Description |
P-CAB agent 2 is a potent and orally active potassium-competitive acid blocker and a gastric acid secretion inhibitor. P-CAB agent 2 inhibits H+/K+-ATPase activity with an IC50 value of <100 nM. P-CAB agent 2 inhibits the hERG potassium channel with an IC50 value of 18.69 M. P-CAB agent 2 shows no acute toxicity and inhibits histamine (HY-B1204)-induced gastric acid secretion[1].
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Related Catalog |
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In Vitro |
P-CAB agent 2 (100 µM) 抑制 hERG 钾通道,抑制率为 86.21%,IC50 值为 18.69 M[1]< /sup>。
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In Vivo |
P-CAB agent 2 (example 1) 抑制组胺 (histamine (HY-B1204)) 诱导的 SD 大鼠胃酸分泌[1]. P-CAB agent 2 (600, 2000 mg/kg; p.o.; once) 无急性毒性,600mg/kg 对 SD 大鼠动物体重无显着影响[1]。 Animal Model: 180-220 g, SPF grade, male SD rats[1] Dosage: 2 mg/kg Administration: P.o.; once Result: Inhibited histamine-induced gastric acid secretion with the acid suppression rate of 55.4%.
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References |
[1]. YinLin Qin, et al. Pyrrole sulfonyl derivative, and preparation method and medical use thereof. WO2016119505A1.
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