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TAK-438

Cat. No. M2043

TAK-438 Structure
Size Price Availability Quantity
5mg USD 220 In stock
10mg USD 300 In stock
25mg USD 450 In stock
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Quality Control
  • Current batch:
  • Purity >99%
  • COA
  • MSDS
Biological Activity

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).

Conversion of different model animals based on BSA (Value based on data from FDA Draft Guidelines)
Species Mouse Rat Rabbit Guinea pig Hamster Dog
Weight (kg) 0.02 0.15 1.8 0.4 0.08 10
Body Surface Area (m2) 0.007 0.025 0.15 0.05 0.02 0.5
Km factor 3 6 12 8 5 20
Animal A (mg/kg) = Animal B (mg/kg) multiplied by  Animal B Km
Animal A Km

For example, to modify the dose of resveratrol used for a mouse (22.4 mg/kg) to a dose based on the BSA for a rat, multiply 22.4 mg/kg by the Km factor for a mouse and then divide by the Km factor for a rat. This calculation results in a rat equivalent dose for resveratrol of 11.2 mg/kg.

Chemical Information
Molecular Weight 461.46
Formula C17H16FN3O2S.C4H4O4
CAS Number 1260141-27-2
Purity >99%
Solubility DMSO 60 mg/mL
Storage at -20°C
References

A study comparing the antisecretory effect of TAK-438, a novel potassium-competitive acid blocker, with lansoprazole in animals.
Hori Y, et al. J Pharmacol Exp Ther. 2011 Jun;337(3):797-804. PMID: 21411494.

A comparative study on the modes of action of TAK-438, a novel potassium-competitive acid blocker, and lansoprazole in primary cultured rabbit gastric glands.
Matsukawa J, et al. Biochem Pharmacol. 2011 May 1;81(9):1145-51. PMID: 21371447.

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Lansoprazole

Lansoprazole is a proton-pump inhibitor (PPI) which prevents the stomach from producing gastric acid.

Diazoxide

Diazoxide is a well-known small molecule that activates KATP channels in the smooth muscle of blood vessels and pancreatic beta-cells by increasing membrane permeability to potassium ions.

Azimilide

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Amiodarone

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  Catalog
Abmole Inhibitor Catalog 2017




Keywords: TAK-438 supplier, Potassium Channel, inhibitors

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