Vonoprazan

Modify Date: 2024-01-02 17:41:33

Vonoprazan Structure
Vonoprazan structure
 Common Name Vonoprazan
CAS Number 881681-00-1 Molecular Weight 345.391
Density 1.3±0.1 g/cm3 Boiling Point 530.3±60.0 °C at 760 mmHg
Molecular Formula C17H16FN3O2S Melting Point N/A
MSDS N/A Flash Point 274.5±32.9 °C

 Use of Vonoprazan


TAK-438 (free base) 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+ ATPasein 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].

 Names

Name Vonoprazan
Synonym More Synonyms

 Vonoprazan Biological Activity

Description TAK-438 (free base) 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+ ATPasein 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].
Related Catalog
References

[1]. Arikawa Y, et al. Discovery of a novel pyrrole derivative 1-[5-(2-fluorophenyl)-1-(pyridin-3-ylsulfonyl)-1H-pyrrol-3-yl]-N-methylmethanamine fumarate (TAK-438) as a potassium-competitive acid blocker (P-CAB). J Med Chem, 2012, 55(9), 4446-4456.

[2]. Hori Y, et al. 1-[5-(2-Fluorophenyl)-1-(pyridin-3-ylsulfonyl)-1H-pyrrol-3-yl]-N-methylmethanamine monofumarate (TAK-438), a novel and potent potassium-competitive acid blocker for the treatment of acid-related diseases. J Pharmacol Exp Ther, 2010, 335(1), 231-238.

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

 Chemical & Physical Properties

Density 1.3±0.1 g/cm3
Boiling Point 530.3±60.0 °C at 760 mmHg
Molecular Formula C17H16FN3O2S
Molecular Weight 345.391
Flash Point 274.5±32.9 °C
Exact Mass 345.094727
LogP 2.74
Vapour Pressure 0.0±1.4 mmHg at 25°C
Index of Refraction 1.622

 Synonyms

1H-Pyrrole-3-methanamine, 5-(2-fluorophenyl)-N-methyl-1-(3-pyridinylsulfonyl)-
Vonoprazan
1-[5-(2-Fluorophenyl)-1-(3-pyridinylsulfonyl)-1H-pyrrol-3-yl]-N-methylmethanamine
TAK-438
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Related Compounds: More...
Vonoprazan Fumarate
1260141-27-2
Vonoprazan Fumarate
881681-01-2
Vonoprazan Impurity 3
928325-41-1
Vonoprazan Impurity 2
881733-36-4
Vonoprazan Impuirty 32
881733-45-5
Vonoprazan Impurity 24
1807642-41-6
Vonoprazan hydrochloride
1957202-44-6
Vonoprazan Fumarate impurity
1885094-62-1
Vonoprazan Fumarate Impurity 6
2250243-23-1
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tert-Butyl-DL-alanine
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4-amino-N-[2-tert-butyl-1-(tetrahydro-2H-pyran-4-ylmethyl)-1H-benzimidazol-5-yl]-N-ethylbenzenesulfonamide
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