BMS-587101 是一种有效的具有口服活性的 leukocyte function associated antigen-1 (LFA-1) 拮抗剂。BMS-587101 具有抗炎作用，可用于类风湿关节炎的研究。
货号:ajcx34578
CAS:509083-77-6
分子式:C26H20Cl2N4O4S
分子量：555.43
溶解度:DMSO : 260 mg/mL (468.11 mM; Need ultrasonic)
纯度：98%
存储：Store at -20°C
库存：现货

Background:

BMS-587101 is a potent and orally active antagonist of leukocyte function associated antigen-1 (LFA-1). BMS-587101 has anti-inflammatory effects and can be used for rheumatoid arthritis research[1][2].

BMS-587101 is a moderately potent inhibitor of LFA-1-mediated T-cell proliferation, with an IC50 of 20 nM in human HUVEC cells. BMS-587101 inhibits LFA-1-mediated adhesion of T cells to endothelial cells, T cell proliferation, and Th1 cytokine production[1][2]. In mouse splenocytes and a mouse ICAM-1 expressing cell lines, bEND, BMS-587101 shows inhibitory activities, with an IC50 of 150 nM[1].

In the mouse ovalbumin-induced lung inflammation model, BMS-587101 (0.1 mg/kg, 1.0 mg/kg, and 10 mg/kg; po.; twice a day) treatment significantly inhibits eosinophil accumulation[1].

[1]. Dominique Potin, et al. Discovery and development of 5-[(5S,9R)-9-(4-cyanophenyl)-3-(3,5-dichlorophenyl)-1-methyl-2,4-dioxo-1,3,7-triazaspiro[4.4]non-7-yl-methyl]-3-thiophenecarboxylic acid (BMS-587101)--a small molecule antagonist of leukocyte function associated antigen-1. J Med Chem. 2006 Nov 30;49(24):6946-9.
[2]. Suzanne J Suchard, et al. An LFA-1 (alphaLbeta2) small-molecule antagonist reduces inflammation and joint destruction in murine models of arthritis. J Immunol. 2010 Apr 1;184(7):3917-26.