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Isradipine

Name: Isradipine
Brand: TargetMol
SKU: T0957
Price: 33 USD
Availability: InStock
Rating: 5 (10 reviews)

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Catalog No. T0957Cas No. 75695-93-1

Alias PN 200-110

Isradipine (PN 200-110) is a dihydropyridine calcium channel blocker with antihypertensive and vasodilator activities. Isradipine blocks calcium entry through calcium ion channels in coronary and peripheral vascular smooth muscle, dilating coronary arteries and peripheral arterioles. This action increases oxygen delivery by enhancing blood flow and decreases oxygen requirements by reducing total peripheral resistance.

Isradipine

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Purity: 99.95%

Catalog No. T0957Alias PN 200-110Cas No. 75695-93-1

Pack Size	Price	USA Warehouse	Global Warehouse
5 mg	$33	In Stock	In Stock
10 mg	$54	In Stock	In Stock
25 mg	$98	In Stock	In Stock
50 mg	$162	In Stock	In Stock
100 mg	$270	-	In Stock
500 mg	$668	-	In Stock
1 mL x 10 mM (in DMSO)	$50	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:99.95%

Appearance:Solid

Color:White to Yellow

Resource Download

COA LCMS HNMR

Product Introduction

Isradipine AI Summary

Isradipine exhibits a diverse range of bioactivities and pharmacokinetic properties. It demonstrates measurable MRP2-mediated estradiol-17-beta-glucuronide transport activity in Sf9 cells with 46.0% relative to the control. Pharmacokinetically, it has a total body clearance of 26.0 mL.min^-1.kg^-1 and a renal clearance of 0.0 mL.min^-1.kg^-1 in humans, indicative of non-renal elimination pathways. It shows significant antitrypanosomal activity against Trypanosoma cruzi with an IC50 of 20800.0 nM and various inhibitory actions on enzymes like Cytochrome P450 subsets, Menin-MLL interaction, and anthrax lethal toxin internalization, with IC50 values ranging from low micromolar to approximately 10 µM. Isradipine also displays antiviral properties including inhibition of Ebola virus entry and various effects on SARS-CoV-2-induced cytotoxicity. It inhibits SARS-CoV-2 3CL-Pro protease and shows activity against several other pathogens, including Naegleria gruberi, Candida albicans, and multiple bacterial strains. In terms of liver toxicity, Isradipine shows moderate liver enzyme elevations but generally low risk of severe liver injury, scoring 3.0 in the DILI severity class. Pharmacologically, it is a potent antagonist of voltage-dependent L-type calcium channels (IC50 = 2.2 nM for human channels), with a notable selectivity ratio favoring rabbit over rat channels. It exhibits moderate cytotoxicity in HepG2 cells at higher concentrations, suggesting a need for monitoring in therapeutic contexts. Isradipine shows high metabolic clearance in human liver microsomes and modest binding to plasma proteins (Fu = 0.04). It presents moderate inhibition on bile salt export pump and renal organic anion transporters (OATPs), with an IC50 of 28000.0 nM for BSEP. Overall, Isradipine is characterized by its moderate duration of action and metabolic clearance, alongside its broad spectrum of bioactivities encompassing enzyme inhibition, anti-parasitic, antiviral, and potential therapeutic roles in oncology and infection control..

Note: Summary generated by AI. Data source: ChEMBL

Bioactivity

Description	Isradipine (PN 200-110) is a dihydropyridine calcium channel blocker with antihypertensive and vasodilator activities. Isradipine blocks calcium entry through calcium ion channels in coronary and peripheral vascular smooth muscle, dilating coronary arteries and peripheral arterioles. This action increases oxygen delivery by enhancing blood flow and decreases oxygen requirements by reducing total peripheral resistance.
Targets&IC50	Ca2+ channel:34±8 μM
In vitro	In vivo oxygen uptake (I50 = 31.1 mM) and growth incubation (I50 = 20.8 mM) assays showed that Isradipine was the most effective derivative. At micromolar concentrations, Isradipine inhibited oxygen consumption and growth incubation of the short-membrane form of Trypanosoma cruzi strain Tulahuen.
In vivo	In vivo oxygen uptake (I50 = 31.1 mM) and growth incubation (I50 = 20.8 mM) assays showed that Isradipine was the most effective derivative. At micromolar concentrations, Isradipine inhibited oxygen consumption and growth incubation of the short-membrane form of Trypanosoma cruzi strain Tulahuen.
Synonyms	PN 200-110

Chemical Properties

Molecular Weight	371.39
Formula	C₁₉H₂₁N₃O₅
Cas No.	75695-93-1
Smiles	C(OC(C)C)(=O)C=1C(C(C(OC)=O)=C(C)NC1C)C=2C=3C(C=CC2)=NON3
Relative Density.	1.249 g/cm3

Storage & Solubility Information

Storage

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

Solubility Information

Ethanol: 7.4 mg/mL (19.93 mM), Sonication is recommended.

DMSO: 250 mg/mL (673.15 mM), Sonication is recommended.

In Vivo Formulation

10% DMSO+40% PEG300+5% Tween 80+45% Saline: 2 mg/mL (5.39 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	2.6926 mL	13.4629 mL	26.9259 mL	134.6294 mL
5 mM	0.5385 mL	2.6926 mL	5.3852 mL	26.9259 mL
10 mM	0.2693 mL	1.3463 mL	2.6926 mL	13.4629 mL

DMSO

	1mg	5mg	10mg	50mg
20 mM	0.1346 mL	0.6731 mL	1.3463 mL	6.7315 mL
50 mM	0.0539 mL	0.2693 mL	0.5385 mL	2.6926 mL
100 mM	0.0269 mL	0.1346 mL	0.2693 mL	1.3463 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