2014年8月10日星期日

TAK-438|cas 1260141-27-2| DC Chem|Supplier|Price|Buy 

TAK-438|cas 1260141-27-2| DC Chem|Supplier|Price|Buy
DC Chemicals SupplyTAK-438|cas 1260141-27-2,Purity: >98% ,Cat No. DC7306, In stock.

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TAK-438|cas 1260141-27-2 ,Synonym: TAK 438; TAK438  ,Chemical name: C17H16FN3O2S.C4H4O4 ,Molecular Formula: C17H16FN3O2S.C4H4O4 ,MW:461.46

TAK-438, cas 1260141-27-2,Purity: >98%, Best Price and quality from DC Chemicals. 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.

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. 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.

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