Cas No.: | 1025967-78-5 |
Chemical Name: | SAR-1118,SAR1118 |
Synonyms: | SAR-1118,SAR1118 |
SMILES: | CS(C1C=C(C[C@@H](NC(C2C(Cl)=C3C(CN(C(C4C=CC5C=COC=5C=4)=O)CC3)=CC=2Cl)=O)C(O)=O)C=CC=1)(=O)=O |
Formula: | C29H24Cl2N2O7S |
M.Wt: | 615.49 |
Sotrage: | 2 years -20°C Powder, 2 weeks 4°C in DMSO, 6 months -80°C in DMSO |
Description: | Lifitegrast is an integrin lymphocyte function-associated antigen-1 (LFA-1) antagonist; inhibits Jurkat T cell attachment to ICAM-1 with an IC50 of 2.98 nM. |
In Vivo: | 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]. |
In Vitro: | 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]. |