Home Cytoskeletal Signaling Integrin antagonist Lifitegrast For research use only.

Lifitegrast

Synonyms: SAR1118,SHP-606

Lifitegrast (SAR1118,SHP-606) is a novel small molecule integrin antagonist that inhibits a specific T cell-mediated inflammatory pathway involved in the pathogenesis of DED.

Lifitegrast Chemical Structure

Lifitegrast Chemical Structure

CAS No. 1025967-78-5

Purity & Quality Control

Lifitegrast Related Products

Signaling Pathway

Integrin Signaling Pathways

Integrin Signaling Pathway

Cell Data

Cell Lines Assay Type Concentration Incubation Time Formulation Activity Description PMID
Jurkat Function assay 1 hr Inhibition of human recombinant ICAM-1 adhesion into human Jurkat cells after 1 hr, IC50=0.00298μM 24900456
HuT-78 Function assay 1 hr Antagonist activity at LFA-1/ICAM-1 in human HuT-78 T-cells assessed as inhibition of cell adhesion after 1 hr by p-nitrophenyl n-acetyl-beta-D-glucosaminide method, IC50=0.009μM 24900456
HuT-78 Function assay 1 hr Antagonist activity at LFA-1/ICAM-1 in human HuT-78 T-cells assessed as inhibition of cell adhesion after 1 hr by p-nitrophenyl n-acetyl-beta-D-glucosaminide method in presence of 10% human serum, IC50=0.074μM 24900456
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Biological Activity

Description Lifitegrast (SAR1118,SHP-606) is a novel small molecule integrin antagonist that inhibits a specific T cell-mediated inflammatory pathway involved in the pathogenesis of DED.
Targets
Integrin [1]
In vitro
In vitro

Lifitegrast inhibits release of cytokines, interferon d, tumor necrosis factor alpha (TNF-α), and other interleukins (ILs). It is a novel integrin antagonist which prevents LFA-1/ICAM-1 interaction preventing T-cell activation/recruitment and release of inflammatory mediators, thereby decreasing the inflammatory responses in DED[1].
In Vivo
In vivo

In vivo study of lifitegrast as radiolabeled drops in rats demonstrated that it was rapidly distributed in ocular and periocular tissues, cleared by normal tear drainage, and was devoid of systemic side effects. A similar dose tolerability study of lifitegrast in dogs suffering from keratoconjunctivitis sicca proved its efficacy and safety. Lifitegrast is found to be a highly potent drug in various clinical trials as it alleviates both the signs and symptoms of DED, which showed rapid onset of action and good therapeutic efficacy as ophthalmic drops. It protected the corneal surfaces and was well tolerated locally as well as systemically[1].
NCT Number Recruitment Conditions Sponsor/Collaborators Start Date Phases
NCT05857748 Withdrawn
Dry Eye Disease
Novartis Pharmaceuticals|Novartis
 July 31 2023 --
NCT03866629 Completed
Dry Eye
MDbackline LLC
 December 20 2018 --
NCT00936520 Terminated
Diabetic Macular Edema (DME)|Pars Plana Vitrectomy
Johns Hopkins University|SARcode Bioscience
 August 2009 Phase 1

Chemical Information & Solubility

Molecular Weight 615.48 Formula

C29H24Cl2N2O7S
CAS No. 1025967-78-5 SDF Download Lifitegrast SDF
Smiles CS(=O)(=O)C1=CC=CC(=C1)CC(C(=O)O)NC(=O)C2=C(C=C3CN(CCC3=C2Cl)C(=O)C4=CC5=C(C=C4)C=CO5)Cl
Storage (From the date of receipt)

In vitro
Batch:

DMSO : 100 mg/mL ( (162.47 mM) Moisture-absorbing DMSO reduces solubility. Please use fresh DMSO.)

Ethanol : 20 mg/mL

Water : Insoluble


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In vivo
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Tech Support

Answers to questions you may have can be found in the inhibitor handling instructions. Topics include how to prepare stock solutions, how to store inhibitors, and issues that need special attention for cell-based assays and animal experiments.

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