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Tenatoprazole(TU-199)
本产品不向个人销售,仅用作科学研究,不用于任何人体实验及非科研性质的动物实验。
Tenatoprazole(TU-199)图片
CAS NO:113712-98-4
规格:≥98%
包装与价格:
包装价格(元)
10mg电议
25mg电议
50mg电议
100mg电议
250mg电议
500mg电议
1g电议

产品介绍
理化性质和储存条件
Molecular Weight (MW)346.4
FormulaC16H18N4O3S
CAS No.113712-98-4
Storage-20℃ for 3 years in powder form
-80℃ for 2 years in solvent
Solubility (In vitro)DMSO: 46 mg/mL (132.8 mM)
Water:<1 mg/mL
Ethanol: 14 mg/mL (40.4 mM)
Other info

Chemical Name: 5-methoxy-2-[(4-methoxy-3,5-dimethylpyridin-2-yl)methylsulfinyl]-1H-imidazo[4,5-b]pyridine

InChi Key: ZBFDAUIVDSSISP-UHFFFAOYSA-N

InChi Code: InChI=1S/C16H18N4O3S/c1-9-7-17-12(10(2)14(9)23-4)8-24(21)16-18-11-5-6-13(22-3)19-15(11)20-16/h5-7H,8H2,1-4H3,(H,18,19,20)

SMILES Code: O=S(C1=NC2=NC(OC)=CC=C2N1)CC3=NC=C(C)C(OC)=C3C

Synonyms

TU199; Tenatoprazole; TU-199; TU 199; Ulsacare; Protop

实验参考方法
In Vitro

In vitro activity: Tenatoprazole labeled only the gastric H+,K+-ATPase alpha-subunit as has been found for other PPIs, approximately 2.6 nmol/mg of tenatoprazole is bound to the H+,K+-ATPase. The two enantiomers (R)- or (S)-tenatoprazole give the same stoichiometry of binding with 88% inhibition. Tenatoprazole 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.


Kinase Assay: The enzyme suspension (20 mg/mL) is incubated at 37°C in a buffer composed of 5 mM Pipes/Tris (pH 6.95), 2 mM MgCl2, 150 mM KCl, 3 mg/mL of valinomycin, 1 mM acridine orange, in the presence of 0.1 mM glutathione, in a SPEX spectrofluorometer for 5 min. Inhibitor (20 mM), omeprazole or tenatoprazole, is added and fluorescence is measured by excitation at 490 nm and emission at 530 nm. After 60 s, ATP (2 mM) is added to initiate acridine orange uptake as a measure of intra-vesicular acidification.

In VivoTenatoprazole provides slow activation in vivo, which is predicted by its chemical activation rate in fasting rats. Tenatoprazole inhibits about 20–30% of enzyme activity even though acid secretion in fasting rats. (S)-tenatoprazole sodium salt hydrate provides a higher Cmax of 183 ng/mL, Tmax of 1.3 hours and AUC of 822 ng*h/mL in dog.
Animal modelRats and dogs
Formulation & Dosage
References

Biochem Pharmacol. 2006 Mar 14;71(6):837-49.