Lifitegrast-d4-1

Lifitegrast-d4-1 is deuterium labeled Lifitegrast. 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[1][2].

Product Specifications

UNSPSC

12352005

Target

Integrin; Isotope-Labeled Compounds

Type

Isotope-Labeled Compounds

Related Pathways

Cytoskeleton; Others

Field of Research

Inflammation/Immunology

Smiles

O=C(N[C@H](C(O)=O)CC1=CC=CC(S(C)(=O)=O)=C1)C2=C(Cl)C3=C(C([2H])([2H])N(C(C4=CC=C5C=COC5=C4)=O)C([2H])([2H])C3)C=C2Cl

Molecular Formula

C29H20D4Cl2N2O7S

Molecular Weight

619.51

References & Citations

[1]Russak EM, et al. Impact of Deuterium Substitution on the Pharmacokinetics of Pharmaceuticals. Ann Pharmacother. 2019 Feb;53 (2) :211-216.|[2]Perez VL, et al. Lifitegrast, a Novel Integrin Antagonist for Treatment of Dry Eye Disease. Ocul Surf. 2016 Apr;14 (2) :207-15.|[3]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.|[4]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.