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Derenofylline

Name: Derenofylline
Brand: TargetMol
SKU: T8312
Price: 35 USD
Availability: InStock
Rating: 5 (10 reviews)

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Catalog No. T8312Cas No. 251945-92-3

Derenofylline is a selective and potent adenosine A(1) antagonist in vitro (Ki=1 nM)

Derenofylline

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Purity: 98.09%

Catalog No. T8312Cas No. 251945-92-3

Derenofylline is a selective and potent adenosine A(1) antagonist in vitro (Ki=1 nM)

Pack Size	Price	USA Warehouse	Global Warehouse
5 mg	$35	In Stock	In Stock
10 mg	$60	In Stock	In Stock
25 mg	$127	In Stock	In Stock
50 mg	$218	In Stock	In Stock
100 mg	$318	In Stock	In Stock
1 mL x 10 mM (in DMSO)	$40	In Stock	In Stock

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In Stock Estimated shipping dateUSA Warehouse[1-2 days] Global Warehouse[5-7 days]

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Purity:98.09%

Appearance:Solid

Color:White

Resource Download

COA LCMS HNMR

Product Introduction

Derenofylline AI Summary

Derenofylline exhibits broad-spectrum antiviral activity, including notable inhibition of Zika virus in human A549 cells with an IC50 of 58.6 nM. It demonstrates a dose-dependent cytotoxicity, showing low cytotoxicity at concentrations of 0.1 μM and 1 μM, but increased cytotoxicity at 10 μM and 100 μM. Against SARS-CoV-2, Derenofylline inhibits virus-induced cytotoxicity in Caco-2 cells by 6.39% at 10 μM after 48 hours, as measured by high content imaging. Furthermore, it partially inhibits the SARS-CoV-2 3CL-Pro protease with a 2.152% inhibition rate at 20 μM. The compound also shows a minor inhibitory effect on SARS-CoV-2 in VERO-6 cells with a 0.19% inhibition at 10 μM after 48 hours. In addition to its antiviral properties, Derenofylline is a potent antagonist of the human adenosine A1 receptor, displaying high binding affinity with Ki values ranging from 0.4 nM to 1.698 nM in different cell assays, and affecting forskolin-stimulated cAMP accumulation. It demonstrates a dissociation constant (Kd) of 5.46 nM, a low off-rate affinity with a rate constant (K) of 0.0034 /s, and high on-rate affinity with a rate constant (K) of 6.27 x 10^5 M/s. The compound also demonstrates mixed inhibition of human histone deacetylase 6 (HDAC6), showing -31.91% inhibition in an enzymatic assay using a commercial peptide substrate and 2.15% inhibition with a custom peptide substrate. This multifaceted bioactivity suggests potential therapeutic applications in viral infections and modulation of adenosine A1 receptor-related pathways..

Note: Summary generated by AI. Data source: ChEMBL

Bioactivity

Description	Derenofylline is a selective and potent adenosine A(1) antagonist in vitro (Ki=1 nM)
Targets&IC50	A1 receptor:1 nM(Ki), A2A receptor:398 nM (Ki), A3 receptor:200 nM (Ki)

Chemical Properties

Molecular Weight	308.38
Formula	C₁₈H₂₀N₄O
Cas No.	251945-92-3
Smiles	O[C@H]1CC[C@@H](CC1)Nc1nc(nc2[nH]ccc12)-c1ccccc1
Relative Density.	1.37 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: 22.5 mg/mL (72.96 mM), Sonication is recommended.

In Vivo Formulation

10% DMSO+40% PEG300+5% Tween 80+45% Saline: 5 mg/mL (16.21 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	3.2428 mL	16.2138 mL	32.4275 mL	162.1376 mL
5 mM	0.6486 mL	3.2428 mL	6.4855 mL	32.4275 mL
10 mM	0.3243 mL	1.6214 mL	3.2428 mL	16.2138 mL
20 mM	0.1621 mL	0.8107 mL	1.6214 mL	8.1069 mL
50 mM	0.0649 mL	0.3243 mL	0.6486 mL	3.2428 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