Zafirlukast

製品コードS1633 バッチS163303

印刷

化学情報

Chemical Structure Synonyms ICI-204219 Storage
(From the date of receipt)		 3 years -20°C powder
1 years -80°C in solvent
化学式

C31H33N3O6S
分子量 575.68 CAS No. 107753-78-6
Solubility (25°C)* 体外 DMSO 100 mg/mL (173.7 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.

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生物活性

製品説明 Zafirlukast is an oral leukotriene receptor antagonist (LTRA), used to prevent asthma symptoms.
in vitro Zafirlukast is similar to 3-methylindole because it contains an N-methylindole moiety that has a 3-alkyl substituent on the indole ring. Zafirlukast readily forms (10% conversion in 60 min) a GSH adduct with molecular mass of 880 Da upon incubation with horseradish peroxidase. Zafirlukast produces time-, concentration-, and NADP(H)-dependent inactivation of CYP3A4. Zafirlukast is shown to inhibit CYP3A enzyme activity in vitro (nonpreincubation inhibition) with a Ki of 2 μM in one report, but higher values have been published, and our KI for the inactivation process is 13.4 μM. Zafirlukast has high plasma protein binding (>99%), which would lower the free-drug concentration. Zafirlukast undergoes two successive one-electron oxidations to afford a highly electrophilic α,β-unsaturated iminium species, which reacts spontaneously with GSH to yield the observed adduct. [1]
in vivo Zafirlukast is a potent and selective cysteinyl leukotriene receptor antagonist which is used mainly in the prophylaxis of bronchial asthma. Zafirlukast in a dose of 80 mg/kg orally produces a significant decrease in tissue malondialdehyde, myeloperoxidase, and an increase in both reduced glutathione and catalase levels, while there is no significant changes with the rectal route. [2]

プロトコル(参考用のみ)

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：

Inhibition of CysLTR1 reduces the levels of aggregated proteins in retinal pigment epithelial cells [ Sci Rep, 2023, 13(1):13239] PubMed: 37580467
Inhibition of CysLTR1 reduces the levels of aggregated proteins in retinal pigment epithelial cells [ Sci Rep, 2023, 13(1):13239] PubMed: 37580467
Zafirlukast Induces VHL- and HIF-2α-Dependent Oxidative Cell Death in 786-O Clear Cell Renal Carcinoma Cells [ Int J Mol Sci, 2022, 23(7)3567] PubMed: 35408930
Development of potent and selective inhibitors targeting the papain-like protease of SARS-CoV-2 [ Cell Chem Biol, 2021, S2451-9456(21)00213-0] PubMed: 33979649
Chronobiological activity of cysteinyl leukotriene receptor 1 during basal and induced autophagy in the ARPE-19 retinal pigment epithelial cell line [ Aging (Albany NY), 2021, 13(24):25670-25693] PubMed: 34919533
Cysteinyl leukotriene receptor 1 modulates autophagic activity in retinal pigment epithelial cells [ Sci Rep, 2020, 10(1):17659] PubMed: 33077798
Pranlukast is a novel small molecule activator of the two-pore domain potassium channel TREK2. [ Biochem Biophys Res Commun, 2019, 520(1):35-40] PubMed: 31564414

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。