Lifitegrast

SKU: orb1303486

Description

Lifitegrast (SAR 1118) is a small molecule antagonist of lymphocyte function-associated antigen-1 (LFA-1). It is used in research to investigate cell adhesion and immune signaling pathways, with applications in studying inflammatory conditions such as dry eye disease in both in vitro and in vivo models.

Research Area

Pharmacology & Drug Discovery, Signal Transduction

Key Properties

• CAS Number: 1025967-78-5
• MW: 615.48
• Purity: 99.66% (May vary between batches)
• Formula: C₂₉H₂₄Cl₂N₂O₇S
• SMILES: CS(=O)(=O)c1cccc(C[C@H](NC(=O)c2c(Cl)cc3CN(CCc3c2Cl)C(=O)c2ccc3ccoc3c2)C(O)=O)c1
• Target: Integrin
• Solubility: DMSO:245 mg/mL (398.06 mM);10% DMSO+40% PEG300+5% Tween 80+45% Saline:2 mg/mL (3.25 mM)

Bioactivity

• Target IC50:
  LFA1:2.98 nM.
• 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. Topical application of lifitegrast to the corneal surface of healthy adults is safe and well tolerated. SAR 1118 ophthalmic drops administered thrice daily deliver therapeutic levels of SAR 1118 in the retina and can alleviate the retinal complications associated with diabetes.
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• In Vitro:
  Lifitegrast is a novel small molecule integrin antagonist that 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. Lifitegrast strongly inhibits Jurkat T cell attachment to ICAM-1 with an IC50 of 2.98 nM.
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Storage & Handling

• Storage: -20°C
• Expiration Date: 12 months from date of receipt.
• Disclaimer: For research use only

Alternative Names

ICAM-1, Integrin, Inhibitor, LFA-1, inflammatory cycle, Lifitegrast, Jurkat T, inhibit, dry eye disease, T cell, SAR1118, SAR-1118, SAR 1118, SHP 606, SHP606, SHP-606

Compound Identifiers

PubChem CID

11965427