TAK-438 free base

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

一种新型强效口服钾竞争性酸阻滞剂 (P-CAB)，可有效抑制 H+,K+-ATP 酶，IC50 为 19 nM。

A novel potent, oral potassium-competitive acid blocker (P-CAB) that potently inhibits H+,K+-ATPase with IC50 of 19 nM; completely inhibits basal and 2-deoxy-d-glucose-stimulated gastric acid secretion in rats (4mg/kg, p.o.); increases the pH of gastric perfusate to a higher value, and sustains longer than those of lansoprazole or SCH28080; a clinical candidate for the treatment of gastroesophageal reflux disease (GERD), peptic ulcer, and other acid-related diseases.Ulcer Phase 3 Clinical(In Vitro):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.(In Vivo):Vonoprazan (1-4 mg/kg; p.o.) completely inhibits basal and 2-deoxy-D-glucose (200 mg/kg; s.c.)-stimulated gastric acid secretion at the 4 mg/kg dose in rats.

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.

Vonoprazan (1-4 mg/kg; p.o.) completely inhibits basal and 2-deoxy-D-glucose (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 mg/kg, 1 mg/kg, 2 mg/kg, 4 mg/kg Administration:Oral administration Result:Inhibited basal gastric acid secretion in a dose-dependent manner.

Vonoprazan | TAK438 free base

Membrane Transporter/Ion Channel

Proton Pump

Proton Pump

Other Indications

Ulcer

881681-00-1

345.3912

C17H16FN3O2S

>98% (HPLC)

DMSO: ≥ 33 mg/mL

CNCC1=CN(C(=C1)C2=CC=CC=C2F)S(=O)(=O)C3=CN=CC=C3

1H-Pyrrole-3-methanamine, 5-(2-fluorophenyl)-N-methyl-1-(3-pyridinylsulfonyl)-

(-20℃)

With Ice Pack

≥ 2 years