Lifitegrast - CAS 1025967-78-5
Catalog number: 1025967-78-5
Category: Inhibitor
Not Intended for Therapeutic Use. For research use only.
Molecular Formula:
Molecular Weight:
Lymphocyte function-associated antigen 1(LFA-1)
Lifitegrast is a Lymphocyte Function-Associated Antigen-1(LFA-1) Antagonist. It is used for the treatment of keratoconjunctivitis sicca (dry eye syndrome). It inhibits T cell-mediated inflammation by blocking the binding of two important cell surface proteins, thus lessening overall inflammatory responses. It was initially developed by SARcode Bioscience, which was acquired by Shire in 2013. It has been listed.
>98 %
Solid powder
SAR1118;L-Phenylalanine,N-[[2-(6-benzofuranylcarbonyl)-5,7-dichloro-1,2,3,4-tetrahydro-6-isoquinolinyl]carbonyl]-3-(methylsulfonyl)-;N-[[2-(6-Benzofuranylcarbonyl)-5,7-dichloro-1,2,3,4-tetrahydro-6-isoquinolinyl]carbonyl]-3-(methylsulfonyl)-L-phenylalanine;SAR-1118;(2S)-2-[[2-(1-benzofuran-6-carbonyl)-5,7-dichloro-3,4-dihydro-1H-isoquinoline-6-carbonyl]amino]-3-(3-methylsulfonylphenyl)propanoic acid;(S)-2-(2-(benzofuran-6-carbonyl)-5,7-dichloro-1,2,3,4-tetrahydroisoquinoline-6-carboxamido)-3-(3-(methylsulfonyl)phenyl)propanoic acid
10 mM in DMSO
-20°C Freezer
Lifitegrast is used for the treatment of keratoconjunctivitis sicca (dry eye syndrome).
Quality Standard:
In-house standard
Shelf Life:
2 month in rt, long time
Grams to Kilograms
Boiling Point:
811.9±65.0 °C | Condition: Press: 760 Torr
1.479±0.06 g/cm3 | Condition: Temp: 20 °C Press: 760 Torr
Canonical SMILES:
Current Developer:
Lifitegrast was initially developed by SARcode Bioscience, which was acquired by Shire in 2013. It has been listed.
1.RGN-259 (thymosin β4) improves clinically important dry eye efficacies in comparison with prescription drugs in a dry eye model.
Kim CE;Kleinman HK;Sosne G;Ousler GW;Kim K;Kang S;Yang J Sci Rep. 2018 Jul 12;8(1):10500. doi: 10.1038/s41598-018-28861-5.
This study evaluated the clinical activity of RGN-259 (thymosin β4) in comparison with cyclosporine A (CsA), diquafosol (DQS), and lifitegrast (LFA) in a murine model of dry eye. The model was NOD.B10-H2;b; mice in a 30-40% humidified environment together with daily scopolamine hydrobromide injections for 10 days. After desiccation stress, all drugs were evaluated after 10 treatment days. RGN-259 increased tear production similar to that in the DQS- and LFA-treated mice while CsA was inactive. RGN-259 improved corneal smoothness and decreased fluorescein staining similar to that of LFA group while CsA and DQS were inactive. Corneal epithelial detachment was reduced by RGN-259, and DQS and LFA showed similar activity but the CsA was inactive. RGN-259 increased conjunctival goblet cells and mucin production comparable to that seen with CsA, while DQS and LFA were inactive. RGN-259 reduced the over-expression of inflammatory factors comparable to that with CsA and LFA, while DQS was inactive. RGN-259 increased mucin production comparable to that observed with CsA, while DQS and LFA were inactive. In conclusion, RGN-259 promoted recovery of mucins and goblet cells, improved corneal integrity, and reduced inflammation in a dry eye mouse model and was equal to or more effective than prescription treatments.
2.The Pathophysiology of Dry Eye Disease: What We Know and Future Directions for Research.
Pflugfelder SC;de Paiva CS Ophthalmology. 2017 Nov;124(11S):S4-S13. doi: 10.1016/j.ophtha.2017.07.010.
Clinical and laboratory studies performed over the past few decades have discovered that dry eye is a chronic inflammatory disease that can be initiated by numerous extrinsic or intrinsic factors that promote an unstable and hyperosmolar tear film. These changes in tear composition, in some cases combined with systemic factors, lead to an inflammatory cycle that causes ocular surface epithelial disease and neural stimulation. Acute desiccation activates stress signaling pathways in the ocular surface epithelium and resident immune cells. This triggers production of innate inflammatory mediators that stimulate the production of matrix metalloprotease, inflammatory cell recruitment, and dendritic cell maturation. These mediators, combined with exposure of autoantigens, can lead to an adaptive T cell-mediated response. Cornea barrier disruption develops by protease-mediated lysis of epithelial tight junctions, leading to accelerated cell death; desquamation; an irregular, poorly lubricated cornea surface; and exposure and sensitization of epithelial nociceptors. Conjunctival goblet cell dysfunction and death are promoted by the T helper 1 cytokine interferon gamma. These epithelial changes further destabilize the tear film, amplify inflammation, and create a vicious cycle.
3.Discovery and Development of Potent LFA-1/ICAM-1 Antagonist SAR 1118 as an Ophthalmic Solution for Treating Dry Eye.
Zhong M;Gadek TR;Bui M;Shen W;Burnier J;Barr KJ;Hanan EJ;Oslob JD;Yu CH;Zhu J;Arkin MR;Evanchik MJ;Flanagan WM;Hoch U;Hyde J;Prabhu S;Silverman JA;Wright J ACS Med Chem Lett. 2012 Jan 31;3(3):203-6. doi: 10.1021/ml2002482. eCollection 2012 Mar 8.
LFA-1/ICAM-1 interaction is essential in support of inflammatory and specific T-cell regulated immune responses by mediating cell adhesion, leukocyte extravasation, migration, antigen presentation, formation of immunological synapse, and augmentation of T-cell receptor signaling. The increase of ICAM-1 expression levels in conjunctival epithelial cells and acinar cells was observed in animal models and patients diagnosed with dry eye. Therefore, it has been hypothesized that small molecule LFA-1/ICAM-1 antagonists could be an effective topical treatment for dry eye. In this letter, we describe the discovery of a potent tetrahydroisoquinoline (THIQ)-derived LFA-1/ICAM-1 antagonist (SAR 1118) and its development as an ophthalmic solution for treating dry eye.
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