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首页-小分子抑制剂&激动剂-Membrane Transporter/Ion Channel-Proton Pump-TAK-438
TAK-438

Chemical Structure : TAK-438

CAS No.: 1260141-27-2

TAK-438 (Vonoprazan, TAK438)

货号: PC-60826Not For Human Use, Lab Use Only.

TAK-438 (Vonoprazan) is 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.

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纯度 & COA & 质检文件 纯度: >98% (HPLC) Select Batch:

生物&药学活性

TAK-438 (Vonoprazan) is 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.
TAK-438 completely inhibits basal and 2-deoxy-d-glucose-stimulated gastric acid secretion in rats at 4 mg/kg (as the free base) orally;
TAK-438 is a more potent and longer-lasting inhibitory action on gastric acid secretion than either lansoprazole or SCH28080.

物理化学性质&存储条件

分子量 461.464
分子式 C21H20FN3O6S
外观性状 Solid
CAS No.
储存条件
固体粉末
-20 °C 12 个月; 4°C 6 个月
配置液
-80 °C 6 个月; -20°C 6 个月
Shipping
Solubility

10 mM in DMSO

Chemical Name/SMILES

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

参考文献

1. Arikawa Y, et al. J Med Chem. 2012 May 10;55(9):4446-56.

2. Hori Y, et al. J Pharmacol Exp Ther. 2010 Oct;335(1):231-8.

3. Matsukawa J, et al. Biochem Pharmacol. 2011 May 1;81(9):1145-51.

4. Shin JM, et al. J Pharmacol Exp Ther. 2011 Nov;339(2):412-20.

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