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AN-2728 PDE4 inhibitor,anti-inflammatory compound

Catalog No.A3178
Size Price Stock Qty
10mM (in 1mL DMSO)
$125.00
In stock
5mg
$115.00
In stock
10mg
$150.00
In stock
50mg
$450.00
In stock

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Email: [email protected]

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Sample solution is provided at 25 µL, 10mM.

Quality Control

Chemical structure

A 77-01

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.

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Chemical Properties

Cas No. 906673-24-3 SDF Download SDF
Synonyms AN2728;AN 2728
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 >12.6mg/mL in DMSO Storage Store at -20°C
Shipping Condition Evaluation sample solution : ship with blue ice.All other available size: ship with RT , or blue ice upon request
General tips For obtaining a higher solubility , please warm the tube at 37 ℃ and shake it in the ultrasonic bath for a while.Stock solution can be stored below -20℃ for several months.

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.