Lifitegrast

Catalog No.S3714 Batch:S371403

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Technical Data

Formula

C29H24Cl2N2O7S
Molecular Weight 615.48 CAS No. 1025967-78-5
Solubility (25°C)* In vitro DMSO 100 mg/mL (162.47 mM)
Ethanol 15 mg/mL (24.37 mM)
Water Insoluble
In vivo (Add solvents to the product individually and in order)
Clear solution
5%DMSO Corn oil
0.7mg/ml Taking the 1 mL working solution as an example, add 50 μL of 14 mg/ml clear DMSO stock solution to 950 μL of corn oil and mix evenly. The mixed solution should be used immediately for optimal results. 
* <1 mg/ml means slightly soluble or insoluble.
* Please note that Selleck tests the solubility of all compounds in-house, and the actual solubility may differ slightly from published values. This is normal and is due to slight batch-to-batch variations.
* Room temperature shipping (Stability testing shows this product can be shipped without any cooling measures.)

Preparing Stock Solutions

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

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 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].

Protocol (from reference)

Selleck's Lifitegrast has been cited by 3 publications

Dihydroergotamine ameliorates liver fibrosis by targeting transforming growth factor β type II receptor [ World J Gastroenterol, 2023, 29(20):3103-3118] PubMed: 37346154
Design, synthesis, and LFA-1/ICAM-1 antagonist activity evaluation of Lifitegrast analogues [ Med Chem Res, 2022, 31(4):555-579] PubMed: 35194364
Repurposing of FDA approved drugs against Salmonella enteric serovar Typhi by targeting dihydrofolate reductase: an in silico study [ J Biomol Struct Dyn, 2020, 1-14] PubMed: 33251976

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SHIPPING AND STORAGE
Selleck products are transported at room temperature. If you receive the product at room temperature, please rest assured, the Selleck Quality Inspection Department has conducted experiments to verify that the normal temperature placement of one month will not affect the biological activity of powder products. After collecting, please store the product according to the requirements described in the datasheet. Most Selleck products are stable under the recommended conditions.

NOT FOR HUMAN, VETERINARY DIAGNOSTIC OR THERAPEUTIC USE.