Lifitegrast sodium
Based on 11 publication(s) in Google Scholar
Lifitegrast (SAR 1118) sodium is a potent integrin antagonist. Lifitegrast sodium blocks the binding of intercellular adhesion molecule 1 (ICAM-1) to lymphocyte function-associated antigen 1 (LFA-1), interrupting the T cell-mediated inflammatory cycle. Lifitegrast sodium inhibits Jurkat T cell attachment to ICAM-1 with an IC50 of 2.98 nM. Lifitegrast sodium can be used for researching dry eye disease.
Nos produits utilisent uniquement pour la recherche. Nous ne vendons pas aux patients.
- Pureté: 99.20%
- CAS No.: 1119276-80-0
- Formule: C29H23Cl2N2NaO7S
- Masse moléculaire:637.46
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Stockage:
4°C, sealed storage, away from moisture
* In solvent : -80°C, 6 months; -20°C, 1 month (sealed storage, away from moisture)
To place orders, for customer services and technical support, please contact: MedChemExpress USA
Tel: 609-228-6898 E-mail: [email protected] [email protected]
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Chemical Information
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Solvant et solubilité
- Pureté et documentation
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Publications Citing Use of MedChemExpress (MCE) Lifitegrast sodium
More- Signal Transduct Target Ther. 2022 Mar 11;7(1):83. [Abstract]
- Redox Biol. 2026 Mar:90:104039. [Abstract]
- Biomed Pharmacother. 2025 Jun 20:189:118246. [Abstract]
- Sci Data. 2024 Sep 19;11(1):1024. [Abstract]
- J Med Chem. 2025 Aug 28;68(16):17202-17220. [Abstract]
- Inflammation. 2025 Aug 4. [Abstract]
- Cancers (Basel). 2024 Nov 12;16(22):3807. [Abstract]
- PLoS Negl Trop Dis. 2022 Oct 7;16(10):e0010848. [Abstract]
- Cell Biomater. 2025 May 27.
- bioRxiv. 2025 Mar 19:2025.03.19.644113. [Abstract]
- Res Sq. 2024 Jun 04.
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Activité biologique
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αLβ2 |
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[1].
Lifitegrast strongly inhibits Jurkat T cell attachment to ICAM-1 with an IC50 of 2.98 nM[1].
MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.
MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.
| NCT Number | Sponsor | Condition | Start Date |
Phase
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|---|---|---|---|---|
| NCT01329991 | Plexxikon| | 2011-05 | PHASE1 |
Chemical Information
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CAS No. 1119276-80-0
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Appearance Solid
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Masse moléculaire 637.46
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Formule C29H23Cl2N2NaO7S
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Color Light yellow to yellow
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SMILES
O=C(O[Na])[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 sodium; SHP-606 sodium
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Livraison
Room temperature in continental US; may vary elsewhere.
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Stockage
4°C, sealed storage, away from moisture
* In solvent : -80°C, 6 months; -20°C, 1 month (sealed storage, away from moisture)
Publications (11)
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Journal Impact Factor
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Most Recent
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Signal Transduct Target Ther
2022 Mar 11;7(1):83. PMID: 35277473
Lifitegrast sodium purchased from MedChemExpress. Usage Cited in: Signal Transduct Target Ther. 2022 Mar 11;7(1):83. [Abstract]
Activated Jurkat cells were pretreated with Lifitegrast, an inhibitor of LFA-1 at different concentrations (50, 100, or 200 nM) at 37 °C for 30 min before infection (MOI = 0.01). Intracellular viral RNA was quantified at 24 h post infection.
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Redox Biol
A LNK-CBL-HNRPA2B1-GPX4 signaling axis mediates dopaminergic neuron vulnerability to ferroptosis in Parkinson's disease. [Abstract]2026 Mar:90:104039. PMID: 41616574 -
Biomed Pharmacother
Identification of nsp16 inhibitors of SARS -CoV-2, SARS -CoV-1 and MERS-CoV from FDA-approved drugs using in silico and in vitro methods. [Abstract]2025 Jun 20:189:118246. PMID: 40543162 -
Sci Data
High-throughput drug screening identifies novel therapeutics for Low Grade Serous Ovarian Carcinoma. [Abstract]2024 Sep 19;11(1):1024. PMID: 39300112 -
J Med Chem
2025 Aug 28;68(16):17202-17220. PMID: 40795266
Lifitegrast sodium purchased from MedChemExpress. Usage Cited in: J Med Chem. 2025 Aug 28;68(16):17202-17220. [Abstract]
Lifitegrast a known inhibitor of the lymphocyte function-associated antigen 1 integrin (LFA-1) inhibits migration of CD3+ T-cells using the transwell assay with an EC50 of 2.2 ± 3.6 nM.
