AN-2728
mRNA synthesis
In vitro transcription of capped mRNA with modified nucleotides and Poly(A) tail
Tyramide Signal Amplification (TSA)
TSA (Tyramide Signal Amplification), used for signal amplification of ISH, IHC and IC etc.
Phos Binding Reagent Acrylamide
Separation of phosphorylated and non-phosphorylated proteins without phospho-specific antibody
Cell Counting Kit-8 (CCK-8)
A convenient and sensitive way for cell proliferation assay and cytotoxicity assay
SYBR Safe DNA Gel Stain
Safe and sensitive stain for visualization of DNA or RNA in agarose or acrylamide gels.
Inhibitor Cocktails
Protect the integrity of proteins from multiple proteases and phosphatases for different applications.
AN-2728是PDE4的抑制剂,IC50值为0.49 μM[1].PDE4是一种磷酸二酯酶,在银屑病和特应性皮炎相关的慢性炎症中起重要作用[2].
AN-2728是一种含硼\抗炎及局部给药的化合物,抑制PDE4的活性和TNF-α\IL-23\IL-12及其它细胞因子的释放[2].在基于细胞的测试中,AN-2728抑制细胞因子TNF-α\IL-2\IFN-γ\IL-5和IL-10的释放,IC50值分别为0.54\0.61\0.83\2.4和5.3 μM[1].
AN-2728耐受性良好,具有很好的治疗潜力.AN-2728目前正在临床开发用于治疗牛皮癣和特应性皮炎[2].
参考文献:
[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.
Physical Appearance | A solid |
Storage | Store at -20°C |
M.Wt | 251.05 |
Cas No. | 906673-24-3 |
Formula | C14H10BNO3 |
Synonyms | AN2728;AN 2728 |
Solubility | insoluble in H2O; ≥12.55 mg/mL in DMSO; ≥94.4 mg/mL in EtOH |
Chemical Name | 4-((1-hydroxy-1,3-dihydrobenzo[c][1,2]oxaborol-5-yl)oxy)benzonitrile |
SDF | Download SDF |
Canonical SMILES | N#CC1=CC=C(OC2=CC=C3C(COB3O)=C2)C=C1 |
运输条件 | 蓝冰运输或根据您的需求运输。 |
一般建议 | 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。溶液形式一般不宜长期储存,请尽快用完。 |
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. |
质量控制和MSDS
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