Lifitegrast sodium

Names

[ CAS No. ]:
1119276-80-0

[ Name ]:
Lifitegrast sodium

[Synonym ]:
Lifitegrast sodium
UNII-QG18FLP1KP
SAR-1118-023

Biological Activity

[Description]:

Lifitegrast (SAR 1118) sodium is a potent integrin antagonist. Lifitegrast sodium blocks the binding of intercellular adhesion molecule 1 (ICAM-1) to lymphocyte function-associated antigen 1 (LFA-1), interrupting the T cell-mediated inflammatory cycle. Lifitegrast sodium inhibits Jurkat T cell attachment to ICAM-1 with an IC50 of 2.98 nM. Lifitegrast sodium can be used for researching dry eye disease[1].

[Related Catalog]:

Research Areas >> Inflammation/Immunology

Signaling Pathways >> Cytoskeleton >> Integrin

[Target]

αLβ2

[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[1]. Lifitegrast strongly inhibits Jurkat T cell attachment to ICAM-1 with an IC50 of 2.98 nM[1].

[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[2].

[References]

[1]. Perez VL, et al. Lifitegrast, a Novel Integrin Antagonist for Treatment of Dry Eye Disease. Ocul Surf. 2016 Apr;14(2):207-15.

[2]. Sun Y, et al. Corneal inflammation is inhibited by the LFA-1 antagonist, lifitegrast (SAR 1118). J Ocul Pharmacol Ther. 2013 May;29(4):395-402.

[3]. Rao VR, et al. Delivery of SAR 1118 to the retina via ophthalmic drops and its effectiveness in a rat streptozotocin(STZ) model of diabetic retinopathy (DR). Invest Ophthalmol Vis Sci. 2010 Oct;51(10):5198-204.

Chemical & Physical Properties

[ Molecular Formula ]:
C₂₉H₂₃Cl₂N₂NaO₇S

[ Molecular Weight ]:
637.46300

[ Exact Mass ]:
636.05000

[ PSA ]:
148.69000

[ LogP ]:
6.23330

Related Compounds

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