Triamterene

製品コードS4080 バッチS408001

印刷

化学情報

Chemical Structure Synonyms SKF8542 Storage
(From the date of receipt)		 3 years -20°C powder
1 years -80°C in solvent
化学式

C12H11N7
分子量 253.26 CAS No. 396-01-0
Solubility (25°C)* 体外 DMSO 5 mg/mL warmed with 50ºC water bath (19.74 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.

溶剤液（一定の濃度）を調合する

生物活性

製品説明 Triamterene (SKF8542) blocks epithelial Na+ channel (ENaC) in a voltage-dependent manner with IC50 of 4.5 μM.
in vitro Triamterene inhibits the epithelial sodium channels on principal cells in the late distal convoluted tubule and collecting tubule, which are responsible for 1-2% of total sodium reabsorption. Triamterene can achieve a modest amount of diuresis by decreasing the osmotic gradient necessary for water reabsorption from lumen to interstitium. Triamterene also has a potassium-sparing effect. Normally, the process of potassium excretion is driven by the electrochemical gradient produced by sodium reabsorption. As sodium is reabsorbed, it leaves a negative potential in the lumen, while producing a positive potential in the principal cell. This potential promotes potassium excretion through apical potassium channels. By inhibiting sodium reabsorption, triamterene also inhibits potassium excretion. [2]
in vivo 4'-hydroxylation of triamterene in humans appears to be mediated exclusively by CYP1A2. Inhibition or induction of CYP1A2 will change the time course of both triamterene and its active phase-II metabolite.[3]

プロトコル(参考用のみ)

キナーゼアッセイ Voltage clamp in Xenopus oocytes
The two-microelectrode voltage-clamp configuration is used to record currents from Xenopus laevis oocytes, 2-8 days after cRNA injection. Recordings are performed at 22 °C using a Geneclamp amplifier, and MacLab D/A converter and software for data acquisition and analysis. The ND 96 solution (control) contained (mM): NaC1 96, KCl 2, CaCl2, 1.8, MgCl2 1, HEPES 5 (titrated with NaOH to pH 7.5). For some experiments the pH of the ND 96 solution is adjusted to either 5.5, 6.5, 8.5 or 9.5, by titration with HCl or NaOH. As indicated below, in some experiments Na+ is replaced by N-methyl-D-glucamine (NMDG) solution.The microelectrodes are filled with 3 M KCl solution and had resistances in the range 0.5-0.9 MΩ. The amplitude of the induced Na+ currents varied considerably, depending on the day of channel expression and the batch of oocytes.

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：

Evolutionary metabolic landscape from preneoplasia to invasive lung adenocarcinoma [ Nat Commun, 2021, 12(1):6479] PubMed: 34759281
Simultaneous Control of Endogenous and User-Defined Genetic Pathways Using Unique ecDHFR Pharmacological Chaperones. [ Cell Chem Biol, 2020, 24 pii: S2451-9456(20)30080-5] PubMed: 32330442

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。

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