Lifitegrast
Based on 11 publication(s) in Google Scholar
Lifitegrast (SAR 1118) is a potent integrin antagonist. Lifitegrast 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 inhibits Jurkat T cell attachment to ICAM-1 with an IC50 of 2.98 nM. Lifitegrast can be used for researching dry eye disease.
商品は「研究用試薬」です。人や動物の医療用・臨床診断用・食品用の製品ではありません。
研究用途以外に使用した場合、当社は一切の責任を負いかねます。
- 純度: 99.29%
- CAS 番号: 1025967-78-5
- 分子式: C29H24Cl2N2O7S
- 分子量:615.48
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保管条件:Powder -20°C, 3 years , 4°C, 2 years ; In solvent -80°C, 1 year , -20°C, 6 months
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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溶剤 & 溶解度
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MedChemExpress（MCE）の使用を引用している文献 Lifitegrast
More- Signal Transduct Target Ther. 2022 Mar 11;7(1):83. [Abstract]
- Redox Biol. 2026 Mar:90:104039. [Abstract]
- J Med Chem. 2025 Aug 28;68(16):17202-17220. [Abstract]
- Sci Data. 2024 Sep 19;11(1):1024. [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]
- Biomed Pharmacother. 2025 Aug:189:118246. [Abstract]
- Cell Biomater. 2025 May 27.
- bioRxiv. 2025 Mar 19:2025.03.19.644113. [Abstract]
- Res Sq. 2024 Jun 04.
Customer Validation & Images
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Cell Migration/Invasion Assay
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生物活性
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αLβ2 |
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Cell Line
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Type | Value | Description | References |
|---|---|---|---|---|
| HuT78 | IC50 |
0.009 μM
Compound: 1g, SAR 1118
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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
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
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[PMID: 24900456] |
| HuT78 | IC50 |
0.074 μM
Compound: 1g, SAR 1118
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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
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
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[PMID: 24900456] |
| Jurkat | IC50 |
2.98 nM
Compound: 1g, SAR 1118
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Inhibition of human recombinant ICAM-1 adhesion into human Jurkat cells after 1 hr
Inhibition of human recombinant ICAM-1 adhesion into human Jurkat cells after 1 hr
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[PMID: 24900456] |
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.
Lifitegrast (SAR 1118) ophthalmic drops administered thrice daily deliver therapeutic levels of Lifitegrast (SAR 1118) in the retina and can alleviate the retinal complications associated with diabetes[3].
MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.
化学情報
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CAS 番号 1025967-78-5
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性状 Solid
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分子量 615.48
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分子式 C29H24Cl2N2O7S
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Color White to off-white
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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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別名
SAR 1118; SHP-606
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輸送条件
Room temperature in continental US; may vary elsewhere.
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保管条件
Powder -20°C 3 years 4°C 2 years In solvent -80°C 1 year -20°C 6 months
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 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 -
J Med Chem
2025 Aug 28;68(16):17202-17220. PMID: 40795266
Lifitegrast 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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Sci Data
High-throughput drug screening identifies novel therapeutics for Low Grade Serous Ovarian Carcinoma. [Abstract]2024 Sep 19;11(1):1024. PMID: 39300112 -
Inflammation
Exposure to Dietary Nitrite Exacerbates Lupus in MRL/lpr Mice by Enhancing Integrin Alpha M. [Abstract]2025 Aug 4. PMID: 40758225
Lifitegrast 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 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 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 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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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 Aug:189:118246. PMID: 40543162 -
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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 -
溶剤 & 溶解度
DMSO : ≥ 29 mg/mL (47.12 mM; Hygroscopic DMSO has a significant impact on the solubility of product, please use newly opened DMSO)
* "≥" means soluble, but saturation unknown.
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, 1 year; -20°C, 6 months. When stored at -80°C, please use it within 1 year. When stored at -20°C, please use it within 6 months.
