Pyrilamine Maleate

製品コードS4382 バッチS438203

印刷

化学情報

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

C17H23N3O1.C4H4O4
分子量 401.46 CAS No. 59-33-6
Solubility (25°C)* 体外 DMSO 80 mg/mL warmed with 50ºC water bath (199.27 mM)
Water 80 mg/mL (199.27 mM)
Ethanol 80 mg/mL warmed with 50ºC water bath (199.27 mM)
* <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 Pyrilamine Maleate (Mepyramine) is a histamine H1 receptor inverse agonist, it binds to a G protein-coupled form of the receptor and promotes a G protein-coupled inactive state of the H1 receptor that interferes with the Gq/11-mediated signaling.
in vitro Pyrilamine blocks the rapidly activating component of the delayed rectifier, IKr, with IC50 of 1.1 μM. Pyrilamine (10 μM) blocks the slowly activating component of the delayed rectifier, IKs and the inward rectifier, IK1 less than 20%. [1]
in vivo Pyrilamine (15 mg/kg/day) significantly decreases the movement time and velocity, as well as the total food consumption and completely abolishes the circadian rhythmicity of locomotion in sham-operated rats. Pyrilamine (15 mg/kg/day) leads to the complete blockade of H(1) receptors in both sham- and portacaval anastomosis-operated rats. [2] Pyrilamine decreases the number of flinches in a dose dependent manner and decreases c-fos mRNA expression in lumbar spinal cord of rats. [3] Pyrilamine is mainly metabolited into the O-glucuronic acid conjugate of O-demethyl pyrilamine in the rats. The terminal plasma elimination half-life of Pyrilamine does not increase with increasing doses (2.3 hours, 0.7 mg/kg; 1.5 hours, 7.0 mg/kg) and thus pyrilamine does not exhibit dose-dependent elimination. [4] Pyrilamine is slightly less mutagenic than Methapyrilene over a comparable range of concentrations, and also induces predominantly small-colony mutants in the L5178Y/TK +/- mouse lymphoma assay. [5]

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：

Critical role of mitogen-inducible gene 6 in restraining endothelial cell permeability to maintain vascular homeostasis [ J Cell Commun Signal, 2023, 17(1):151-165] PubMed: 36284029

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。