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Inflammation
Exposure to Dietary Nitrite Exacerbates Lupus in MRL/lpr Mice by Enhancing Integrin Alpha M. [Abstract]2025 Aug 4. PMID: 40758225
Lifitegrast sodium purchased from MedChemExpress. Usage Cited in: Inflammation. 2025 Aug 4. [Abstract]
Lifitegrast (15 mg/kg) reduces the expression of Itgam protein in kidney tissue.
Lifitegrast sodium purchased from MedChemExpress. Usage Cited in: Inflammation. 2025 Aug 4. [Abstract]
Lifitegrast (15 mg/kg) . Immunofluorescence staining was performed to visualize C3 deposition (red) and IgG accumulation (green) in kidney sections, and the objective magnification was 40×.
Lifitegrast sodium purchased from MedChemExpress. Usage Cited in: Inflammation. 2025 Aug 4. [Abstract]
Effects of Lifitegrast (15 mg/kg) on spleen immune cells in MRL/lpr mice. Flow cytometry analysis images depicting the mean abundance of DN T, Tfh, and plasma cells in the spleen.
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Cancers (Basel)
2024 Nov 12;16(22):3807. PMID: 39594764 -
PLoS Negl Trop Dis
LFA-1/ ICAM-1 promotes NK cell cytotoxicity associated with the pathogenesis of ocular toxoplasmosis in murine model. [Abstract]2022 Oct 7;16(10):e0010848. PMID: 36206304
Lifitegrast sodium purchased from MedChemExpress. Usage Cited in: PLoS Negl Trop Dis. 2022 Oct 7;16(10):e0010848. [Abstract]
Histology of the eye at Day 30 after infection in the OT murine model treated with vehicle or Lifitegrast(1%; 5 μL).
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bioRxiv
Mast cells interact directly with colorectal cancer cells to promote epithelial-to-mesenchymal transition. [Abstract]2025 Mar 19:2025.03.19.644113. PMID: 40166179 -
Solvant et solubilité
DMSO : 100 mg/mL (156.87 mM; Need ultrasonic; Hygroscopic DMSO has a significant impact on the solubility of product, please use newly opened DMSO)
H2O : 100 mg/mL (156.87 mM; Need ultrasonic)
Please refer to the solubility information to select the appropriate solvent. Once prepared, please aliquot and store the solution to prevent product inactivation from repeated freeze-thaw cycles.
Storage method and period of stock solution: -80°C, 6 months; -20°C, 1 month (sealed storage, away from moisture). When stored at -80°C, please use it within 6 months. When stored at -20°C, please use it within 1 month.
* Note: If you choose water as the stock solution, please dilute it to the working solution, then filter and sterilize it with a 0.22 μm filter before use.
Please refer to the solubility information to select the appropriate solvent. Once prepared, please aliquot and store the solution to prevent product inactivation from repeated freeze-thaw cycles.
Storage method and period of stock solution: -80°C, 6 months; -20°C, 1 month (sealed storage, away from moisture). When stored at -80°C, please use it within 6 months. When stored at -20°C, please use it within 1 month.
* Note: If you choose water as the stock solution, please dilute it to the working solution, then filter and sterilize it with a 0.22 μm filter before use.
Concentration (start) × Volume (start) = Concentration (final) × Volume (final)
Select the appropriate dissolution method based on your experimental animal and administration route.
- For the following dissolution methods, please ensure to first prepare a clear stock solution using an In Vitro approach and then sequentially add co-solvents:
- To ensure reliable experimental results, the clarified stock solution can be appropriately stored based on storage conditions. As for the working solution for In Vivo experiments, it is recommended to prepare freshly and use it on the same day.
- The percentages shown for the solvents indicate their volumetric ratio in the final prepared solution. If precipitation or phase separation occurs during preparation, heat and/or sonication can be used to aid dissolution.
