes, antiviral properties against SARS-CoV-2, as well as potential cardiovascular effects, meriting further investigation for therapeutic development while considering safety and bioavailability aspects..
Note: Summary generated by AI. Data source: ChEMBL
Bioactivity
Description
Nitrendipine (BAY-E-5009) is a calcium channel blocker with marked vasodilator action. It is an effective antihypertensive agent and differs from other calcium channel blockers in that it does not reduce glomerular filtration rate and is mildly natriuretic, rather than sodium retentive.
Targets&IC50
Ca2+ channel:95 nM
SynonymsBayotensin, BAY-E-5009
Chemical Properties
Molecular Weight360.36
FormulaC18H20N2O6
Cas No.39562-70-4
SmilesC(OCC)(=O)C=1C(C(C(OC)=O)=C(C)NC1C)C2=CC(N(=O)=O)=CC=C2
Relative Density.1.3595 g/cm3 (Estimated)
Storage & Solubility Information
StorageIn solvent: -80°C for 1 year | Shipping with blue ice/Shipping at ambient temperature.
Solubility Information
DMSO: 45 mg/mL (124.88 mM), Sonication is recommended.
H2O: < 1 mg/mL (insoluble or slightly soluble)
Ethanol: < 1 mg/mL (insoluble or slightly soluble)
In Vivo Formulation
10% DMSO+40% PEG300+5% Tween 80+45% Saline: 2 mg/mL (5.55 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
1mg5mg10mg50mg
1 mM2.7750 mL13.8750 mL27.7500 mL138.7501 mL
5 mM0.5550 mL2.7750 mL5.5500 mL27.7500 mL
10 mM0.2775 mL1.3875 mL2.7750 mL13.8750 mL
20 mM0.1388 mL0.6938 mL1.3875 mL6.9375 mL
50 mM0.0555 mL0.2775 mL0.5550 mL2.7750 mL
100 mM0.0278 mL0.1388 mL0.2775 mL1.3875 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:
TargetMol | Animal experiments 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 DMSOTargetMol | 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 DMSOTargetMol | reagent stock solution to 400 μL PEG300TargetMol | reagent 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 ddH2OTargetMol | 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.
1 Enter information below:
mg/kg
g
μL
2 Enter the in vivo formulation:
% DMSO
%
% Tween 80
% Saline/PBS/ddH2O

Dose Conversion

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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

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