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Abeprazan

Cat. No. M29007
Abeprazan Structure
Synonym:

DWP14012; Fexuprazan

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Biological Activity

Abeprazan (DWP14012) is a potassium-competitive acid blocker. Abeprazan inhibits H+, K+- ATPase by reversible potassium-competitive ionic binding with no acid activation required. Abeprazan is developed as a potential alternative to proton pump inhibitor for the treatment of acid-related diseases.

Chemical Information
Molecular Weight 410.41
Formula C19H17F3N2O3S
CAS Number 1902954-60-2
Form Solid
Solubility (25°C) DMSO 50 mg/mL (ultrasonic)
Storage Powder          -20°C   3 years ;  4°C   2 years
In solvent       -80°C   6 months ;  -20°C   1 month
Conversion of different model animals based on BSA (PMID: 27057123)
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 Compound A used for a mouse (20 mg/kg) to a dose based on the BSA for a rat, multiply 20 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 Compound A of 10 mg/kg.

References

[1] Kang Nyeong Lee, et al. World J Gastroenterol. Randomized controlled trial to evaluate the efficacy and safety of fexuprazan compared with esomeprazole in erosive esophagitis

[2] Min-Soo Kim, et al. Pharmaceuticals (Basel). Model-Based Prediction of Acid Suppression and Proposal of a New Dosing Regimen of Fexuprazan in Humans

[3] Yoo-Seong Jeong, et al. Pharmaceutics. Development of Physiologically Based Pharmacokinetic Model for Orally Administered Fexuprazan in Humans

[4] Carmelo Scarpignato, et al. Aliment Pharmacol Ther. Editorial: acid suppression with potassium-competitive acid blockers dismissing genotype concerns

[5] Jun Gi Hwang, et al. Aliment Pharmacol Ther. Editorial: acid suppression with potassium-competitive acid blockers-dismissing genotype concerns. Authors' reply

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Abeprazan hydrochloride

Abeprazan hydrochloride (DWP14012 hydrochloride) is a potassium-competitive acid blocker. Abeprazan hydrochloride inhibits H+, K+- ATPase by reversible potassium-competitive ionic binding with no acid activation required. Abeprazan hydrochloride is developed as a potential alternative to proton pump inhibitor for the treatment of acid-related diseases.

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Keywords: Abeprazan, DWP14012; Fexuprazan supplier, Proton Pump, inhibitors, activators


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