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Vonoprazan (fumarate)

Item № 24200
CAS № 1260141-27-2
Purity ≥98%
product image
                (CAS 1260141-27-2)
SIZE PRICE QUANTITY SUBTOTAL
CART TOTAL
     500 mg $35.00 0.00
     1 g $63.00 0.00
     5 g $245.00 0.00
     10 g $350.00 0.00

Pricing updated 2019-04-24. Prices are subject to change without notice.

Description
Synonyms
  • TAK-438

Vonoprazan is a selective, reversible, and potassium-competitive proton pump inhibitor that inhibits gastric H+/K+ ATPase (IC50 = 17 nM) but does not inhibit porcine Na+/K+ ATPase activity when used at a concentration of 10 µM.1,2 It maintains its inhibitory effect in both weakly acidic (pH 6.5) and neutral (pH 7.5) conditions with IC50 values of 19 and 28 nM, respectively. In vivo, vonoprazan (1, 2, and 4 mg/kg) inhibits histamine-stimulated acid secretion in a dose-dependent manner in rats, with complete inhibition when administered at a dose of 4 mg/kg.3 It also inhibits acid secretion for more than 48 hours in dogs when administered at doses ranging from 0.1 to 1 mg/kg.

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Technical Information
Formal Name
5-(2-fluorophenyl)-N-methyl-1-(3-pyridinylsulfonyl)-1H-pyrrole-3-methanamine, 2-butenedioate
CAS Number
1260141-27-2
Synonyms
  • TAK-438
Molecular Formula
C17H16FN3O2S • C4H4O4
Formula Weight
461.5
Purity
≥98%
Formulation
A crystalline solid
SMILES
FC(C=CC=C1)=C1C2=CC(CNC)=CN2S(C3=CC=CN=C3)(=O)=O.OC(/C=C/C(O)=O)=O
InChI Code
InChI=1S/C17H16FN3O2S.C4H4O4/c1-19-10-13-9-17(15-6-2-3-7-16(15)18)21(12-13)24(22,23)14-5-4-8-20-11-14;5-3(6)1-2-4(7)8/h2-9,11-12,19H,10H2,1H3;1-2H,(H,5,6)(H,7,8)/b;2-1+
InChI Key
ROGSHYHKHPCCJW-WLHGVMLRSA-N

Warning - this product is not for human or veterinary use.

Shipping & Storage
Storage
-20°C
Shipping
Room temperature in continental US; may vary elsewhere
Stability
≥ 2 years
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Additional Information

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References & Product Citations
Product Description References

1. Shin, J.M., Inatomi, N., Munson, K., et al. Characterization of a novel potassium-competitive acid blocker of the gastric H,K-ATPase, 1-[5-(2-fluorophenyl)-1-(pyridin-3-ylsulfonyl)-1H-pyrrol-3-yl]-N-methylmethanamine monofumarate (TAK-438) J. Pharmacol. Exp. Ther. 339(2), 412-420 (2011).

2. Hori, Y., Imanishi, A., Matsukawa, J., 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. 335(1), 231-238 (2010).

3. Hori, Y., Matsukawa, J., Takeuchi, T., 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. 337(3), 797-804 (2011).

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