Tenatoprazole

製品コードS4212 バッチS421202

印刷

化学情報

 Chemical Structure Synonyms TU-199,STU-Na Storage
(From the date of receipt)
3 years -20°C powder
1 years -80°C in solvent
化学式

C16H18N4O3S

分子量 346.4 CAS No. 113712-98-4
Solubility (25°C)* 体外 DMSO 69 mg/mL (199.19 mM)
Ethanol (warmed with 50ºC water bath) 31 mg/mL (89.49 mM)
Water Insoluble
体内 (毎回新しく調製した物を用意してください)
Homogeneous suspension
CMC-NA
≥5mg/ml Taking the 1 mL working solution as an example, add 5 mg of this product to 1 ml of CMC-Na solution, mix evenly to obtain a homogeneous suspension with a final concentration of 5 mg/ml.
* <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 Tenatoprazole (TU-199,STU-Na) is a prodrug of the proton pump inhibitor (PPI) class, which inhibits proton transport with IC50 of 3.2 μM. Tenatoprazole labels only the gastric H(+),K(+)-ATPase alpha-subunit, approximately 2.6 nM/mg of tenatoprazole is bound to the H(+),K(+)-ATPase.
in vitro

Tenatoprazole labeled only the gastric H+,K+-ATPase alpha-subunit as has been found for other PPIs, approximately 2.6 nmol/mg of this compound is bound to the H+,K+-ATPase. The two enantiomers (R)- or (S)-tenatoprazole give the same stoichiometry of binding with 88% inhibition. This compound labels only the peptide containing fifth and sixth transmembrane segments, these contain two cysteines, cysteine 813 in the luminal vestibule and cysteine 822 in the sixth transmembrane domain. [1]

in vivo

Tenatoprazole provides slow activation in vivo, which is predicted by its chemical activation rate in fasting rats. This compound inhibits about 20–30% of enzyme activity even though acid secretion in fasting rats. This chemical provides a higher Cmax of 183 ng/mL, Tmax of 1.3 hours and AUC of 822 ng*h/mL in dog. [1]

プロトコル(参考用のみ)

参考

  • https://pubmed.ncbi.nlm.nih.gov/16405921/

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:

Tsg101 UEV Interaction with Nedd4 HECT Relieves E3 Ligase Auto-Inhibition, Promoting HIV-1 Assembly and CA-SP1 Maturation Cleavage [ Viruses, 2024, 16(10)1566] PubMed: 39459900
Ilaprazole and other novel prazole-based compounds that bind Tsg101 inhibit viral budding of HSV-1/2 and HIV from cells [ J Virol, 2021, JVI.00190-21] PubMed: 33731460

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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