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, 1 year; -20°C, 6 months. When stored at -80°C, please use it within 1 year. When stored at -20°C, please use it within 6 months.
濃度 (開始) × 体積 (開始) = 濃度 (終了) × 体積 (終了)
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 (4.06 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: ≥ 2.08 mg/mL (3.38 mM); Clear solution
This protocol yields a clear solution of ≥ 2.08 mg/mL (saturation unknown).
Taking 1 mL working solution as an example, add 100 μL DMSO stock solution (20.8 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.
Please enter your animal formula composition:
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%DMSO +
Recommended: Keep the proportion of DMSO in working solution below 2% if your animal is weak.
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%+
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+%Tween-80 + +
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%Saline +
The co-solvents required include: DMSO, . All of co-solvents are available by MedChemExpress (MCE). , Tween 80. All of co-solvents are available by MedChemExpress (MCE).
Working solution concentration: 0.22 mg/mL
Method for preparing stock solution: mg drug dissolved in μL DMSO. Stock solution concentration: mg/mL.
1. Take μL DMSO stock solution;
2. Add μL .
μL , mix evenly;
3. Then add μL Tween 80, mix evenly;
4. Then add μL
Please ensure that the stock solution in the first step is dissolved to a clear state, and add co-solvents in sequence. You can use ultrasonic heating (ultrasonic cleaner, recommended frequency 20-40 kHz), vortexing, etc. to assist dissolution.
プロトコル
Rats: The ocular pharmacokinetics of Lifitegrast (SAR 1118) are studied in rats after a single topical dose of 14C-SAR 1118 (1 mg/eye; 40 μCi; 15.5 μL). Lifitegrast (SAR 1118) concentration time profiles in plasma and ocular tissues are quantified by liquid scintillation counting (LSC). The pharmacologic activity of SAR 1118 eye drops administered thrice daily for 2 months at 1% (0.3 mg/eye/d) and 5% (1.5 mg/eye/d) is assessed in an STZ-induced diabetic rat model by determining retinal leukostasis and blood–retinal barrier breakdown[3].
Mice: The role of LFA-1 (CD11a/CD18) is examined either in CD18-/- mice, by intraperitoneal injection of anti-CD11a, or by topical application of lifitegrast. Corneal inflammation is induced by epithelial abrasion and exposure to either tobramycin-killed Pseudomonas aeruginosa or Staphylococcus aureus in the presence of a 2-mm-diameter punch from a silicone hydrogel contact lens. After 24 h, corneal thickness and haze are examined by confocal microscopy, and neutrophil recruitment to the corneal stroma is detected by immunohistochemistry[2].
MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.
純度とドキュメンテーション
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データシート (278 KB)
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参考文献
[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, 1 year; -20°C, 6 months. When stored at -80°C, please use it within 1 year. When stored at -20°C, please use it within 6 months.
| Optional Solvent | Concentration Solvent Mass | 1 mg | 5 mg | 10 mg | 25 mg |
|---|---|---|---|---|---|
| DMSO | 1 mM | 1.6247 mL | 8.1237 mL | 16.2475 mL | 40.6187 mL |
| 5 mM | 0.3249 mL | 1.6247 mL | 3.2495 mL | 8.1237 mL | |
| 10 mM | 0.1625 mL | 0.8124 mL | 1.6247 mL | 4.0619 mL | |
| 15 mM | 0.1083 mL | 0.5416 mL | 1.0832 mL | 2.7079 mL | |
| 20 mM | 0.0812 mL | 0.4062 mL | 0.8124 mL | 2.0309 mL | |
| 25 mM | 0.0650 mL | 0.3249 mL | 0.6499 mL | 1.6247 mL | |
| 30 mM | 0.0542 mL | 0.2708 mL | 0.5416 mL | 1.3540 mL | |
| 40 mM | 0.0406 mL | 0.2031 mL | 0.4062 mL | 1.0155 mL |
Lifitegrast 関連分類
HY-19344 関連分類
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