| Size | Price | Stock | Qty |
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| 25mg |
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| 50mg |
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| 100mg |
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| 250mg |
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| 500mg |
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Lifitegrast (formerly SAR 1118; SAR 1118-023; SAR-1118; trade name Xiidra) is a novel and potent integrin lymphocyte function-associated antigen-1 (LFA-1) antagonist approved in 2016 for the the treatment of Dry Eye Disease. It inhibits Jurkat T cell attachment to ICAM-1 with an IC50 of 2.98 nM. It inhibits Jurkat T cell attachment to ICAM-1 with an IC50 of 2.98 nM.
| ln Vitro |
By preventing the interaction of two crucial cell surface proteins—lymphocyte function-associated antigen 1 and intercellular adhesion molecule 1—ligifestegrast (SAR 1118) reduces T cell-mediated inflammation and lowers the total inflammatory response [1]. Lifitegrast has an IC50 of 2.98 nM, which results in a substantial inhibition of Jurkat T cell adhesion to ICAM-1[1].
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| ln Vivo |
Lifitegrast (SAR 1118) is best used with 1% solution applied two or three times prior to use. It has strong anti-inflammatory activity against corneal inflammation caused by antibiotic-killed Pseudomonas aeruginosa and Staphylococcus aureus in the presence of silicone hydrogel lenses [2]. Three times a day administration of Lifitegrast (SAR 1118) eye drops results in therapeutic levels of the substance in the retina and may lessen diabetic-related retinal complications [3].
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| References |
[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 |
| Molecular Formula |
C₂₉H₂₄CL₂N₂O₇S
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|---|---|
| Molecular Weight |
615.48
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| CAS # |
1025967-78-5
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| Related CAS # |
Lifitegrast sodium;1119276-80-0
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| SMILES |
O=C(O)[C@H](CC1=CC=CC(S(=O)(C)=O)=C1)NC(C2=C(Cl)C3=C(CN(C(C4=CC=C5C=COC5=C4)=O)CC3)C=C2Cl)=O
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| Synonyms |
SAR 1118 SAR 1118-023SAR-1118SHP-606SAR1118-02SHP606SAR 1118SHP 606SAR1118Lifitegrast sodium SAR-1118-023 Xiidra
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| Storage |
Powder -20°C 3 years 4°C 2 years In solvent -80°C 6 months -20°C 1 month |
| Shipping Condition |
Room temperature (This product is stable at ambient temperature for a few days during ordinary shipping and time spent in Customs)
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| Solubility (In Vitro) |
DMSO : ≥ 29 mg/mL (~47.12 mM)
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| Solubility (In Vivo) |
Solubility in Formulation 1: ≥ 2.5 mg/mL (4.06 mM) (saturation unknown) in 10% DMSO + 40% PEG300 + 5% Tween80 + 45% Saline (add these co-solvents sequentially from left to right, and one by one), clear solution.
For example, if 1 mL of working solution is to be prepared, you can add 100 μL of 25.0 mg/mL clear DMSO stock solution to 400 μL PEG300 and mix evenly; then add 50 μL Tween-80 to the above solution and mix evenly; then add 450 μL normal saline to adjust the volume to 1 mL. Preparation of saline: Dissolve 0.9 g of sodium chloride in 100 mL ddH₂ O to obtain a clear solution. Solubility in Formulation 2: ≥ 2.5 mg/mL (4.06 mM) (saturation unknown) in 10% DMSO + 90% Corn Oil (add these co-solvents sequentially from left to right, and one by one), clear solution. For example, if 1 mL of working solution is to be prepared, you can add 100 μL of 25.0 mg/mL clear DMSO stock solution to 900 μL of corn oil and mix evenly. View More
Solubility in Formulation 3: ≥ 2.08 mg/mL (3.38 mM) (saturation unknown) in 10% DMSO + 90% (20% SBE-β-CD in Saline) (add these co-solvents sequentially from left to right, and one by one), clear solution. |
| Preparing Stock Solutions | 1 mg | 5 mg | 10 mg | |
| 1 mM | 1.6247 mL | 8.1237 mL | 16.2475 mL | |
| 5 mM | 0.3249 mL | 1.6247 mL | 3.2495 mL | |
| 10 mM | 0.1625 mL | 0.8124 mL | 1.6247 mL |
*Note: Please select an appropriate solvent for the preparation of stock solution based on your experiment needs. For most products, DMSO can be used for preparing stock solutions (e.g. 5 mM, 10 mM, or 20 mM concentration); some products with high aqueous solubility may be dissolved in water directly. Solubility information is available at the above Solubility Data section. Once the stock solution is prepared, aliquot it to routine usage volumes and store at -20°C or -80°C. Avoid repeated freeze and thaw cycles.
Calculation results
Working concentration： mg/mL；
Method for preparing DMSO stock solution： mg drug pre-dissolved in μL DMSO (stock solution 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 stock solution, next add μL PEG300, mix and clarify, next addμL Tween 80, mix and clarify, next add μL ddH2O，mix and clarify.
(1) Please be sure that the solution is clear before the addition of next solvent. Dissolution methods like vortex, ultrasound or warming and heat may be used to aid dissolving.
(2) Be sure to add the solvent(s) in order.
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