Tripelennamine HCl

製品コードS3146 バッチS314601

印刷

化学情報

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

C16H21N3.HCl
分子量 291.82 CAS No. 154-69-8
Solubility (25°C)* 体外 Water 58 mg/mL (198.75 mM)
DMSO 2 mg/mL (6.85 mM)
Ethanol 1 mg/mL (3.42 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 Tripelennamine (Pyribenzamine) is a widely used H1 antagonist, inhibiting PhIP glucuronidation with IC50 of 30 μM.
in vitro Tripelennamine is a substrate for a tertiary amine UDP-glucuronosyltransferases which catalyzes the formation of quaternary ammonium-linked glucuronides. Tripelennamine inhibits the glucuronidation of 2-amino-1-methyl-6-phenylimidazo[4,5-b] pyridine (PhIP) by a mixture of competitive and noncompetitive inhibition in both human and rabbit liver microsomes. [1] Vibrations of the aminopyridine chromophore in Tripelennamine at neutral pH, where the aminoalkyl chain is protonated, are modified when compared to the vibrational pattern recorded for a fully neutral molecule in alkaline solution. [2]
in vivo Tripelennamine HCl (i.v.) causes central nervous system (CNS) excitement in standing horses, and the horses became very alert, agitated, and uncomfortable, as indicated by their raising the head and tightening the neck muscles, excessive rapid movements of eyes and ears, biting, snorting, briskly swishing the tail, and stomping and pawing with front feet. Accordingly, hemoglobin concentration of standing horses increase significantly after Tripelennamine HCl treatment. Tripelennamine HCl (i.v.) significantly increases mixed venous blood O2 tension and hemoglobin-O2 saturation in standing horse, as well as arterial and mixed-venous blood O2 contents, but the arterial-to-mixed-venous O2 content gradient of standing horses is not significantly affected. [3] Tripelennamine HCl (0.5 mg/kg i.v.) administrated both in horses and camels results in the terminal elimination half-lives of 2.39 and 2.08 hours, total body clearances of 0.97 and 0.84 L/h/kg. The volumes of distribution at steady state are 2.87 and 1.69 L/kg, the volumes of the central compartment of the two compartment pharmacokinetic model are 1.75 and 1.06 L/kg. [4]

プロトコル(参考用のみ)

キナーゼアッセイ Enzyme assay
The extent of PhIP glucuronidation is measured using microsomes (1-2 mg/mL) suspended in 0.5 M Tris acetate buffer (pH 8.0), containing 0.5 mM MgCl2, 0.5 mM [14C]PhIP, and 5 mM UDP-glucuronic acid. Blank reaction mixtures do not receive UDP-glucuronic acid and/or use boiled microsomes. Reaction mixtures (200 μL) are incubated at 37 ℃ for 60 min, whereupon each reaction is terminated with the addition of 5 mL of ethyl acetate followed by 2 mL of H2O. Product formation is linear with time through 120 min, and with protein concentration up to 4 mg/mL. In cases where HPLC analysis is performed, reactions are stopped with ice-cold ethanol, and protein is precipitated by centrifugation at 1×104g for 10 min at room temperature. The supernatant fraction is then directly applied to HPLC. Otherwise, reaction mixtures are shaken for 10 min and centrifuged for 5 min at 2×103 rpm at room temperature. The organic phase, which contained the unconjugated PhIP, is removed, and the extraction is repeated two more times with 5 mL of fresh ethyl acetate each time. The aqueous phase (0.5 mL) is added to 10 mL of Scintiverse, and radioactivity is measured using liquid scintillation analysis.

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。