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Lifitegrast

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Catalog No. T3977Cas No. 1025967-78-5
Alias SHP-606, SAR 1118

Lifitegrast (SAR 1118) is an antagonist of lymphocyte function-associated antigen-1.

Lifitegrast

Lifitegrast

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Purity: 99.66%
Catalog No. T3977Alias SHP-606, SAR 1118Cas No. 1025967-78-5
Lifitegrast (SAR 1118) is an antagonist of lymphocyte function-associated antigen-1.
Pack SizePriceUSA WarehouseGlobal WarehouseQuantity
5 mg$33In StockIn Stock
10 mg$52In StockIn Stock
25 mg$93In StockIn Stock
50 mg$147In StockIn Stock
100 mg$239In StockIn Stock
500 mg$588In StockIn Stock
1 mL x 10 mM (in DMSO)$55In StockIn Stock
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In Stock Estimated shipping dateUSA Warehouse[1-2 days] Global Warehouse[5-7 days]
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Purity:99.66%
Color:White
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Product Introduction

Bioactivity
Description
Lifitegrast (SAR 1118) is an antagonist of lymphocyte function-associated antigen-1.
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].
SynonymsSHP-606, SAR 1118
Chemical Properties
Molecular Weight615.48
FormulaC29H24Cl2N2O7S
Cas No.1025967-78-5
SmilesCS(=O)(=O)c1cccc(C[C@H](NC(=O)c2c(Cl)cc3CN(CCc3c2Cl)C(=O)c2ccc3ccoc3c2)C(O)=O)c1
Relative Density.no data available
Storage & Solubility Information
StoragePowder: -20°C for 3 years | In solvent: -80°C for 1 year | Shipping with blue ice/Shipping at ambient temperature.
Solubility Information
DMSO: 245 mg/mL (398.06 mM), Sonication is recommended.
In Vivo Formulation
10% DMSO+40% PEG300+5% Tween 80+45% Saline: 2 mg/mL (3.25 mM), Sonication is recommended.
Please add the solvents sequentially, clarifying the solution as much as possible before adding the next one. Dissolve by heating and/or sonication if necessary. Working solution is recommended to be prepared and used immediately. The formulation provided above is for reference purposes only. In vivo formulations may vary and should be modified based on specific experimental conditions.
Solution Preparation Table
DMSO
1mg5mg10mg50mg
1 mM1.6247 mL8.1237 mL16.2475 mL81.2374 mL
5 mM0.3249 mL1.6247 mL3.2495 mL16.2475 mL
10 mM0.1625 mL0.8124 mL1.6247 mL8.1237 mL
20 mM0.0812 mL0.4062 mL0.8124 mL4.0619 mL
50 mM0.0325 mL0.1625 mL0.3249 mL1.6247 mL
100 mM0.0162 mL0.0812 mL0.1625 mL0.8124 mL

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In Vivo Formulation Calculator (Clear solution)

Please enter your animal experiment information in the following box and click Calculate to obtain the stock solution preparation method and in vivo formula preparation method:
TargetMol | Animal experiments For example, if the intended dosage is 10 mg/kg for animals weighing 20 g , with a dosing volume of 100 μL per animal, TargetMol | Animal experiments and a total of 10 animals are to be administered, using a formulation of TargetMol | reagent 10% DMSO+ 40% PEG300+ 5% Tween 80+ 45% Saline/PBS/ddH2O , the resulting working solution concentration would be 2 mg/mL.
Stock Solution Preparation:

Dissolve 2 mg of the compound in 100 μL DMSOTargetMol | reagent to obtain a stock solution at a concentration of 20 mg/mL . If the required concentration exceeds the compound's known solubility, please contact us for technical support before proceeding.

Preparation of the In Vivo Formulation:

1) Add 100 μL of the DMSOTargetMol | reagent stock solution to 400 μL PEG300TargetMol | reagent and mix thoroughly until the solution becomes clear.

2) Add 50 μL Tween 80 and mix well until fully clarified.

3) Add 450 μL Saline,PBS or ddH2OTargetMol | reagent and mix thoroughly until a homogeneous solution is obtained.

This example is provided solely to demonstrate the use of the In Vivo Formulation Calculator and does not constitute a recommended formulation for any specific compound. Please select an appropriate dissolution and formulation strategy based on your experimental model and route of administration.
All co-solvents required for this protocol, includingDMSO, PEG300/PEG400, Tween 80, SBE-β-CD, and Corn oil, are available for purchase on the TargetMol website.
1 Enter information below:
mg/kg
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μL
2 Enter the in vivo formulation:
% DMSO
%
% Tween 80
% Saline/PBS/ddH2O

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Please see Inhibitor Handling Instructions for more frequently ask questions. Topics include: how to prepare stock solutions, how to store products, and cautions on cell-based assays & animal experiments, etc

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