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Vonoprazan Fumarate (TAK438) 是质子泵的有效抑制剂,是口服有效的高效钾竞争性酸阻断剂,具有抗分泌活性。在 pH 为 6.5 时,它抑制猪胃微粒体中的 H+,K+-ATPase 酶活性,IC50为 19 nM。它被开发用于研究酸相关疾病,如消化性溃疡和胃食管反流病。
Vonoprazan Fumarate (TAK438) 是质子泵的有效抑制剂,是口服有效的高效钾竞争性酸阻断剂,具有抗分泌活性。在 pH 为 6.5 时,它抑制猪胃微粒体中的 H+,K+-ATPase 酶活性,IC50为 19 nM。它被开发用于研究酸相关疾病,如消化性溃疡和胃食管反流病。
规格 | 价格 | 库存 | 数量 |
---|---|---|---|
25 mg | ¥ 113 | 现货 | |
50 mg | ¥ 148 | 现货 | |
100 mg | ¥ 198 | 现货 | |
500 mg | ¥ 413 | 现货 | |
1 g | ¥ 588 | 现货 | |
5 g | ¥ 1,470 | 现货 |
产品描述 | Vonoprazan Fumarate (TAK438) , a novel potassium-competitive acid blocker, inhibits gastric acid secretion. Vonoprazan Fumarate (TAK438) inhibited H+,K+-ATPase activity in porcine gastric microsomes with IC50 value of 19 nM at pH 6.5. |
靶点活性 | H+, K+-ATPase:19 nM |
体外活性 | 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[4]. |
体内活性 | 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[4]. |
别名 | 富马酸沃诺拉赞, Vonoprazan Fumurate, TAK-438, TAK438, TAK 438 |
分子量 | 461.46 |
分子式 | C21H20FN3O6S |
CAS No. | 881681-01-2 |
Smiles | OC(=O)\C=C\C(O)=O.CNCc1cc(-c2ccccc2F)n(c1)S(=O)(=O)c1cccnc1 |
密度 | no data available |
存储 | Powder: -20°C for 3 years | In solvent: -80°C for 1 year | Shipping with blue ice. | ||||||||||||||||||||
溶解度信息 | DMSO: 4.61 mg/mL (10 mM), Sonication is recommended. | ||||||||||||||||||||
溶液配制表 | |||||||||||||||||||||
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