| CAS |
No.1025967-78-5 |
| 中文名称 |
立他司特 |
| 英文名称 |
Lifitegrast |
| 别名 |
SAR-1118 |
| 分子式 |
C29H24Cl2N2O7S |
| 分子量 |
615.48 |
| 溶解性 |
Soluble in DMSO |
| 纯度 |
≥98% |
| 外观(性状) |
White to off-white Solid |
| 储存条件 |
Powder:-20℃，2 years;Insolvent(母液):-20℃，6 months;-80℃，1 year |
| EC |
EINECS 813-044-8 |
| MDL |
MFCD28502439 |
| 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 |
| 靶点 |
Integrin |
| 通路 |
Cytoskeleton |
| 背景说明 |
Lifitegrast是一种新型的integrin拮抗剂。 |
| 生物活性 |
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[1]. |
| In Vitro |
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]. |
| In Vivo |
Lifitegrast(SAR 1118)，has potent anti-inflammatory activity on corneal inflammation induced by antibiotic-killed P. aeruginosa and S. aureus in the presence of a silicone hydrogel lens with the optimal application being a 1% solution applied either 2 or 3 times prior[2]. |
| 动物实验 |
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]. |
| 数据来源文献 |
[1]. Perez VL， et al. Lifitegrast， a Novel Integrin Antagonist for Treatment of Dry Eye Disease. Ocul Surf. 2016 Apr;14(2):207-15.
[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. |
| 规格 |
1mg 5mg 10mg 25mg 50mg |
| 单位 |
瓶 |
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