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AN-2728

现货
Catalog No.
A3178
PDE4抑制剂,抗炎化合物
组合的产品项目
规格价格库存 数量
10mM (in 1mL DMSO)
¥ 610.00
现货
5mg
¥ 580.00
现货
10mg
¥ 1,000.00
现货
50mg
¥ 2,280.00
现货

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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

Physical AppearanceA solid
StorageStore at -20°C
M.Wt251.05
Cas No.906673-24-3
FormulaC14H10BNO3
SynonymsAN2728;AN 2728
Solubility≥12.55 mg/mL in DMSO, ≥94.4 mg/mL in EtOH, <2.62 mg/mL in H2O
Chemical Name4-((1-hydroxy-1,3-dihydrobenzo[c][1,2]oxaborol-5-yl)oxy)benzonitrile
SDFDownload SDF
Canonical SMILESN#CC1=CC=C(OC2=CC=C3C(COB3O)=C2)C=C1
运输条件试用装:蓝冰运输。 其他可选规格:常温运输或根据您的要求用蓝冰运输。
一般建议为了使其更好的溶解,请用37℃加热试管并在超声波水浴中震动片刻。不同厂家不同批次产品溶解度各有差异,仅做参考。若实验所需浓度过大至产品溶解极限,请添加助溶剂助溶或自行调整浓度。

试验操作

细胞实验 [1]:

细胞系

外周血单核细胞(PBMCs)

溶解方法

该化合物在DMSO中的溶解度大于12.6 mg/mL。若获取更高浓度的溶液,可在37℃下孵育10分钟,随后在超声波浴中摇匀。-20℃以下可储存数月。

反应条件

10 μM

应用

AN-2728广泛抑制细胞因子释放,如TNF-α、IL-23、IL-12等细胞因子。

动物实验 [1]:

动物模型

佛波酯诱导小鼠耳水肿模型

给药剂量

1 mg/ear×2

应用

在佛波酯诱导的小鼠耳水肿模型中,局部应用AN-2728具有体内功效。AN-2728显著抑制耳朵水肿。

注意事项

由于实验环境的不同,实际溶解度可能与理论值略有不同,请测试室内所有化合物的溶解度。

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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