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.
AN-2728
| 规格 | 价格 | 库存 | 数量 | 操作 |
|---|---|---|---|---|
| 1mg | ¥98.00 | 现货 | 1 | |
| 5mg | ¥197.00 | 现货 | 1 | |
| 10mg | ¥315.00 | 现货 | 1 | |
| 50mg | ¥490.00 | 现货 | 1 | |
| 100mg | ¥665.00 | 现货 | 1 | |
| 10mM (in 1mL DMSO) | ¥350.00 | 现货 | 1 |
文献被引
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Nature641, 529–536 (2025)
Nature628, 630–638 (2024)
Nature632, 686–694 (2024)
Nature618, 1017–1023 (2023)
Nature610, 366–372 (2022)
Cell187(9):2288-2304 (2024)
Cell183(7):1867-1883 (2020)
Science388(6745) (2025)
Science387(6739) (2025)
Science387(6734) (2025)
Cell Research35, 97–116 (2025)
Cell Research34, 683–706 (2024)
Cell Research33, 273–287 (2023)
Cell Research33, 546–561 (2023)
Cell Research33, 904–922 (2023)
Cell Research31, 1291–1307 (2021)
产品描述 Description
实验参考方法 Experimental Reference Method
| Cell experiment [1]: | |
|
Cell lines |
Peripheral blood mononuclear cells (PBMCs) |
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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]: | |
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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. |
产品文档 Product Documents
化学性质Chemical Properties
储备液的保存方式和期限：-80°C 储存时，请在 6 个月内使用，-20°C 储存时，请在 1 个月内使用。
为了提高溶解度，请将管子加热至 37°C，然后在超声波浴中震荡一段时间。