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A-286982

A-286982用途

A-286982是一种有效的变构LFA-1/ICAM-1相互作用抑制剂,在LFA-1/ICAM-1结合和LFA-1介导的细胞粘附试验中,IC50分别为44 nM和35 nM[1][2]。

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A-286982名称

[ CAS 号 ]:
280749-17-9

[ 英文名 ]:
A 286982

[英文别名 ]:

unii-5i8wfs075a

A-286982生物活性

[ 描述 ]:

A-286982是一种有效的变构LFA-1/ICAM-1相互作用抑制剂,在LFA-1/ICAM-1结合和LFA-1介导的细胞粘附试验中,IC50分别为44 nM和35 nM[1][2]。

[ 相关类别 ]:

研究领域 >> 炎症/免疫

信号通路 >> 细胞骨架 >> Integrin

[ 靶点 ]

IC50: 44 nM (LFA-1/ICAM-1 interaction in an LFA-1/ICAM-1 binding assay) and 35 nM (LFA-1/ICAM-1 interaction in LFA-1-mediated cellular adhesion assay)[1]

[体外研究]

A-286982与I结构域变构位点(IDAS)结合。由于这种变构通过A-286982结合位点从β亚单位I样结构域传递到α亚单位ICAM结合位点[2],我们已经观察到A-286982的变构ICAM抑制可能会表现出不可调和的竞争。

[参考文献]

[1]. G Liu, et al. Discovery of novel p-arylthio cinnamides as antagonists of leukocyte function-associated 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 Oct 19;43(21):4025-40.

[2]. Susan M Keating, et al. Competition between intercellular adhesion molecule-1 and a small-molecule antagonist for a common binding site on the alphal subunit of lymphocyte function-associated antigen-1. Protein Sci. 2006 Feb;15(2):290-303.

A-286982物理化学性质

[ 分子式 ]:
C₂₄H₂₇N₃O₄S

[ 分子量 ]:
453.55400

[ 精确质量 ]:
453.17200

[ PSA ]:
111.74000

[ LogP ]:
4.97230

[ 外观性状 ]:
固体

[ 储存条件 ]:
-20°C

A-286982MSDS

详细MSDS(安全技术说明书)

A-286982安全信息

[ 危险品运输编码 ]:
NONH for all modes of transport