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).
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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。 |
靶点 |
|
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]. |
Dose | Rat: 10 mg/kg[2] (i.v.) | ||||||||||
Administration | i.v. | ||||||||||
Pharmacokinetics |
|
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 |
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 |