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BMS-587101
本产品不向个人销售,仅用作科学研究,不用于任何人体实验及非科研性质的动物实验。
BMS-587101图片
CAS NO:509083-77-6
包装与价格:
包装价格(元)
5mg电议
10mg电议

产品介绍
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。
Cas No.509083-77-6
分子式C26H20Cl2N4O4S
分子量555.43
溶解度DMSO : 260 mg/mL (468.11 mM; Need ultrasonic)
储存条件Store at -20°C
General tipsFor obtaining a higher solubility , please warm the tube at 37 ℃ and shake it in the ultrasonic bath for a while.
Shipping ConditionEvaluation sample solution : ship with blue ice
All other available size: ship with RT , or blue ice upon request
产品描述

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.