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Vonoprazan (TAK-438 free base) 是有一种口服活性的 钾竞争性酸阻断剂，抑制 H+, K+-ATPase的 IC50 值为 19 nM。
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Vonoprazan Chemical Structure
CAS No. : 881681-00-1
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Size
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Price
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Stock
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Quantity
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Free Sample (0.1-0.5 mg)
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Apply now
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10 mM * 1 mL in DMSO
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￥539
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In-stock
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0 1 2 3 4 5 6 7
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50 mg
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￥490
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In-stock
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0 1 2 3 4 5 6 7
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100 mg
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￥630
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In-stock
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0 1 2 3 4 5 6 7
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250 mg
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￥1250
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In-stock
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0 1 2 3 4 5 6 7
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500 mg
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Get quote
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1 g
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Get quote
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Description
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Vonoprazan (TAK-438 free base) is an orally active potassium-competitive acid blocker which inhibits H+, K+-ATPase activity with an IC50 of 19 nM.
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Clinical Trial
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NCT Number
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Sponsor
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Condition
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Start Date
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Phase
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NCT03050359
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Takeda
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Duodenal Ulcer
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April 5, 2017
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Phase 3
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NCT02123927
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Takeda
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Ascending Single Dose Study
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September 2007
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Phase 1
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NCT03214094
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Takeda
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Gastric or Duodenal Ulcers
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September 1, 2016
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Molecular Weight
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Formula
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CAS No.
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SMILES
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O=S(N1C=C(CNC)C=C1C2=CC=CC=C2F)(C3=CC=CN=C3)=O
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Shipping
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Room temperature in continental US; may vary elsewhere.
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Storage
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Powder
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-20°C
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3 years
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4°C
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2 years
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In solvent
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-80°C
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6 months
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-20°C
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1 month
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Solvent & Solubility
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In Vitro:
DMSO : ≥ 33 mg/mL (95.54 mM)
* "≥" means soluble, but saturation unknown.
Preparing
Stock Solutions
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ConcentrationSolventMass
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1 mg
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5 mg
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10 mg
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1 mM
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2.8953 mL
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14.4764 mL
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28.9528 mL
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5 mM
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0.5791 mL
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2.8953 mL
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5.7906 mL
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10 mM
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0.2895 mL
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1.4476 mL
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2.8953 mL
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*
请根据产品在不同溶剂中的溶解度选择合适的溶剂配制储备液；一旦配成溶液，请分装保存，避免反复冻融造成的产品失效。
储备液的保存方式和期限：-80°C, 6 months; -20°C, 1 month。 -80°C 储存时，请在 6 个月内使用，-20°C 储存时，请在 1 个月内使用。
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References
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[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.
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