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Amlodipine

Name: Amlodipine
Brand: TargetMol
SKU: T1385
Price: 30 USD
Availability: InStock
Rating: 5 (10 reviews)

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Catalog No. T1385Cas No. 88150-42-9

Alias UK-48340

Amlodipine (UK-48340) is a synthetic dihydropyridine and a calcium channel blocker with antihypertensive and antianginal properties.

Amlodipine

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Purity: 99.60%

Catalog No. T1385Alias UK-48340Cas No. 88150-42-9

Amlodipine (UK-48340) is a synthetic dihydropyridine and a calcium channel blocker with antihypertensive and antianginal properties.

Pack Size	Price	USA Warehouse	Global Warehouse
200 mg	$30	In Stock	In Stock
500 mg	$45	In Stock	In Stock
1 g	$72	In Stock	In Stock
2 g	$98	In Stock	In Stock
5 g	$169	-	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:99.60%

Appearance:Solid

Color:White

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COA HNMR LCMS

Product Introduction

Amlodipine AI Summary

Amlodipine demonstrates multifaceted pharmacological and pharmacokinetic profiles. It acts as an in vitro calcium channel antagonist, showing high potency against calcium-induced contractions in potassium-depolarized rat aorta with IC50 values from 1.995 nM to 1584.89 nM and a notable IC50 of 7.943 nM. It also induces a negative inotropic effect on Langendorff-perfused guinea pig heart with a pIC25 of 7.2 and exhibits significant bioactivity in terms of IC50 values, including binding affinities to several adrenergic receptors and the L-type calcium channel. The compound has shown bioactivities such as antihypertensive effects in spontaneously hypertensive rats with an IC50 value of 2.5 nM, and antileishmanial activities against Leishmania donovani. Pharmacokinetic evaluations in dogs reveal a plasma clearance rate of 11.0 mL.min-1.kg-1, volume of distribution at 25.0 L.kg-1, and a half-life of 30.0 hours. Human pharmacokinetics indicate a similar plasma clearance rate of 7.0 mL.min-1.kg-1, volume of distribution of 17.0 L.kg-1, and a half-life of 34.0 hours. The compound displays a high oral bioavailability of 79.0%, strong protein binding affinity of 98.09%, and a moderate lipophilicity with log P and log D values around 1.55 to 3.3. Amlodipine inhibits several key enzymes, such as the L-type calcium channel with various IC50 values, TREK-1 channel at 400.0 nM, and human BSEP at 16000.0 nM. It also demonstrates significant antiviral activity against SARS-CoV-2, with an impressive inhibition rate of 94.32% at 10 uM concentration and some inhibitory activity on the SARS-CoV-2 3CL-Pro protease. Additionally, it has shown moderate inhibition of fungal growth and bacterial activities, albeit with lower efficacy against certain pathogens. The compound has also exhibited hepatotoxicity potential, indicated by relevant liver enzyme increases in various assays. Collectively, these characteristics underscore Amlodipine’s potential for diverse therapeutic applications subject to further evaluations on safety, efficacy, and selectivity..

Note: Summary generated by AI. Data source: ChEMBL

Bioactivity

Description	Amlodipine (UK-48340) is a synthetic dihydropyridine and a calcium channel blocker with antihypertensive and antianginal properties.
In vitro	In large coronary arteries and aorta, Amlodipine increased nitrite production. Intracellularly, Amlodipine caused neuronal Ca2+ elevation by attenuating KCl depolarization.
In vivo	In large coronary arteries and aorta, Amlodipine increased nitrite production. Intracellularly, Amlodipine caused neuronal Ca2+ elevation by attenuating KCl depolarization.
Synonyms	UK-48340

Chemical Properties

Molecular Weight	408.88
Formula	C₂₀H₂₅ClN₂O₅
Cas No.	88150-42-9
Smiles	OS(=O)(=O)C1=CC=CC=C1.CCOC(=O)C1=C(COCCN)NC(C)=C(C1C1=CC=CC=C1Cl)C(=O)OC
Relative Density.	1.227 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

DMSO: 90 mg/mL (220.11 mM), Sonication is recommended.

Ethanol: 76 mg/mL (185.87 mM), Sonication is recommended.

In Vivo Formulation

10% DMSO+40% PEG300+5% Tween 80+45% Saline: 2.5 mg/mL (6.11 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

Ethanol/DMSO

	1mg	5mg	10mg	50mg
1 mM	2.4457 mL	12.2285 mL	24.4571 mL	122.2853 mL
5 mM	0.4891 mL	2.4457 mL	4.8914 mL	24.4571 mL
10 mM	0.2446 mL	1.2229 mL	2.4457 mL	12.2285 mL
20 mM	0.1223 mL	0.6114 mL	1.2229 mL	6.1143 mL
50 mM	0.0489 mL	0.2446 mL	0.4891 mL	2.4457 mL
100 mM	0.0245 mL	0.1223 mL	0.2446 mL	1.2229 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