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Vonoprazan Fumarate
CAS No. 881681-01-2
Vonoprazan Fumarate ( TAK-438 | TAK 438 | TAK438 | Vonoprazan Fumurate )
产品货号. M27383 CAS No. 881681-01-2
Vonoprazan Fumurate 是一种新型钾竞争性酸阻滞剂，可抑制胃酸分泌。 Vonoprazan Fumurate 抑制猪胃微粒体中的 H+,K+-ATPase 活性，pH 6.5 时的 IC50 值为 19 nM。
纯度: >98% (HPLC)
COA
Datasheet
HNMR
HPLC
MSDS
Handing Instructions
| 规格 | 价格/人民币 | 库存 | 数量 |
| 100MG | ￥332 | 有现货 |
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| 200MG | ￥527 | 有现货 |
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| 500MG | ￥1142 | 有现货 |
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| 1G | 获取报价 | 有现货 |
|
生物学信息
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产品名称Vonoprazan Fumarate
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注意事项本公司产品仅用于科研实验，不得用于人体或动物的临床与诊断
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产品简述Vonoprazan Fumurate 是一种新型钾竞争性酸阻滞剂，可抑制胃酸分泌。 Vonoprazan Fumurate 抑制猪胃微粒体中的 H+,K+-ATPase 活性，pH 6.5 时的 IC50 值为 19 nM。
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产品描述Vonoprazan Fumurate, a novel potassium-competitive acid blocker, inhibits gastric acid secretion. Vonoprazan Fumurate inhibited H+,K+-ATPase activity in porcine gastric microsomes with IC50 value of 19 nM at pH 6.5.(In Vitro):The inhibitory activity of Vonoprazan Fumurate was unaffected by ambient pH. The inhibition by Vonoprazan Fumurate was reversible and achieved in a K(+)-competitive manner, quite different from that by lansoprazole. Vonoprazan Fumurate exhibits porcine gastric H+ ,K+-ATPase activity in a concentration-dependent manner.(In Vivo):Vonoprazan Fumurate, at a dose of 4 mg/kg (as the free base) orally, completely inhibited basal and 2-deoxy-d-glucose-stimulated gastric acid secretion in rats, and its effect on both was stronger than that of lansoprazole. Vonoprazan Fumurate increased the pH of gastric perfusate to a higher value than did lansoprazole or SCH28080, and the effect of Vonoprazan Fumurate was sustained longer than that of lansoprazole or SCH28080.
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体外实验Vonoprazan (0.1 nM-10 μM; 30 minutes) exhibits porcine gastric H+ ,K+-ATPase activity in a concentration-dependent manner.Vonoprazan does not inhibit Na+,K+-ATPase activity, even at concentrations 500 times higher than their IC50 values against gastric H+,K+-ATPase activity.
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体内实验Vonoprazan (1-4 mg/kg; p.o.) completely inhibits basal and 2-deoxy-D-glucose (2DG, 200 mg/kg s.c.)-stimulated gastric acid secretion at the 4 mg/kg dose in rats. Animal Model:Male 7- or 8-week-old Sprague-Dawley rat Dosage:0.5, 1, 2, and 4 mg/kg.Administration:Oral administration Result:Inhibited basal gastric acid secretion in a dose-dependent manner.
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同义词TAK-438 | TAK 438 | TAK438 | Vonoprazan Fumurate
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通路Membrane Transporter/Ion Channel
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靶点Proton Pump
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受体Antiviral
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研究领域——
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适应症——
化学信息
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CAS Number881681-01-2
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分子量461.46
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分子式C21H20FN3O6S
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纯度>98% (HPLC)
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溶解度In Vitro:?DMSO : 50 mg/mL (108.35 mM)
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SMILESOC(=O)\C=C\C(O)=O.CNCc1cc(-c2ccccc2F)n(c1)S(=O)(=O)c1cccnc1
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化学全称——
运输与储存
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储存条件(-20℃)
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运输条件With Ice Pack
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稳定性≥ 2 years
参考文献
1.Yu W, Goddard C, Clearfield E, Mills C, Xiao T, Guo H, Morrey JD, Motter NE, Zhao K, Block TM, Cuconati A, Xu X. Design, synthesis, and biological evaluation of triazolo-pyrimidine derivatives as novel inhibitors of hepatitis B virus surface antigen (HBsAg) secretion. J Med Chem. 2011 Aug 25;54(16):5660-70. doi: 10.1021/jm200696v. Epub 2011 Aug 2. PubMed PMID: 21786803; PubMed Central PMCID: PMC3158247.
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