[CAS NO. 1260141-27-2] Vonoprazan Fumarate (TAK-438)

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PRODUCTS SPECIFICATIONS [1260141-27-2]

Catalog

SLK-S8016

Brand

Selleck

CAS

1260141-27-2

DESCRIPTION [1260141-27-2]

Overview

MDL	MFCD18633280
Molecular Weight	461.46
Molecular Formula	C17H16FN3O2S.C4H4O4
SMILES	-

For research use only.

Storage

3 years,-20°C,powder
1 years,-80°C,in solvent

Shipping

Room temperature shipping(Stability testing shows this product can be shipped without any cooling measures.)

Preparing Stock Solutions

Concentration Volume Mass	1 mg	5 mg	10 mg
1 mM	2.1670 mL	10.8352 mL	21.6704 mL
5 mM	0.4334 mL	2.1670 mL	4.3341 mL
10 mM	0.2167 mL	1.0835 mL	2.1670 mL
50 mM	0.0433 mL	0.2167 mL	0.4334 mL

Description

Vonoprazan Fumarate (TAK-438) is a novel (potassium-competitive acid blocker) that reversibly inhibits with of 19 nM (pH 6.5), controls gastric acid secretion. Phase 3.

Features

Capable of inhibiting H+, K+-ATPase under acidic or neutral conditions.

Targets

H+/K+-ATPase ^[1]

19 nM

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 K of 3 nM.

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. 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.

References

[1] Arikawa Y, et al. J Med Chem, 2012, 55(9), 4446-4456.
[2] Hori Y, et al. J Pharmacol Exp Ther, 2010, 335(1), 231-238.
[3] Hori Y, et al. J Pharmacol Exp Ther, 2011, 337(3), 797-804.