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Cat. No. M5852
Lifitegrast Structure

SAR 1118

Size Price Availability Quantity
5mg USD 100 In stock
10mg USD 150 In stock
50mg USD 450 In stock
100mg USD 770 In stock
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Quality Control
  • Current batch:
  • Purity >98%
  • COA
  • MSDS
Biological Activity

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. 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.

Cell Experiment
Cell lines T-cell
Preparation method Lifitegrast potently inhibits human T-cell binding to human ICAM-1, T-cell activation and cytokine release, and formation of the immunologic synapse.
Concentrations 3 nM
Incubation time
Animal Experiment
Animal models dogs diagnosed with keratoconjunctivitis sicca
Administration i.v.
Conversion of different model animals based on BSA (Value based on data from FDA Draft Guidelines)
Species Mouse Rat Rabbit Guinea pig Hamster Dog
Weight (kg) 0.02 0.15 1.8 0.4 0.08 10
Body Surface Area (m2) 0.007 0.025 0.15 0.05 0.02 0.5
Km factor 3 6 12 8 5 20
Animal A (mg/kg) = Animal B (mg/kg) multiplied by  Animal B Km
Animal A Km

For example, to modify the dose of resveratrol used for a mouse (22.4 mg/kg) to a dose based on the BSA for a rat, multiply 22.4 mg/kg by the Km factor for a mouse and then divide by the Km factor for a rat. This calculation results in a rat equivalent dose for resveratrol of 11.2 mg/kg.

Chemical Information
Molecular Weight 615.48
Formula C29H24Cl2N2O7S
CAS Number 1025967-78-5
Purity >98%
Solubility 29 mg/mL in DMSO
Storage at -20°C

Development of lifitegrast: a novel T-cell inhibitor for the treatment of dry eye disease.
Semba CP, et al. Clin Ophthalmol. 2016 Jun 10;10:1083-94. PMID: 27354762.

Lifitegrast Ophthalmic Solution 5.0% versus Placebo for Treatment of Dry Eye Disease: Results of the Randomized Phase III OPUS-2 Study.
Tauber J, et al. Ophthalmology. 2015 Dec;122(12):2423-31. PMID: 26365210.

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Keywords: Lifitegrast, SAR 1118 supplier, Integrin, inhibitors

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