| Description | Vonoprazan fumarate (TAK-438) is a novel P-CAB (potassium-competitive acid blocker) that reversibly inhibits H+/K+, ATPase. |
| In vitro | TAK-438对大鼠和狗的组胺刺激的胃酸分泌显示出有效和更持久的抑制作用.TAK-438通过胃组织的高积累和低清除力表现出显著的抗分泌活性.与PPIs不同,TAK-438不受胃分泌状态的影响.TAK-438以剂量依赖性方式抑制基础胃酸分泌,ID50值为1.26 mg/kg.静脉注射TAK-438剂量依赖性地增加胃灌注液的pH值,并且在施用后5小时内pH的增加持续.用1 mg/kg TAK-438处理,90分钟后,pH值达到稳定状态,最高pH值为5.9. |
| In vivo | TAK-438以浓度依赖性方式抑制胃H+,K+-ATP酶活性。在中性条件下（pH 7.5）,TAK-438的抑制活性几乎与弱酸性条件（pH 6.5）下的抑制活性相同。 即使浓度高于它们对胃H+,K+-ATP-ATPase活性的IC50值500倍,TAK-438也不抑制Na+,K+ -ATPase活性。TAK-438以3 nM的Ki以K+竞争性方式抑制胃H+,K+-ATP酶。 |
| Target activity | H+, K+-ATPase:19 nM |
| Synonyms | 富马酸沃诺拉赞, TAK-438 |
| molecular weight | 461.46 |
| Molecular formula | C17H16FN3O2S·C4H4O4 |
| CAS | 1260141-27-2 |
| Storage | Powder: -20°C for 3 years | In solvent: -80°C for 1 year |
| Solubility | Ethanol: < 1 mg/mL (insoluble or slightly soluble) DMSO: 16.67 mg/mL (36.12 mM), Sonication is recommended. H2O: < 1 mg/mL (insoluble or slightly soluble) |
| References | 1. Arikawa Y, et al. J Med Chem, 2012, 55(9), 4446-4456. 2. Hori Y, et al. J Pharmacol Exp Ther, 2010, 335(1), 231-238. 3. Hori Y, et al. J Pharmacol Exp Ther, 2011, 337(3), 797-804. |