Lifitegrast

SKU: orb1227126

Description

A potent LFA-1/ICAM-1 antagonist with IC50 of 9 nM in HuT78 cells; exhibits good in vitro safety profile and low potency on CYP3A4, CYP2C9 and hERG; development as an ophthalmic solution for treating dry eye.Other Indication Approved(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.Lifitegrast strongly inhibits Jurkat T cell attachment to ICAM-1 with an IC50 of 2.98 nM.\n(In Vivo):Lifitegrast (SAR 1118), 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.Lifitegrast (SAR 1118) ophthalmic drops administered thrice daily deliver therapeutic levels of Lifitegrast (SAR 1118) in the retina and can alleviate the retinal complications associated with diabetes.

Research Area

Pharmacology & Drug Discovery

Key Properties

• CAS Number: 1025967-78-5
• MW: 615.4811
• Purity: >98% (HPLC)
• Formula: C₂₉H₂₄Cl₂N₂O₇S
• SMILES: O=C(O)[C@@H](NC(C1=C(Cl)C2=C(CN(C(C3=CC=C4C=COC4=C3)=O)CC2)C=C1Cl)=O)CC5=CC=CC(S(=O)(C)=O)=C5
• Target: Integrin
• Solubility: DMSO: ≥ 29 mg/mL

Bioactivity

• In Vivo:
  Lifitegrast (SAR 1118), 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. Lifitegrast (SAR 1118) ophthalmic drops administered thrice daily deliver therapeutic levels of Lifitegrast (SAR 1118) in the retina and can alleviate the retinal complications associated with diabetes.
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• 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. Lifitegrast strongly inhibits Jurkat T cell attachment to ICAM-1 with an IC50 of 2.98 nM.
  Read more...

Storage & Handling

• Storage: Storage temperature: -20°C. Stability: ≥ 2 years
• Expiration Date: 12 months from date of receipt.
• Disclaimer: For research use only

Alternative Names

SAR1118 | SAR 1118 | SAR-1118

Quick Database Links

Gene Symbol

Integrin