Lifitegrast

Research use only, not for human use.

A potent LFA-1/ICAM-1 antagonist with IC50 of 9 nM in HuT78 cells; exhibits good in vitro safety profile and low potency on CYP3A4, CYP2C9 and hERG.

A potent LFA-1/ICAM-1 antagonist with IC50 of 9 nM in HuT78 cells; exhibits good in vitro safety profile and low potency on CYP3A4, CYP2C9 and hERG; development as an ophthalmic solution for treating dry eye.Other Indication Approved(In Vitro):Lifitegrast (SAR 1118) 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. (In Vivo):Lifitegrast (SAR 1118), 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.Lifitegrast (SAR 1118) ophthalmic drops administered thrice daily deliver therapeutic levels of Lifitegrast (SAR 1118) in the retina and can alleviate the retinal complications associated with diabetes.

Lifitegrast (SAR 1118) 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.

Lifitegrast (SAR 1118), 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.Lifitegrast (SAR 1118) ophthalmic drops administered thrice daily deliver therapeutic levels of Lifitegrast (SAR 1118) in the retina and can alleviate the retinal complications associated with diabetes.

SAR1118 | SAR 1118 | SAR-1118

Cell Cycle/DNA Damage

Integrin

LFA-1

Other Indications

Other Disease

1025967-78-5

615.4811

C29H24Cl2N2O7S

>98% (HPLC)

DMSO: ≥ 29 mg/mL

O=C(O)[C@@H](NC(C1=C(Cl)C2=C(CN(C(C3=CC=C4C=COC4=C3)=O)CC2)C=C1Cl)=O)CC5=CC=CC(S(=O)(C)=O)=C5

L-Phenylalanine, N-[[2-(6-benzofuranylcarbonyl)-5,7-dichloro-1,2,3,4-tetrahydro-6-isoquinolinyl]carbonyl]-3-(methylsulfonyl)-

(-20℃)

With Ice Pack

≥ 2 years