Lifitegrast
A potent LFA-1/ICAM-1 antagonist with IC50 of 9 nM in HuT78 cells; exhibits good in vitro safety profile and low potency on CYP3A4, CYP2C9 and hERG; development as an ophthalmic solution for treating dry eye.Other Indication Approved (In Vitro) :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.Lifitegrast strongly inhibits Jurkat T cell attachment to ICAM-1 with an IC50 of 2.98 nM. (In Vivo) :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.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.
Product Specifications
CAS Number
1025967-78-5
Product Name Alternative
SAR1118 | SAR 1118 | SAR-1118
Field of Research
Pharmacology & Drug Discovery
Purity
>98% (HPLC)
Solubility
DMSO: ≥ 29 mg/mL
Smiles
O=C (O) [C@@H] (NC (C1=C (Cl) C2=C (CN (C (C3=CC=C4C=COC4=C3) =O) CC2) C=C1Cl) =O) CC5=CC=CC (S (=O) (C) =O) =C5
Molecular Formula
C29H24Cl2N2O7S
Molecular Weight
615.4811
Storage Conditions
Storage temperature: -20°C. Stability: ≥ 2 years
Notes
For research use only.
Other Product Names
L-Phenylalanine, N-[[2- (6-benzofuranylcarbonyl) -5,7-dichloro-1,2,3,4-tetrahydro-6-isoquinolinyl]carbonyl]-3- (methylsulfonyl) -
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