BMS-587101_product_DataBase

Bioactivity

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].

Invitro

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 Vivo

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].

Name

BMS-587101

CAS

509083-77-6

Formula

C26H20Cl2N4O4S

Molar Mass

555.43

Appearance

Solid

Transport

Room temperature in continental US; may vary elsewhere.

Storage

Powder	-20°C	3 years
	4°C	2 years
In solvent	-80°C	6 months
	-20°C	1 month

Reference

[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 a [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.

PeptideDB

BMS-587101

CAS: 509083-77-6 F: C26H20Cl2N4O4S W: 555.43