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Nitrendipine [39562-70-4]

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Referentie NB-64-00260-50mg

Formaat : 50mg

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Nitrendipine

(Synonyms: Bayotensin, BAY-E-5009) Copy Product Info

Synonyms: Bayotensin, BAY-E-5009

Catalog No. T0119 Copy Product Info

Purity: 99.55%

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.

Cas No. 39562-70-4

For research use only—not for human use. No sales to individuals. Use as intended only.

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Purity:99.55%

Appearance:Solid

Color:White

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
Synonyms	Bayotensin, BAY-E-5009

Chemical Properties

Molecular Weight	360.36
Formula	C₁₈H₂₀N₂O₆
Cas No.	39562-70-4
Smiles	C(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

Storage

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

Solubility Information

DMSO: 247.5 mg/mL (686.81 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+90% Saline: < 10 mg/mL (27.75 mM), Lower concentrations may be soluble, but exact solubility limit is unknown.

10% DMSO+40% PEG300+5% Tween 80+45% Saline: 10 mg/mL (27.75 mM), Suspension.

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	2.7750 mL	13.8750 mL	27.7500 mL	138.7501 mL
5 mM	0.5550 mL	2.7750 mL	5.5500 mL	27.7500 mL
10 mM	0.2775 mL	1.3875 mL	2.7750 mL	13.8750 mL
20 mM	0.1388 mL	0.6938 mL	1.3875 mL	6.9375 mL
50 mM	0.0555 mL	0.2775 mL	0.5550 mL	2.7750 mL
100 mM	0.0278 mL	0.1388 mL	0.2775 mL	1.3875 mL

Note : The dilution table applies only to solid products. For liquid products, please calculate the stock solution based on the stated concentration and/or density.

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

Keywords

vasculatureperipheralNitrendipineInhibitorinhibithypertensiondilatorchannelCalciumChannelCalcium ChannelcalciumCa2+ channelsCa channelsBAY-E5009BAY-E 5009Autophagyantihypertensive

Related Tags: Nitrendipine chemical structure | Nitrendipine formula | Nitrendipine molecular weight

Nitrendipine [39562-70-4]

Referentie NB-64-00260-50mg

Neem contact op met een lokale distributeur :

Neem contact op met een lokale distributeur :

Nitrendipine

Product Introduction

Calculator

In Vivo Formulation Calculator (Clear solution)

Dose Conversion

Keywords

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