An inhibitor of LFA-1/ICAM-1 interaction (IC50 = 2.98 nM in Jurkat T-cells); decreases T cell-mediated inflammation; increases tear production in dogs with dry eye disease; inhibits LFA-1-dependent neutrophil recruitment to the eye in mouse models of corneal and bacterial eye inflammation

Lifitegrast – 50 mg

Brand:
Cayman
CAS:
1025967-78-5
Storage:
-20
UN-No:
Non-Hazardous - /

Lifitegrast binds to lymphocyte function-associated antigen-1 (LFA-1) on T cells and inhibits interaction with intercellular adhesion molecule-1 (ICAM-1; IC50 = 2.98 nM in Jurkat T cells), which decreases T cell-mediated inflammation.{39088} It inhibits secretion of cytokines associated with dry eye disease, including INF-γ, TNF-α, MIP-1α, IL-1α, IL-1β, IL-2, IL-4, and IL-6.{39086} In a T cell adhesion assay, lifitegrast blocks adhesion of HuT 78 cells to ICAM-1 with an IC50 value of 9 nM. It also increases tear production in dogs with idiopathic keratoconjunctivitis sicca (dry eye syndrome).{39085} Topical application of lifitegrast in mouse models of corneal and bacterial inflammation inhibits LFA-1-dependent neutrophil recruitment to the eye.{39087} Formulations containing lifitegrast are used for the treatment of dry eye disease.  

 

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Description

An inhibitor of LFA-1/ICAM-1 interaction (IC50 = 2.98 nM in Jurkat T-cells); decreases T cell-mediated inflammation; increases tear production in dogs with dry eye disease; inhibits LFA-1-dependent neutrophil recruitment to the eye in mouse models of corneal and bacterial eye inflammation,

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

Synonyms:  SAR 1118

Molecular weight: 615.5

CAS: 1025967-78-5

Purity: ≥98%

Formulation: A crystalline solid

Product Type|Biochemicals||Research Area|Immunology & Inflammation|Adaptive Immunity||Research Area|Immunology & Inflammation|Innate Immunity||Research Area|Infectious Disease|Bacterial Diseases||Research Area|Neuroscience|Ophthalmology

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