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Lifitegrast

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Chemical Structure| 1025967-78-5 同义名 : 利非司特 ;SAR 1118;SHP-606
CAS号 : 1025967-78-5
货号 : A113895
分子式 : C29H24Cl2N2O7S
纯度 : 97%
分子量 : 615.481
MDL号 : MFCD28502439
存储条件：

粉末 Sealed in dry,2-8°C

液体 -20°C:3-6个月-80°C:12个月
溶解度 :

DMSO: 30 mg/mL(48.74 mM)，注意：DMSO长时间开封后，会吸水并导致溶解能力下降，请避免使用长期开封的DMSO
动物实验配方：
生物活性
靶点

  • Integrin
描述 Integrins are cell surface receptors involved in the integration between extracellular and intracellular signals in many biological processes, including cytoskeletal organization and cell adhesion, migration, proliferation, differentiation, and survival. During an immune response, integrins mediate cell adhesion to the extracellular matrix, and cell-cell interactions (e.g., T cell activation), which are central to the pathology of many inflammatory diseases, including dry eye disease (DED)[2]. Lifitegrast is a novel small molecule integrin antagonist that blocks the binding of intercellular adhesion molecule 1 (ICAM-1) to lymphocyte function-associated antigen 1 (LFA-1), thus interrupting the T cell-mediated inflammatory cycle[2]. Lifitegrast demonstrated concentration-dependent inhibition of Jurkat cell attachment with an IC50 value of 2.98 nM, suggesting it to be a potent antagonist of LFA-1/ICAM-1–mediated T-cell binding. Lifitegrast also demonstrated potent concentration-dependent inhibition of superantigen induced inflammatory cytokine release from human PBMCs, particularly the Th1 and Th2 T-cell cytokines, IFN-γ and IL-4, respectively. In normal healthy beagles, lifitegrast was well tolerated at concentrations as high as 10% with no apparent adverse effects on the cornea surface or overall ocular health[3].
实验方案
1mg 5mg 10mg

1 mM

5 mM

10 mM

1.62mL

0.32mL

0.16mL

8.12mL

1.62mL

0.81mL

16.25mL

3.25mL

1.62mL
参考文献

[1]XIIDRA

[2]Perez VL, Pflugfelder SC, Zhang S, Shojaei A, Haque R. Lifitegrast, a Novel Integrin Antagonist for Treatment of Dry Eye Disease. Ocul Surf. 2016 Apr;14(2):207-15. doi: 10.1016/j.jtos.2016.01.001. Epub 2016 Jan 22. PMID: 26807723.

[3]Murphy CJ, Bentley E, Miller PE, McIntyre K, Leatherberry G, Dubielzig R, Giuliano E, Moore CP, Phillips TE, Smith PB, Prescott E, Miller JM, Thomas P, Scagliotti R, Esson D, Gadek T, O'Neill CA. The pharmacologic assessment of a novel lymphocyte function-associated antigen-1 antagonist (SAR 1118) for the treatment of keratoconjunctivitis sicca in dogs. Invest Ophthalmol Vis Sci. 2011 May 16;52(6):3174-80. doi: 10.1167/iovs.09-5078. PMID: 21330663.