Lifitegrast

Lifitegrast is an inhibitor of the protein-protein interaction between lymphocyte function-associated antigen-1 (LFA-1) and intercellular adhesion molecule-1 (ICAM-1). It binds to LFA-1 and blocks the adhesion of Jurkat T cells or HuT 78 cells to ICAM-1 (IC50s = 2.98 and 9 nM, respectively) and inhibits the secretion of various cytokines, including IFN-gamma, TNF-alpha, IL-1beta, and IL-6, from these cells. Lifitegrast increases tear production in dogs with idiopathic keratoconjunctivitis sicca. Topical application of lifitegrast inhibits LFA-1-dependent neutrophil recruitment to the eye in mouse models of contact lens-associated corneal inflammation induced by corneal abrasion and tobramycin-killed bacteria. Formulations containing lifitegrast have been used in the treatment of dry eye disease.Formal Name: N-[[2-(6-benzofuranylcarbonyl)-5,7-dichloro-1,2,3,4-tetrahydro-6-isoquinolinyl]carbonyl]-3-(methylsulfonyl)-L-phenylalanine. CAS Number: 1025967-78-5. Synonyms: SAR 1118. Molecular Formula: C29H24Cl2N2O7S. Formula Weight: 615.5. Purity: >98%. Formulation: (Request formulation change), A crystalline solid. Solubility: DMF: 30 mg/ml, DMSO: 30 mg/ml, DMSO:PBS(pH 7.2) (1:4): 0.2 mg/ml. lambdamax: 260 nm. SMILES: CS(C1=CC=CC(C[C@@H](C(O)=O)NC(C2=C(Cl)C=C(CN(C(C3=CC(OC=C4)=C4C=C3)=O)CC5)C5=C2Cl)=O)=C1)(=O)=O. InChi Code: InChI=1S/C29H24Cl2N2O7S/c1-41(38,39)20-4-2-3-16(11-20)12-23(29(36)37)32-27(34)25-22(30)13-19-15-33(9-7-21(19)26(25)31)28(35)18-6-5-17-8-10-40-24(17)14-18/h2-6,8,10-11,13-14,23H,7,9,12,15H2,1H3,(H,32,34)(H,36,37)/t23-/m0/s1. InChi Key: JFOZKMSJYSPYLN-QHCPKHFHSA-N.