TAK-438

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

一种新型强效钾竞争性酸阻断剂 (P-CAB)，可抑制猪胃微粒体中的 H(+),K(+)-ATP 酶活性，pH 6.5 时 IC50 为 19 nM。

A novel potent, potassium-competitive acid blocker (P-CAB) that inhibits H(+),K(+)-ATPase activity in porcine gastric microsomes with IC50 of 19 nM at pH 6.5; the inhibitory activity of TAK-438 is unaffected by ambient pH, but not SCH28080 and lansoprazole; completely inhibits basal and 2-deoxy-d-glucose-stimulated gastric acid secretion in rats at 4 mg/kg (as the free base) orally; a more potent and longer-lasting inhibitory action on gastric acid secretion than either lansoprazole or SCH28080.Ulcer Approved(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 (2DG, 200 mg/kg s.c.)-stimulated gastric acid secretion at the 4 mg/kg dose in rats.

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TAK 438 | TAK438 | Vonoprazan

Membrane Transporter/Ion Channel

Proton Pump

H+/K+-ATPase

Other Indications

Ulcer

1260141-27-2

461.464

C21H20FN3O6S

>98% (HPLC)

DMSO: 58 mg/mL (125.7 mM); Ethanol: <1 mg/mL; Water: <1 mg/mL （ < 1 mg/ml refers to the product slightly soluble or insoluble )

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

1-[5-(2-fluorophenyl)-1-(pyridin-3-ylsulfonyl)-1H-pyrrol-3-yl]-N-methylmethanamine monofumarate

(-20℃)

With Ice Pack

≥ 2 years