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立他司特 /Lifitegrast {[allProObj[0].p_purity_real_show]}

货号:A113895 同义名: 利非司特 / SAR 1118;SHP-606

Lifitegrast is a novel small molecule integrin antagonist which can inhibit an integrin, lymphocyte function-associated antigen 1 (LFA-1), from binding to intercellular adhesion molecule 1 (ICAM-1).

Lifitegrast 化学结构 CAS号:1025967-78-5
Lifitegrast 化学结构
CAS号:1025967-78-5
Lifitegrast 3D分子结构
CAS号:1025967-78-5
Lifitegrast 化学结构 CAS号:1025967-78-5
Lifitegrast 3D分子结构 CAS号:1025967-78-5
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Lifitegrast 纯度/质量文件 产品仅供科研

货号:A113895 标准纯度: {[allProObj[0].p_purity_real_show]}
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产品名称 Integrin 其他靶点 纯度
Tirofiban 99%+
ATN-161 98%
RGD 98%
A-205804 ++

ICAM-1, IC50: 25 nM

E-selectin, IC50: 20 nM

98%
SB-273005 ++++

αvβ3 receptor, IC50: 1.2 nM

αvβ5 receptor, IC50: 0.3 nM

98+%
Lifitegrast 97%
Cilengitide TFA +++

αvβ3 receptor, IC50: 4.1 nM

αvβ5 receptor, IC50: 79 nM

99%+
Cyclo(-RGDfK) TFA 99%+
Cyclo(RGDyK) trifluoroacetate ++

αVβ3 integrin, IC50: 20 nM

99%+
1. 鼠标悬停在“+”上可以显示相关IC50的具体数值。"+"越多,抑制作用越强。2. "✔"表示该化合物对相应的亚型有抑制作用,但抑制强度暂时没有相关数据。

Lifitegrast 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].

Lifitegrast 动物研究

Dose Rat: 10 mg/kg[2] (i.v.)
Administration i.v.
Pharmacokinetics
Animal Rats[2]
Dose 10 mg/eye
Administration i.v.
T1/2β 36.2 h (male)
40.7 h (female)
Vd 21.2 L/kg (male)
21.3 L/kg (female)

Lifitegrast 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.

Lifitegrast 实验方案

计算器
存储液制备 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

Lifitegrast 技术信息

CAS号1025967-78-5
分子式C29H24Cl2N2O7S
分子量 615.481
别名 利非司特 ;SAR 1118;SHP-606
运输蓝冰
存储条件

液体 -20°C:3-6个月-80°C:12个月

粉末 Sealed in dry,2-8°C

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
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