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TAK-438 is a novel potassium-competitive acid blocker (P-CAB) type antisecretory agent that reversibly inhibits gastric H+, K+-ATPase with a K(i) of 10 nM at pH 7. TAK-438 exhibited potent H(+),K(+)-ATPase inhibitory activity and potent gastric acid secretion inhibitory action in vivo. TAK-438 increased the pH of the gastric perfusate to 5.7 in an unstimulated condition, and this effect was maintained in the presence of subsequent histamine stimulation. TAK-438 exerted a more potent and longer-lasting antisecretory effect than lansoprazole through high accumulation and slow clearance from the gastric tissue. In addition, TAK-438 was unaffected by the gastric secretory state, unlike proton pump inhibitors (PPIs).
| Molecular Weight | 461.46 |
| Formula | C17H16FN3O2S.C4H4O4 |
| CAS Number | 1260141-27-2 |
| Solubility (25°C) | DMSO 60 mg/mL |
| Storage |
Powder -20°C 3 years ; 4°C 2 years In solvent -80°C 6 months ; -20°C 1 month |
| Related Potassium Channel Products |
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ML133 hydrochloride is a selective inhibitor of the Kir2 family of inward rectifier (IRK, KCNJ) potassium channels. |
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Gliquidone is an ATP-sensitive K+ channel antagonist with IC50 of 27.2 nM. |
| Pinacidil monohydrate
Pinacidil monohydrate is known to augment a time-independent outward current in cardiac tissues by activating the ATP-regulated potassium channels. |
| Terfenadine
Terfenadine is a potent open-channel blocker of hERG with an IC50 of 204 nM. Terfenadine is an antihistamine compound that is normally fully metabolized in the liver by the cytochrome P450 CYP3A4 subtype enzyme into the active form fexofenadine. |
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