SAR 1118; SHP-606 MedChemExpress (MCE)

Product Name	Lifitegrast
Synonyms	CS-2633;SAR1118;SAR-1118;ifitegrast;Lifitegrast;lifitegrast;Lifitegrast-d4;Lifitegrast Impurity;Lifitegrast, SAR 1118
CAS	1025967-78-5
EINECS	813-044-8
Chemical Formula	C29H24Cl2N2O7S
Molecular Weight	615.48
inchi
Package	10 mM * 1 mL;1 mg;5 mg;10 mg;25 mg;50 mg;100 mg
Price	Email to quote
Descriptions	Lifitegrast Lifitegrast MedChemExpress (MCE) HY-19344 1025967-78-5 SAR 1118 Descriptions Lifitegrast Lifitegrast MedChemExpress (MCE) HY-19344 1025967-78-5 SAR 1118 SHP-606 99.29% Powder -20°C 3 years 4°C 2 years In solvent -80°C 1 year -20°C 6 months Room temperature in continental US may vary elsewhere. Lifitegrast (SAR 1118) is a potent integrin antagonist. Lifitegrast blocks the binding of intercellular adhesion molecule 1 (ICAM-1) to lymphocyte function-associated antigen 1 (LFA-1), interrupting the T cell-mediated inflammatory cycle. Lifitegrast inhibits Jurkat T cell attachment to ICAM-1 with an IC50 of 2.98 nM. Lifitegrast can be used for researching dry eye disease. 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[1]. Lifitegrast strongly inhibits Jurkat T cell attachment to ICAM-1 with an IC50 of 2.98 nM[1]. 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[2]. 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[3]. Rats: The ocular pharmacokinetics of Lifitegrast (SAR 1118) are studied in rats after a single topical dose of 14C-SAR 1118 (1 mg/eye 40 μCi 15.5 μL). Lifitegrast (SAR 1118) concentration time profiles in plasma and ocular tissues are quantified by liquid scintillation counting (LSC). The pharmacologic activity of SAR 1118 eye drops administered thrice daily for 2 months at 1% (0.3 mg/eye/d) and 5% (1.5 mg/eye/d) is assessed in an STZ-induced diabetic rat model by determining retinal leukostasis and blood–retinal barrier breakdown[3]. Mice: The role of LFA-1 (CD11a/CD18) is examined either in CD18-/- mice, by intraperitoneal injection of anti-CD11a, or by topical application of lifitegrast. Corneal inflammation is induced by epithelial abrasion and exposure to either tobramycin-killed Pseudomonas aeruginosa or Staphylococcus aureus in the presence of a 2-mm-diameter punch from a silicone hydrogel contact lens. After 24 h, corneal thickness and haze are examined by confocal microscopy, and neutrophil recruitment to the corneal stroma is detected by immunohistochemistry[2]. αLβ2 \| \| \| \| \| \| \| \| \| \| [1]. Perez VL, et al. Lifitegrast, a Novel Integrin Antagonist for Treatment of Dry Eye Disease. Ocul Surf. 2016 Apr 14(2):207-15. [Content Brief] [2]. Sun Y, et al. Corneal inflammation is inhibited by the LFA-1 antagonist, lifitegrast (SAR 1118). J Ocul Pharmacol Ther. 2013 May 29(4):395-402. [Content Brief] [3]. Rao VR, et al. Delivery of SAR 1118 to the retina via ophthalmic drops and its effectiveness in a rat streptozotocin(STZ) model of diabetic retinopathy (DR). Invest Ophthalmol Vis Sci. 2010 Oct 51(10):5198-204. [Content Brief]
Last Update	2025-04-01 14:45:47

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