Lifitegrast

製品コードS3714 バッチS371402

化学情報

	Synonyms	SAR1118,SHP-606	Storage (From the date of receipt)	3 years -20°C powder 1 years -80°C in solvent
	化学式	C₂₉H₂₄Cl₂N₂O₇S
	分子量	615.48	CAS No.	1025967-78-5
Solubility (25°C)*	体外	DMSO	14 mg/mL (22.74 mM)
		Water	Insoluble
		Ethanol	Insoluble
* <1 mg/ml means slightly soluble or insoluble. * Please note that Selleck tests the solubility of all compounds in-house, and the actual solubility may differ slightly from published values. This is normal and is due to slight batch-to-batch variations.

溶剤液（一定の濃度）を調合する

生物活性

製品説明	Lifitegrast (SAR1118,SHP-606) is a novel small molecule integrin antagonist that inhibits a specific T cell-mediated inflammatory pathway involved in the pathogenesis of DED.
in vitro	Lifitegrast inhibits release of cytokines, interferon d, tumor necrosis factor alpha (TNF-α), and other interleukins (ILs). It is a novel integrin antagonist which prevents LFA-1/ICAM-1 interaction preventing T-cell activation/recruitment and release of inflammatory mediators, thereby decreasing the inflammatory responses in DED^[1].
in vivo	In vivo study of lifitegrast as radiolabeled drops in rats demonstrated that it was rapidly distributed in ocular and periocular tissues, cleared by normal tear drainage, and was devoid of systemic side effects. A similar dose tolerability study of lifitegrast in dogs suffering from keratoconjunctivitis sicca proved its efficacy and safety. Lifitegrast is found to be a highly potent drug in various clinical trials as it alleviates both the signs and symptoms of DED, which showed rapid onset of action and good therapeutic efficacy as ophthalmic drops. It protected the corneal surfaces and was well tolerated locally as well as systemically^[1].

プロトコル(参考用のみ)

参考

[1] Afroz Abidi, et al. J Pharmacol Pharmacother. 2016, 7(4): 194–198.

Selleckの高級品が、幾つかの出版された研究調査結果（以下を含む）で使われた：

Dihydroergotamine ameliorates liver fibrosis by targeting transforming growth factor β type II receptor [ World J Gastroenterol, 2023, 29(20):3103-3118]	PubMed: 37346154
Design, synthesis, and LFA-1/ICAM-1 antagonist activity evaluation of Lifitegrast analogues [ Med Chem Res, 2022, 31(4):555-579]	PubMed: 35194364
Repurposing of FDA approved drugs against Salmonella enteric serovar Typhi by targeting dihydrofolate reductase: an in silico study [ J Biomol Struct Dyn, 2020, 1-14]	PubMed: 33251976

長期の保管のために-20°Cの下で製品を保ってください。

人間や獣医の診断であるか治療的な使用のためにでない。

各々の製品のための特定の保管と取扱い情報は、製品データシートの上で示されます。大部分のSelleck製品は、推薦された状況の下で安定です。製品は、推薦された保管温度と異なる温度で、時々出荷されます。長期の保管のために必要とされてそれと異なる温度で、多くの製品は、短期もので安定です。品質を維持するが、夜通しの積荷のために最も経済的な貯蔵状況を用いてあなたの送料を保存する状況の下に、製品が出荷されることを、我々は確実とします。製品の受領と同時に、製品データシートの上で貯蔵推薦に従ってください。