| CAS NO: | 280749-17-9 |
| 包装 | 价格(元) |
| 10mg | 电议 |
| 50mg | 电议 |
| Physical Appearance | Yellow solid |
| Storage | Store at RT |
| M.Wt | 453.55 |
| Cas No. | 280749-17-9 |
| Formula | C24H27N3O4S |
| Solubility | <45.35mg/ml in DMSO;<22.68mg/ml in ethanol |
| Chemical Name | (E)-1-(4-acetylpiperazin-1-yl)-3-[3-nitro-4-(2-propan-2-ylphenyl)sulfanylphenyl]prop-2-en-1-one |
| Canonical SMILES | CC(C)C1=CC=CC=C1SC2=C(C=C(C=C2)C=CC(=O)N3CCN(CC3)C(=O)C)[N+](=O)[O-] |
| 运输条件 | 蓝冰运输或根据您的需求运输。 |
| 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。溶液形式一般不宜长期储存，请尽快用完。 |
A 286982是LFA-1/ICAM-1结合及LFA-1的选择性抑制剂,IC50值分别为44 nM和35 nM [1].
淋巴细胞功能相关抗原-1(LFA-1)是白细胞整合素家族的一员,参与T细胞与抗原呈递细胞的结合.胞内粘附分子-1(ICAM-1)是胞内粘附分子的一种类型,在细胞与细胞相互作用中起重要作用.LFA-1/ICAM-1相互作用在炎症疾病的发病机制中发挥重要作用[2].
A 286982是高效的LFA-1/ICAM-1抑制剂,在化合物2B的结合中发挥不同作用.在LFA-1/ICAM-1结合实验和LFA-1介导的细胞粘附实验中,A 286982处理28小时能够抑制LFA-1/ICAM-1相互作用[1].LFA-1/ICAM-1 ELISA实验表明,A 286982通过降低二者配体亲和力与结合能力,从而抑制ICAM-1结合LFA-1 [3].
参考文献：
[1]. Liu, G., et al., Discovery of novel p-arylthio cinnamides as antagonists of leukocyte functionassociated antigen-1/intracellular adhesion molecule-1 interaction. 1. Identification of an additional binding pocket based on an anilino diaryl sulfide lead. J Med Chem, 2000. 43(21): p. 4025-40.
[2]. Katakai, T., K. Habiro, and T. Kinashi, Dendritic cells regulate high-speed interstitial T cell migration in the lymph node via LFA-1/ICAM-1. J Immunol, 2013. 191(3): p. 1188-99.
[3]. Keating, S.M., et al., Competition between intercellular adhesion molecule-1 and a smallmolecule antagonist for a common binding site on the alphal subunit of lymphocyte functionassociated antigen-1. Protein Sci, 2006. 15(2): p. 290-303.
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