Add each solvent one by one: 10% DMSO 40% PEG300 5% Tween-80 45% Saline
Solubility: ≥ 2.5 mg/mL (3.92 mM); Clear solution
This protocol yields a clear solution of ≥ 2.5 mg/mL (saturation unknown).
Taking 1 mL working solution as an example, add 100 μL DMSO stock solution (25.0 mg/mL) to 400 μL PEG300, and mix evenly; then add 50 μL Tween-80 and mix evenly; then add 450 μL Saline to adjust the volume to 1 mL.
Preparation of Saline: Dissolve 0.9 g sodium chloride in ddH₂O and dilute to 100 mL to obtain a clear Saline solution.
Add each solvent one by one: 10% DMSO 90% (20% SBE-β-CD in Saline)
Solubility: ≥ 2.5 mg/mL (3.92 mM); Clear solution
This protocol yields a clear solution of ≥ 2.5 mg/mL (saturation unknown).
Taking 1 mL working solution as an example, add 100 μL DMSO stock solution (25.0 mg/mL) to 900 μL 20% SBE-β-CD in Saline, and mix evenly.
Preparation of 20% SBE-β-CD in Saline (4°C, storage for one week): 2 g SBE-β-CD powder is dissolved in 10 mL Saline, completely dissolve until clear.
Please enter the basic information of animal experiments:
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Recommended: Prepare an additional quantity of animals to account for potential losses during experiments.
Working solution concentration: 0.22 mg/mL
This product has good water solubility, please refer to the measured solubility data in water/PBS/Saline for details.
Pureté et documentation
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Fiche technique (274 KB)
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SDS (252 KB)
- English - EN (252 KB)
- Français - FR (252 KB)
- Deutsch - DE (252 KB)
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- Español - ES (252 KB)
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- Italian - IT (252 KB)
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Instruction de manipulation (2659 KB)
Références
[1]. Perez VL, et al. Lifitegrast, a Novel Integrin Antagonist for Treatment of Dry Eye Disease. Ocul Surf. 2016 Apr;14(2):207-15. [Content Brief]
[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. [Content Brief]
[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. [Content Brief]
Complete Stock Solution Preparation Table
Please refer to the solubility information to select the appropriate solvent. Once prepared, please aliquot and store the solution to prevent product inactivation from repeated freeze-thaw cycles.
Storage method and period of stock solution: -80°C, 6 months; -20°C, 1 month (sealed storage, away from moisture). When stored at -80°C, please use it within 6 months. When stored at -20°C, please use it within 1 month.
| Optional Solvent | Concentration Solvent Mass | 1 mg | 5 mg | 10 mg | 25 mg |
|---|---|---|---|---|---|
| DMSO / H2O | 1 mM | 1.5687 mL | 7.8436 mL | 15.6873 mL | 39.2181 mL |
| 5 mM | 0.3137 mL | 1.5687 mL | 3.1375 mL | 7.8436 mL | |
| 10 mM | 0.1569 mL | 0.7844 mL | 1.5687 mL | 3.9218 mL | |
| 15 mM | 0.1046 mL | 0.5229 mL | 1.0458 mL | 2.6145 mL | |
| 20 mM | 0.0784 mL | 0.3922 mL | 0.7844 mL | 1.9609 mL | |
| 25 mM | 0.0627 mL | 0.3137 mL | 0.6275 mL | 1.5687 mL | |
| 30 mM | 0.0523 mL | 0.2615 mL | 0.5229 mL | 1.3073 mL | |
| 40 mM | 0.0392 mL | 0.1961 mL | 0.3922 mL | 0.9805 mL | |
| 50 mM | 0.0314 mL | 0.1569 mL | 0.3137 mL | 0.7844 mL | |
| 60 mM | 0.0261 mL | 0.1307 mL | 0.2615 mL | 0.6536 mL | |
| 80 mM | 0.0196 mL | 0.0980 mL | 0.1961 mL | 0.4902 mL | |
| 100 mM | 0.0157 mL | 0.0784 mL | 0.1569 mL | 0.3922 mL |
* Note: If you choose water as the stock solution, please dilute it to the working solution, then filter and sterilize it with a 0.22 μm filter before use.
Lifitegrast sodium Related Classifications
HY-19344A Related Classifications
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