Terfenadine

製品コードS4353 バッチS435302

印刷

化学情報

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

C32H41NO2
分子量 471.67 CAS No. 50679-08-8
Solubility (25°C)* 体外 DMSO (warmed with 50ºC water bath) 31 mg/mL (65.72 mM)
Ethanol (warmed with 50ºC water bath) 11 mg/mL (23.32 mM)
Water Insoluble
体内 （毎回新しく調製した物を用意してください）
Clear solution
5% DMSO 95% Corn oil
0.35mg/ml Taking the 1 mL working solution as an example, add 50 μL of 7 mg/ml clear DMSO stock solution to 950 μL of corn oil and mix evenly. The mixed solution should be used immediately for optimal results. 
Clear solution
5%DMSO 40%PEG300 5%Tween80 50%ddH2O
1.55mg/ml Taking the 1 mL working solution as an example, add 50 μL of 31 mg/ml clarified DMSO stock solution to 400 μL of PEG300, mix evenly to clarify it; add 50 μL of Tween80 to the above system, mix evenly to clarify; then continue to add 500 μL of ddH2O to adjust the volume to 1 mL. The mixed solution should be used immediately for optimal results. 
* <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 Terfenadine is an antihistamine, generally completely metabolizes to the active form fexofenadine in the liver by the enzyme cytochrome P450 CYP3A4 isoform. Terfenadine ((±)-Terfenadine) is a potent open-channel blocker of hERG with an IC50 of 204 nM. Terfenadine, an H1 histamine receptor antagonist, acts as a potent apoptosis inducer in melanoma cells through modulation of Ca2+ homeostasis. Terfenadine induces ROS-dependent apoptosis, simultaneously activates Caspase-4, -2, -9.
in vitro

Terfenadine is equipotent to quinidine as a blocker of the delayed rectifier potassium current in isolated feline myocytes. [1] Terfenadine inhibits the human ether-a-go-go related gene (HERG) encoded channels expressed in Xenopus oocytes at nanomolar concentrations in a use- and voltage-dependent fashion. [2] Terfenadine (2 μM) blocks the steady-state maximum current at 0 mV by 65% in Xenopus oocytes. Terfenadine block is dose dependent and equally potent on the maximal steady-state and tail currents, its Kd values are 350 nM and 390 nM, respectively. Terfenadine blocks Kv1.5 (a member of the Kv1 subfamily of voltage-dependent K+ channels) in human atrial myocytes and in the human embryonic kidney cell expression system. Terfenadine (10 μM) produces a dose-dependent block with a 60% reduction of steady-state current in Xenopus oocytes. [3] Terfenadine is oxidated into oxidative N-dealkylation to 4-(hydroxydiphenylmethyl)-piperidine and oxidation of a tert-butyl methyl group to a primary alcohol, which is subsequently oxidized to a carboxylic acid, which is markedly inhibited by gestodene, a selective mechanism-based inactivator of P-450 3A enzymes but not by any of several other P-450 inhibitors. [4] Terfenadine significantly increases action potential duration of guinea pig myocytes. Terfenadine potently blocks the rapidly activating component of the delayed rectifier, IKr, with IC50 values of 1.5 nM and 50 nM, respectively. Terfenadine (10 μM) blocks the slowly activating component of the delayed rectifier, IKs (58.4%), and the inward rectifier, IK1 (20.5%). [5]
in vivo

Terfenadine (1.0 to 3.0 mg/kg, i.v.) significantly prolongs the QTc interval and ventricular effective refractory period in chloralose-anesthetized dogs. [5]

プロトコル(参考用のみ)

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。