Lifitegrast|1025967-78-5|(立他司特; SAR 1118; SHP-606)-陌孚医药/Medlife

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Lifitegrast (Synonyms: 立他司特; SAR 1118; SHP-606)

目录号: PL14867 纯度: ≥99%

CAS No. :1025967-78-5

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中文名称	Lifitegrast
中文别名	立他司特;利菲司特;利非司特;立他斯特杂质;(S)-2-[2-(苯并呋喃-6-羰基)-5,7-二氯-1,2,3,4-四氢异喹啉-6-甲酰胺基]-3-(3-甲磺酰基苯基)丙酸
英文名称	Lifitegrast
英文别名	(S)-2-(2-(Benzofuran-6-carbonyl)-5,7-dichloro-1,2,3,4-tetrahydroisoquinoline-6-carboxamido)-3-(3-(methylsulfonyl)phenyl)propanoic acid;1-(Pyrimidin-2-yl)cyclopropanamine hydrochloride;lifitegrast;Lifitegrast(SAR 1118);SAR 1118;SAR-1118;N-[[2-(6-Benzofuranylcarbonyl)-5,7-dichloro-1,2,3,4-tetrahydro-6-isoquinolinyl]carbonyl]-3-(methylsulfonyl)-L-phenylalanine;liftegrast;Lifitegrast, SAR 1118;L-Phenylalanine,N-[[2-(6-benzofuranylcarbonyl)-5,7-dichloro-1,2,3,4-tetrahydro-6-isoquinolinyl]carbonyl]-3-(methylsulfonyl)-;(S)-2-(2-(benzofuran-6-carbonyl)-5,7-dichloro-1,2,3,4-tetrahydroisoquinoline-6-carboxamido)-3-(3-(methylsulfonyl)phenyl)propanoic;Xiidra;SAR1118;038E5L962W;(S)-2-(2-(benzofuran-6-carbonyl)-5,7-dichloro-1,2,3,4-tetrahydroisoquinoline-6-carboxamido)-3-(3-(methylsulfonyl)phenyl)propanoic acid;(S)-2-(2-(benzofuran-6-carbonyl)-5,7-dichloro-1,2,3,4-tetrahydroisoquinoline-6-carboxamido)-3-(3-(methylsulfonyl)phenyl)propanoic a;Lifitegrast
Cas No.	1025967-78-5
分子式	C₂₉H₂₄Cl₂N₂O₇S
分子量	615.48
包装储存	Powder -20°C 3 years；4°C 2 years

产品详情

Lifitegrast (SAR 1118) 是一种有效的整合素 (integrin) 拮抗剂。Lifitegrast 阻断细胞间粘附分子1 (ICAM-1) 与淋巴细胞功能相关抗原 (LFA-1) 的结合，中断 T 细胞介导的炎症周期。 Lifitegrast 抑制 Jurkat T 细胞附着于 ICAM-1 的 IC₅₀ 为 2.98 nM。Lifitegrast 可用于干眼症的研究。

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 IC 50 of 2.98 nM. Lifitegrast can be used for researching dry eye disease.

性状

Solid

IC50 & Target[1][2]

αLβ2

体外研究(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.
Lifitegrast strongly inhibits Jurkat T cell attachment to ICAM-1 with an IC50 of 2.98 nM. has not independently confirmed the accuracy of these methods. They are for reference only.

体内研究(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.
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. has not independently confirmed the accuracy of these methods. They are for reference only.

运输条件

Room temperature in continental US; may vary elsewhere.

储存方式

Powder -20°C 3 years；4°C 2 years

ClinicalTrial

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.
[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.
[3]. Rao VR, et al. Delivery of SAR 1

溶解度数据	In Vitro: DMSO : ≥ 29 mg/mL (47.12 mM)配制储备液

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Data Sheet

1：一般建议：溶解度为Medlife测试数据，可能与文献描述存在差异。这是由于生产工艺和批次不同产生的正常现象。为了使其更好的溶解，请用37℃加热试管并在超声波水浴中震动片刻。不同批次产品溶解度各有差异，仅做参考，具体以实验方案为准。

2：储存条件：粉末-20°C一般情况可以保存3年，溶于溶剂-80°C一般情况可以保存1年。不同产品及不同批次产品可能存在差异，请细致阅读产品信息，并辅助参考相关文献描述。

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