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Lifitegrast

Catalog No. T3977   CAS 1025967-78-5
Synonyms: SHP-606, SAR 1118

Lifitegrast (SAR 1118) is a lymphocyte, function-associated antigen-1 antagonist.

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Lifitegrast Chemical Structure
Lifitegrast, CAS 1025967-78-5
Pack Size Availability Price/USD Quantity
5 mg In stock $ 36.00
10 mg In stock $ 52.00
25 mg In stock $ 94.00
50 mg In stock $ 163.00
100 mg In stock $ 271.00
500 mg In stock $ 663.00
1 mL * 10 mM (in DMSO) In stock $ 55.00
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Purity: 99.66%
Purity: 99.40%
Purity: 99.39%
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Biological Description
Chemical Properties
Storage & Solubility Information
Description Lifitegrast (SAR 1118) is a lymphocyte, function-associated antigen-1 antagonist.
Targets&IC50 LFA1:2.98 nM.
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].
Synonyms SHP-606, SAR 1118
Molecular Weight 615.48
Formula C29H24Cl2N2O7S
CAS No. 1025967-78-5

Storage

Powder: -20°C for 3 years | In solvent: -80°C for 1 year

Solubility Information

DMSO: 29 mg/mL

TargetMolReferences and Literature

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.

Related compound libraries

This product is contained In the following compound libraries:
Inhibitor Library Drug Repurposing Compound Library Cytoskeletal Signaling Pathway Compound Library FDA-Approved & Pharmacopeia Drug Library Bioactive Compound Library Immunology/Inflammation Compound Library Nonsteroidal Anti-Inflammatory Compound Library Human Metabolite Library ReFRAME Related Library Clinical Compound Library

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Keywords

Lifitegrast 1025967-78-5 Cytoskeletal Signaling Integrin ICAM-1 T cell SHP-606 inhibit SAR 1118 SHP606 SHP 606 dry eye disease SAR-1118 Jurkat T LFA-1 SAR1118 inflammatory cycle Inhibitor inhibitor

 

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