LifitegRast 是一种整合素淋巴细胞功能相关抗原 1 拮抗剂, 抑制 Jurkat T 细胞附着于ICAM-1的IC50为 2.98 nM。
产品描述
Lifitegrast is a lymphocyte, function-associated antigen-1 antagonist.
体外活性
Lifitegrast is a novel small molecule integrin antagonist that inhibits T cell-mediated inflammation by blocking the binding of two important cell surface proteins (lymphocyte function-associated antigen 1 and intercellular adhesion molecule 1), thus lessening overall inflammatory responses. Lifitegrast strongly inhibits Jurkat T cell attachment to ICAM-1 with an IC50 of 2.98 nM[1].
体内活性
Lifitegrast, has potent anti-inflammatory activity on corneal inflammation induced by antibiotic-killed P. aeruginosa and S. aureus in the presence of a silicone hydrogel lens with the optimal application being a 1% solution applied either 2 or 3 times prior. Topical application of lifitegrast to the corneal surface of healthy adults is safe and well tolerated[2]. SAR 1118 ophthalmic drops administered thrice daily deliver therapeutic levels of SAR 1118 in the retina and can alleviate the retinal complications associated with diabetes[3].
Cas No.
1025967-78-5
分子式
C29H24Cl2N2O7S
分子量
615.48
别名
利非司特;SAR 1118;立他司特;SHP-606
储存和溶解度
DMSO:29 mg/mL
Powder: -20°C for 3 years
In solvent: -80°C for 2 years