Lifitegrast

Modify Date: 2024-01-03 10:24:04

Lifitegrast Structure
Lifitegrast structure
 Common Name Lifitegrast
CAS Number 1025967-78-5 Molecular Weight 615.481
Density 1.5±0.1 g/cm3 Boiling Point 811.9±65.0 °C at 760 mmHg
Molecular Formula C29H24Cl2N2O7S Melting Point N/A
MSDS N/A Flash Point 444.8±34.3 °C

 Use of Lifitegrast


Lifitegrast is an integrin lymphocyte function-associated antigen-1 (LFA-1) antagonist; inhibits Jurkat T cell attachment to ICAM-1 with an IC50 of 2.98 nM.

 Names

Name Lifitegrast
Synonym More Synonyms

 Lifitegrast Biological Activity

Description Lifitegrast is an integrin lymphocyte function-associated antigen-1 (LFA-1) antagonist; inhibits Jurkat T cell attachment to ICAM-1 with an IC50 of 2.98 nM.
Related Catalog
Target

IC50: 2.98 nM (LFA-1)[1]
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[1].
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[2]. 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[3].
Animal Admin Rats: The ocular pharmacokinetics of SAR 1118 are studied in rats after a single topical dose of 14C-SAR 1118 (1 mg/eye; 40 μCi; 15.5 μL). 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].
References

[1]. Perez VL, et al. Lifitegrast, a Novel Integrin Antagonist for Treatment of Dry Eye Disease. Ocul Surf. 2016 Apr;14(2):207-15.

[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.

[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.

 Chemical & Physical Properties

Density 1.5±0.1 g/cm3
Boiling Point 811.9±65.0 °C at 760 mmHg
Molecular Formula C29H24Cl2N2O7S
Molecular Weight 615.481
Flash Point 444.8±34.3 °C
Exact Mass 614.068115
PSA 142.37000
LogP 1.54
Vapour Pressure 0.0±3.1 mmHg at 25°C
Index of Refraction 1.661
Storage condition -20℃

 Synonyms

L-Phenylalanine, N-[[2-(6-benzofuranylcarbonyl)-5,7-dichloro-1,2,3,4-tetrahydro-6-isoquinolinyl]carbonyl]-3-(methylsulfonyl)-
N-{[2-(1-Benzofuran-6-ylcarbonyl)-5,7-dichloro-1,2,3,4-tetrahydro-6-isoquinolinyl]carbonyl}-3-(methylsulfonyl)-L-phenylalanine
Lifitegrast
N-[[2-(6-Benzofuranylcarbonyl)-5,7-dichloro-1,2,3,4-tetrahydro-6-isoquinolinyl]carbonyl]-3-(methylsulfonyl)-L-phenylalanine
SAR 1118
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Related Compounds: More...
Lifitegrast sodium
1119276-80-0
Lifitegrast Impurity 9
1289646-90-7
Lifitegrast Impurity 5
1289646-93-0
Lifitegrast Impurity 1
1194550-61-2
Lifitegrast Impurity 2
2049127-88-8
Lifitegrast Impurity 7
1194550-67-8
Lifitegrast Impurity 4
1194550-65-6
Lifitegrast Impurity 8
2271299-08-0
Lifitegrast Intermediate 4
1194550-59-8
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