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AN-2728 (Synonyms: Crisaborole)

Catalog No.GC11472

A selective PDE4 inhibitor

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AN-2728 Chemical Structure

Cas No.: 906673-24-3

Size Price Stock Qty
10mM (in 1mL DMSO)
$45.00
In stock
5mg
$32.00
In stock
10mg
$41.00
In stock
50mg
$63.00
In stock

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Sample solution is provided at 25 µL, 10mM.

Product Documents

Quality Control & SDS

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Protocol

Cell experiment [1]:

Cell lines

Peripheral blood mononuclear cells (PBMCs)

Preparation method

The solubility of this compound in DMSO is >12.6mg/mL. General tips for obtaining a higher concentration: Please warm the tube at 37 ℃ for 10 minutes and/or shake it in the ultrasonic bath for a while. Stock solution can be stored below -20℃ for several months.

Reacting condition

10 μM

Applications

AN-2728 showed a broad range of potent cytokine release inhibition, such as TNF-α, IL-23, IL-12 and other cytokines.

Animal experiment [2]:

Animal models

Phorbol ester-induced mouse ear edema model

Dosage form

1 mg/ear×2

Application

AN-2728 demonstrated in vivo efficacy in phorbol ester-induced mouse ear edema model by topical application. AN-2728 showed significant inhibition against the ear edema.

Other notes

Please test the solubility of all compounds indoor, and the actual solubility may slightly differ with the theoretical value. This is caused by an experimental system error and it is normal.

References:

[1]. Akama T, Baker S J, Zhang Y K, et al. Discovery and structure–activity study of a novel benzoxaborole anti-inflammatory agent (AN2728) for the potential topical treatment of psoriasis and atopic dermatitis[J]. Bioorganic & medicinal chemistry letters, 2009, 19(8): 2129-2132.

Background

AN-2728 is an inhibitor of PDE4 with IC50 value of 0.49 μM [1]. PDE4 is a phosphodiesterase and plays an important role in the chronic inflammation associated with psoriasis and atopic dermatitis [2].
AN-2728 is a boron-containing, anti-inflammatory, topically administered compound that inhibits PDE4 activity and suppresses the release of TNF-α, IL-23, IL-12 and other cytokines [2]. In cell based assays, AN-2728 inhibited cytokine release of TNF-α, IL-2, IFN-γ, IL-5 and IL-10 with IC50 values of 0.54, 0.61, 0.83, 2.4 and 5.3 μM, respectively [1].
AN-2728 was well tolerated and had good therapeutic potential. AN-2728 is now in clinical development for the treatment of psoriasis and atopic dermatitis [2].
References:
[1]. Akama T, Baker SJ, Zhang YK, et al. Discovery and structure-activity study of a novel benzoxaborole anti-inflammatory agent (AN2728) for the potential topical treatment of psoriasis and atopic dermatitis. Bioorg Med Chem Lett, 2009, 19(8): 2129-2132.
[2]. Nazarian R, Weinberg JM. AN-2728, a PDE4 inhibitor for the potential topical treatment of psoriasis and atopic dermatitis. Curr Opin Investig Drugs, 2009, 10(11): 1236-1242.

Chemical Properties

Cas No. 906673-24-3 SDF
Synonyms Crisaborole
Chemical Name 4-((1-hydroxy-1,3-dihydrobenzo[c][1,2]oxaborol-5-yl)oxy)benzonitrile
Canonical SMILES N#CC1=CC=C(OC2=CC=C3C(COB3O)=C2)C=C1
Formula C14H10BNO3 M.Wt 251.05
Solubility ≥ 12.55 mg/mL in DMSO, ≥ 94.4 mg/mL in EtOH Storage Store at -20°C
General tips Please select the appropriate solvent to prepare the stock solution according to the solubility of the product in different solvents; once the solution is prepared, please store it in separate packages to avoid product failure caused by repeated freezing and thawing.Storage method and period of the stock solution: When stored at -80°C, please use it within 6 months; when stored at -20°C, please use it within 1 month.
To increase solubility, heat the tube to 37°C and then oscillate in an ultrasonic bath for some time.
Shipping Condition Evaluation sample solution: shipped with blue ice. All other sizes available: with RT, or with Blue Ice upon request.

Complete Stock Solution Preparation Table

Prepare stock solution
1 mg 5 mg 10 mg
1 mM 3.9833 mL 19.9164 mL 39.8327 mL
5 mM 0.7967 mL 3.9833 mL 7.9665 mL
10 mM 0.3983 mL 1.9916 mL 3.9833 mL
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Method for preparing DMSO master liquid: mg drug pre-dissolved in μL DMSO ( Master liquid concentration mg/mL, Please contact us first if the concentration exceeds the DMSO solubility of the batch of drug. )

Method for preparing in vivo formulation: Take μL DMSO master liquid, next addμL PEG300, mix and clarify, next addμL Tween 80, mix and clarify, next add μL ddH2O, mix and clarify.

Method for preparing in vivo formulation: Take μL DMSO master liquid, next add μL Corn oil, mix and clarify.

Note: 1. Please make sure the liquid is clear before adding the next solvent.
2. Be sure to add the solvent(s) in order. You must ensure that the solution obtained, in the previous addition, is a clear solution before proceeding to add the next solvent. Physical methods such as vortex, ultrasound or hot water bath can be used to aid dissolving.
3. All of the above co-solvents are available for purchase on the GlpBio website.

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