CasNo.1260141-27-2,TAK438,(1260141-27-2) Suppliers

100 Gram	FOB Price: USD 1.0000

Min.Order :100 Gram
Purity: 98%
Payment Terms : L/C

Keywords

TAK438 TAK-438;5-(2-Fluorophenyl)-N-methyl-1-(3-pyridinylsulfonyl)-1H-pyrrole-3-methanamine 2-butenedioate;Vonoprazan FuMarate;Vonaprazan;vonoprazan(tak-438)1260141-27-2;fuMarate vonoprazan;vonoprazan(tak-43 1260141-27-2

Quick Details

Appearance:White crystal
Application:CAS：1260141-27-2； TAK-438;5-(2-Fluorophenyl)-N-methyl-1-(3-pyridinylsulfonyl)-1H-pyrrole-3-methanamine 2-butenedioate;Vonoprazan FuMarate;Vonaprazan;vonoprazan(tak-438)1260141-27-2;fuMarate vonopra
PackAge:100g,500,1kg.....
ProductionCapacity:1000|Metric Ton|Month
Storage:Dry seal
Transportation:shipping

Superiority:

We are specialized in custom synthesis, chemical/pharmaceutical/ pesticides outsourcing and contract research.

We are committed to provide excellence in researching, manufacturing and drug discovery process.

Our research team of scientists consists of western-trained Ph.D.s with experience and capabilities in drug R&D methodologies and medicinal chemistry.

Details:

TAK-438 is a novel P-CAB (potassium-competitive acid blocker) that reversibly inhibits H+/K+, ATPase with IC50 of 19 nM (pH 6.5), controls gastric acid secretion.
IC50 value: 19 nM [1]
Target: H+/K+ATPase
in vitro: TAK-438 is a pyrrole derivative with a chemical structure that is completely different from the P-CABs developed to date. TAK-438 inhibits gastric H+, K+-ATPase activity in a concentration-dependent manner. Under neutral conditions (pH 7.5), the inhibitory activity of TAK-438 is almost the same as that under weakly acidic conditions (pH 6.5). TAK-438 does not inhibit Na+, K+-ATPase activity even at concentration 500 times higher than their IC50 values against gastric H+,K+-ATPase activity. TAK-438 inhibits gastric H+, K+-ATPase in a K+-competitive manner with Ki of 3 nM [2].
in vivo: TAK-438 inhibits basal gastric acid secretion in a dose-dependent manner, and the ID50 value is 1.26 mg/kg . Intravenous administration of TAK-438 dose-dependently increases the pH of the gastric perfusate, and the increase in pH is sustained for 5 h after administration. At the 1 mg/kg dose, the pH plateaues 90 min after administration, and the highest pH value reached is 5.9 [2]. In addition, TAK-438 shows a potent and longer-lasting inhibitory effect on the histamine-stimulated gastric acid secretion in rats and dogs. TAK-438 shows significant antisecretory activity through high accumulation and slow clearance from the gastric tissue. TAK-438 is unaffected by the gastric secretory state, unlike PPIs [3].