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Zaprinast

Name: Zaprinast
Brand: TargetMol
SKU: T2129
Price: 29 USD
Availability: InStock
Rating: 5 (10 reviews)

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Catalog No. T2129Cas No. 37762-06-4

Zaprinast is a cGMP-selective phosphodiesterase (PDE) inhibitor and a GPR35 agonist. It has a strong activating effect on rat GPR35 and a certain activating effect on human GPR35. It reduces vascular remodeling through anti-proliferative and pro-apoptotic effects.

Zaprinast

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Purity: 99.77%

Catalog No. T2129Cas No. 37762-06-4

Pack Size	Price	USA Warehouse	Global Warehouse	Quantity
5 mg	$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:99.77%

Appearance:Solid

Color:White to Red

Resource Download

COA HPLC HNMR

Product Introduction

Zaprinast AI Summary

Zaprinast is a potent phosphodiesterase inhibitor, particularly effective against PDE5 with IC50 values ranging from 200.0 nM to 3162.28 nM, depending on the assay conditions and biological source. It also inhibits other isoenzymes including PDE1, PDE2, PDE3, and PDE4 at varying potencies, showing notable selectivity and potency for PDE5. Additionally, Zaprinast has demonstrated antiplasmodial activity against Plasmodium falciparum in various strains with IC50 values in the range of 10000.0 nM to 35000.0 nM. The compound also acts as an agonist and antagonist at the GPR35 receptor in human cells, with EC50 values of 160.0 nM to 4200.0 nM. Moreover, Zaprinast has shown inhibition of the SARS-CoV-2 3CL-Pro protease and antiviral activity against SARS-CoV-2 induced cytotoxicity in VERO-6 cells at concentrations higher than 20000.0 nM. It displays inhibitory effects on multiple biological targets including leukocyte and placental alkaline phosphatase, PDE4 in human neutrophils, and contributes to the modulation of cyclic nucleotide signaling pathways. Zaprinast has diverse bioactivities making it a candidate for multiple therapeutic applications including erectile dysfunction, antimalarial treatment, and potential antiviral therapies..

Note: Summary generated by AI. Data source: ChEMBL

Bioactivity

Description

Chemical Properties

Molecular Weight	271.27
Formula	C₁₃H₁₃N₅O₂
Cas No.	37762-06-4
Smiles	CCCOc1ccccc1-c1nc2[nH]nnc2c(=O)[nH]1
Relative Density.	1.48 g/cm3 (Predicted)

Storage & Solubility Information

Storage

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

Solubility Information

DMSO: 30 mg/mL (110.59 mM), Sonication is recommended.

In Vivo Formulation

10% DMSO+40% PEG300+5% Tween 80+45% Saline: 2 mg/mL (7.37 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	3.6864 mL	18.4318 mL	36.8636 mL	184.3182 mL
5 mM	0.7373 mL	3.6864 mL	7.3727 mL	36.8636 mL
10 mM	0.3686 mL	1.8432 mL	3.6864 mL	18.4318 mL
20 mM	0.1843 mL	0.9216 mL	1.8432 mL	9.2159 mL
50 mM	0.0737 mL	0.3686 mL	0.7373 mL	3.6864 mL
100 mM	0.0369 mL	0.1843 mL	0.3686 mL	1.8432 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