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Lifitegrast sodium (SAR 1118; SHP-606; SAR-1118-023; Xiidra), the sodium salt of Lifitegrast, is an integrin lymphocyte function-associated antigen-1 (LFA-1) antagonist with the potential for Treatment of Dry Eye Disease. It inhibits Jurkat T cell attachment to ICAM-1 with an IC50 of 2.98 nM. In 2016, Lifitegrast received FDA approval for the treatment of signs and symptoms of dry eye, a syndrome called keratoconjunctivitis sicca. Lifitegrast reduces inflammation by inhibiting inflammatory cell binding.
| ln Vitro |
Lifitegrast (SAR 1118) reduces the total inflammatory response by inhibiting the binding of two crucial cell surface proteins, lymphocyte function-associated antigen 1 and intercellular adhesion molecule 1, which in turn decreases T cell-mediated inflammation [1]. With an IC50 of 2.98 nM, liditelegrast potently prevents Jurkat T cell adhesion to ICAM-1[1].
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| ln Vivo |
When silicone hydrogel lenses are present, ligifegrast exhibits strong anti-inflammatory efficacy against corneal irritation brought on by antibiotic-killed Pseudomonas aeruginosa and Staphylococcus aureus. The best dosage is two or three pre-applies of 1% solution[2].
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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 |
C29H23CL2N2NAO7S
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|---|---|
| Molecular Weight |
637.46289563179
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| CAS # |
1119276-80-0
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| Related CAS # |
Lifitegrast;1025967-78-5
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| SMILES |
CS(=O)(c1cc(C[C@H](NC(c2c(Cl)c(CCN(C(c(cc3)cc4c3cco4)=O)C5)c5cc2Cl)=O)C([O-])=O)ccc1)=O.[Na+]
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| Chemical Name |
sodium
(S)-2-(2-(benzofuran-6-carbonyl)-5,7-dichloro-1,2,3,4-tetrahydroisoquinoline-6-carboxamido)-3-(3-(methylsulfonyl)phenyl)propanoate
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| Synonyms |
SAR-1118 SAR 1118-023SAR 1118 SAR1118-02 SAR1118Lifitegrast sodium SAR-1118-023 Xiidra
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| HS Tariff Code |
2934.99.9001
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| Storage |
Powder -20°C 3 years 4°C 2 years In solvent -80°C 6 months -20°C 1 month Note: Please store this product in a sealed and protected environment, avoid exposure to moisture. |
| 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) |
H2O : ~100 mg/mL (~156.87 mM)
DMSO : ~100 mg/mL (~156.87 mM) |
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| Solubility (In Vivo) |
Solubility in Formulation 1: ≥ 2.5 mg/mL (3.92 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 (3.92 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. 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 20% SBE-β-CD physiological saline solution and mix evenly. Preparation of 20% SBE-β-CD in Saline (4°C，1 week): Dissolve 2 g SBE-β-CD in 10 mL saline to obtain a clear solution. (Please use freshly prepared in vivo formulations for optimal results.) |
| Preparing Stock Solutions | 1 mg | 5 mg | 10 mg | |
| 1 mM | 1.5687 mL | 7.8436 mL | 15.6873 mL | |
| 5 mM | 0.3137 mL | 1.5687 mL | 3.1375 mL | |
| 10 mM | 0.1569 mL | 0.7844 mL | 1.5687 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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