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Crisaborole

Name: Crisaborole
Brand: TargetMol
SKU: T4285
Price: 38 USD
Availability: InStock
Rating: 5 (10 reviews)

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Catalog No. T4285Cas No. 906673-24-3

Alias PF-06930164, AN-2728

Crisaborole (AN-2728) is a phosphodiesterase 4 inhibitor.

Crisaborole

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Purity: 99.70%

Catalog No. T4285Alias PF-06930164, AN-2728Cas No. 906673-24-3

Crisaborole (AN-2728) is a phosphodiesterase 4 inhibitor.

Pack Size	Price	USA Warehouse	Global Warehouse
10 mg	$38	In Stock	In Stock
50 mg	$50	In Stock	In Stock
100 mg	$83	In Stock	In Stock
200 mg	$111	In Stock	In Stock
1 mL x 10 mM (in DMSO)	$46	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:99.70%

Appearance:Solid

Color:White

Resource Download

COA LCMS HNMR HPLC

Product Introduction

Bioactivity

Description	Crisaborole (AN-2728) is a phosphodiesterase 4 inhibitor.
Targets&IC50	PDE4:0.49 μM
In vitro	AN-2728 inhibits PDE isozymes PDE1A3, PDE3Cat , PDE4Cat and PDE7A1 with IC50 values of 6.1, 6.4, 0.11 and 0.73 μM. AN-2728 inhibits PDE4, TNF-α, IL-2, IFN-γ, IL-5 and IL-10 with IC50 values of 0.49, 0.54, 0.61, 0.83, 2.4 and 5.3 μM. AN-2728 shows the most potent activity against PDE4 catalytic domain, but it also shows inhibition against PDE1A3, PDE3Cat, and PDE7A1. Crystallography reveals that interaction of benzoxaboroles with the hydrophobic pocket in the PDE4 catalytic domain increase their affinity for PDE4. These benzoxaboroles strongly suppresses the secretion of cytokines associated with Ps and AD.
In vivo	AN-2728 is well tolerated and significantly impacts efficacy markers, showing comparable results to positive controls in clinical trials. It effectively inhibits ear edema induced by phorbol ester with a dosing of 1 mg/ear×2 (78% and 68%, respectively), mirroring the efficacy of dexamethasone. This suggests AN-2728 possesses notable anti-inflammatory properties and skin penetration capabilities.
Synonyms	PF-06930164, AN-2728

Chemical Properties

Molecular Weight	251.05
Formula	C₁₄H₁₀BNO₃
Cas No.	906673-24-3
Smiles	OB1OCc2cc(Oc3ccc(cc3)C#N)ccc12
Relative Density.	1.33 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: 250 mg/mL (995.82 mM), Sonication is recommended.

In Vivo Formulation

10% DMSO+40% PEG300+5% Tween 80+45% Saline: 2 mg/mL (7.97 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	3.9833 mL	19.9164 mL	39.8327 mL	199.1635 mL
5 mM	0.7967 mL	3.9833 mL	7.9665 mL	39.8327 mL
10 mM	0.3983 mL	1.9916 mL	3.9833 mL	19.9164 mL
20 mM	0.1992 mL	0.9958 mL	1.9916 mL	9.9582 mL
50 mM	0.0797 mL	0.3983 mL	0.7967 mL	3.9833 mL
100 mM	0.0398 mL	0.1992 mL	0.3983 mL	1.9916 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