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Lifitegrast Integrin antagonist

Name: Lifitegrast
SKU: S3714
Availability: InStock
Rating: 5 (4 reviews)

Cat.No.S3714

Lifitegrast (SAR1118,SHP-606) is a novel small molecule integrin antagonist that inhibits a specific T cell-mediated inflammatory pathway involved in the pathogenesis of DED.

Chemical Structure

Molecular Weight: 615.48

Jump to Mechanism of Action Cell Culture & Working Concentration Solubility Chemical Information, Storage & Stability Specificity

Quality Control

Batch: Purity: 99.74%

99.74

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Cell Culture, Treatment & Working Concentration

Cell Lines	Assay Type	Incubation Time	Activity Description	PMID
Jurkat	Function assay	1 hr	Inhibition of human recombinant ICAM-1 adhesion into human Jurkat cells after 1 hr, IC50=0.00298μM	24900456
HuT-78	Function assay	1 hr	Antagonist activity at LFA-1/ICAM-1 in human HuT-78 T-cells assessed as inhibition of cell adhesion after 1 hr by p-nitrophenyl n-acetyl-beta-D-glucosaminide method, IC50=0.009μM	24900456
HuT-78	Function assay	1 hr	Antagonist activity at LFA-1/ICAM-1 in human HuT-78 T-cells assessed as inhibition of cell adhesion after 1 hr by p-nitrophenyl n-acetyl-beta-D-glucosaminide method in presence of 10% human serum, IC50=0.074μM	24900456
Click to View More Cell Line Experimental Data

Chemical Information, Storage & Stability

Molecular Weight	615.48	Formula	C₂₉H₂₄Cl₂N₂O₇S	Storage (From the date of receipt)	3 years-20°Cpowder
CAS No.	1025967-78-5	Download SDF		Storage of Stock Solutions	1 year-80°Cin solvent 1 month-20°Cin solvent
Synonyms	SAR1118,SHP-606			Smiles	CS(=O)(=O)C1=CC=CC(=C1)CC(C(=O)O)NC(=O)C2=C(C=C3CN(CCC3=C2Cl)C(=O)C4=CC5=C(C=C4)C=CO5)Cl

Solubility

In vitro
Batch:

DMSO : 100 mg/mL (162.47 mM)
(Moisture-contaminated DMSO may reduce solubility. Use fresh, anhydrous DMSO.)

Ethanol : 20 mg/mL

Water : Insoluble

Molarity Calculator

Mass	Concentration	Volume	Molecular Weight
=	×	×

Dilution Calculator Molecular Weight Calculator

In vivo Batch:
Homogeneous suspension	CMC-NA	≥5mg/ml	Taking the 1 mL working solution as an example, add 5 mg of this product to 1 ml of CMC-Na solution, mix evenly to obtain a homogeneous suspension with a final concentration of 5 mg/ml.
Homogeneous suspension	CMC-NA	≥5mg/ml	Taking the 1 mL working solution as an example, add 5 mg of this product to 1 ml of CMC-Na solution, mix evenly to obtain a homogeneous suspension with a final concentration of 5 mg/ml.
Clear solution	5%DMSO 1 Corn oil Validated by Selleck labs. Should you need adjustments to this formulation, contact our sales team for custom testing.	0.700mg/ml (1.14mM)	Taking the 1 mL working solution as an example, add 50 μL of 14 mg/ml clear DMSO stock solution to 950 μL of corn oil and mix evenly. The mixed solution should be used immediately for optimal results.
Homogeneous suspension	CMC-NA	≥5mg/ml	Taking the 1 mL working solution as an example, add 5 mg of this product to 1 ml of CMC-Na solution, mix evenly to obtain a homogeneous suspension with a final concentration of 5 mg/ml.

In vivo Formulation Calculator (Clear solution)

Step 1: Enter information below (Recommended: An additional animal making an allowance for loss during the experiment)

Dosage: mg/kg Average weight of animals: g Dosing volume per animal:μL Number of animals:

Step 2: Enter the in vivo formulation (This is only the calculator, not formulation. Please contact us first if there is no in vivo formulation at the solubility Section.)

% DMSO + % + % Tween 80 + % ddH₂O

%DMSO+ %

Calculation results:

Working concentration: mg/ml;

Method for preparing DMSO master liquid: mg drug pre-dissolved in μL DMSO ( Master liquid concentration mg/mL, Please contact us first if the concentration exceeds the DMSO solubility of the batch of drug. )

Method for preparing in vivo formulation: Take μL DMSO master liquid, next addμL PEG300, mix and clarify, next addμL Tween 80, mix and clarify, next add μL ddH₂O, mix and clarify.

Method for preparing in vivo formulation: Take μL DMSO master liquid, next add μL Corn oil, mix and clarify.

Note: 1. Please make sure the liquid is clear before adding the next solvent.
2. Be sure to add the solvent(s) in order. You must ensure that the solution obtained, in the previous addition, is a clear solution before proceeding to add the next solvent. Physical methods such
as vortex, ultrasound or hot water bath can be used to aid dissolving.

Mechanism of Action

Targets/IC₅₀/Ki	Integrin ^[1]
In vitro	Lifitegrast inhibits release of cytokines, interferon d, tumor necrosis factor alpha (TNF-α), and other interleukins (ILs). It is a novel integrin antagonist which prevents LFA-1/ICAM-1 interaction preventing T-cell activation/recruitment and release of inflammatory mediators, thereby decreasing the inflammatory responses in DED^[1].
In vivo	In vivo study of lifitegrast as radiolabeled drops in rats demonstrated that it was rapidly distributed in ocular and periocular tissues, cleared by normal tear drainage, and was devoid of systemic side effects. A similar dose tolerability study of lifitegrast in dogs suffering from keratoconjunctivitis sicca proved its efficacy and safety. Lifitegrast is found to be a highly potent drug in various clinical trials as it alleviates both the signs and symptoms of DED, which showed rapid onset of action and good therapeutic efficacy as ophthalmic drops. It protected the corneal surfaces and was well tolerated locally as well as systemically^[1].
References	[1] https://www.ncbi.nlm.nih.gov/pmc/articles/PMC5242036/

Clinical Trial Information

(data from https://clinicaltrials.gov, updated on 2024-05-22)

NCT Number	Recruitment	Conditions	Sponsor/Collaborators	Start Date	Phases
NCT05857748	Withdrawn	Dry Eye Disease	Novartis Pharmaceuticals\|Novartis	July 31 2023	--
NCT03866629	Completed	Dry Eye	MDbackline LLC	December 20 2018	--
NCT00936520	Terminated	Diabetic Macular Edema (DME)\|Pars Plana Vitrectomy	Johns Hopkins University\|SARcode Bioscience	August 2009	Phase 1

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