Azatadine dimaleate

製品コードS3186 バッチS318601

印刷

化学情報

Chemical Structure Synonyms SCH10649,Azatadine Maleate Storage
(From the date of receipt)		 3 years -20°C powder
1 years -80°C in solvent
化学式

C20H22N2.2C4H4O4
分子量 522.55 CAS No. 3978-86-7
Solubility (25°C)* 体外 DMSO 105 mg/mL (200.93 mM)
Water 105 mg/mL (200.93 mM)
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 Azatadine (SCH10649,Azatadine Maleate) is an histamine and cholinergic inhibitor with IC50 of 6.5 nM and 10 nM, respectively.
in vitro

95% of Azatadine is biotransformed in Sabouraud dextrose broth within 72 hours treatment with two major metabolites, 7-hydroxyazatadine (25%) and 8-hydroxyazatadine (50%), and two minor metabolites, N-desmethylazatadine and 9-hydroxyazatadine. [2]
in vivo

Azatadine delays the onset of dyspnea-induced by aerosolized histamine, acetylcholine and serotonin in the conscious guinea-pig with PD50 of 0.01 mg/kg, 0.739 mg/kg and 0.86 mg/kg. Azatadine protects conscious guinea-pigs against death induced by the intravenous injection of histamine with oral PD50 of 0.009 mg/kg in guinea-pig and 0.22 mg/kg in mice. [1] Following a single oral dose of Azatadine (4 mg) in fasted volunteers, a Cmax of 3 μg/L has been measured by RIA 4.2 hours after administration. Azatadine is almost completely metabolised by hydroxylation, demethylation and formation of zwitterion isomers by oxidative ring opening. Azatadine (8.8 mg oral) in healthy volunteers results in a Csub>max of 5.9 μg/L at 5.3 hours after treatment and bioavailability of 80%. [3] Azatadine (1 mg twice daily for 14 days) is effective in relieving the histamine-mediated symptoms of seasonal allergic rhinitis. [4]

プロトコル(参考用のみ)

キナーゼアッセイ Binding assay
Drug-receptor interactions are performed to determine the nature of the antagonism of histamine, acetylcholine and serotonin by Azatadine. Agonists are added to the bath in 0.05 mL volumes and allowed to act for 45 seconds before increasing log doses are given. Azatadine is added to the bath in volumes between 0.1 mL-0.3 mL and allowed to remain for 3 minutes before initial challenges with the agonists. The log shift at the ED50 is calculated and this data is analyzed statistically by paired t-tests on the log shifts.

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：

Bucillamine Prevents Afatinib-Mediated Inhibition of Epidermal Growth Factor Receptor Signaling. [ Pharmaceuticals (Basel), 2019, 12(4)] PubMed: 31703435

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。