| Size | Price | Stock | Qty |
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Abeprazan (also called Fexuprazan; DWP-14012) is a novel and potent acid pump inhibitor which inhibits H+, K+- ATPase by reversible potassium-competitive ionic binding with no acid activation required.
| ln Vitro |
Reversibly binding to H+, K+-ATPase is the mechanism of action of abeprazan; in contrast to PPIs, this drug activation does not require an acidic environment[1].
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|---|---|
| ln Vivo |
A number of in vivo studies using pylorus-ligated rats, lumen-perfused models, and heidenhain pouch dog models have shown that beprazan inhibits acid secretion in a dose-dependent manner, with the inhibition of gastric acid secretion being equal to or greater than that of vonoprazan, a P-CAB that has previously been approved[1].
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| References | |
| Additional Infomation |
Abeprazan is under investigation in clinical trial NCT04341454 (Study to Evaluate the Efficacy and Safety of DWP14012 in Patients With Acute or Chronic Gastritis).
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| Molecular Formula |
C19H17F3N2O3S
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|---|---|
| Molecular Weight |
410.4112
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| Exact Mass |
410.091
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| CAS # |
1902954-60-2
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| Related CAS # |
Abeprazan hydrochloride;1902954-87-3
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| PubChem CID |
122662112
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| Appearance |
White to light yellow solid powder
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| Density |
1.4±0.1 g/cm3
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| Boiling Point |
497.9±55.0 °C at 760 mmHg
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| Flash Point |
254.9±31.5 °C
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| Vapour Pressure |
0.0±1.3 mmHg at 25°C
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| Index of Refraction |
1.575
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| LogP |
3.89
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| Hydrogen Bond Donor Count |
1
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| Hydrogen Bond Acceptor Count |
7
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| Rotatable Bond Count |
6
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| Heavy Atom Count |
28
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| Complexity |
618
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| Defined Atom Stereocenter Count |
0
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| InChi Key |
OUNXGNDVWVPCOL-UHFFFAOYSA-N
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| InChi Code |
InChI=1S/C19H17F3N2O3S/c1-23-10-12-11-24(28(25,26)15-5-3-4-13(20)8-15)18(19(12)27-2)16-7-6-14(21)9-17(16)22/h3-9,11,23H,10H2,1-2H3
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| Chemical Name |
1-[5-(2,4-difluorophenyl)-1-(3-fluorophenyl)sulfonyl-4-methoxypyrrol-3-yl]-N-methylmethanamine
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| Synonyms |
AbeprazanFexuprazan DWP-14012
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| HS Tariff Code |
2934.99.9001
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| Storage |
Powder -20°C 3 years 4°C 2 years In solvent -80°C 6 months -20°C 1 month |
| Shipping Condition |
Room temperature (This product is stable at ambient temperature for a few days during ordinary shipping and time spent in Customs)
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| Solubility (In Vitro) |
DMSO : ~50 mg/mL (~121.83 mM)
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|---|---|
| Solubility (In Vivo) |
Solubility in Formulation 1: ≥ 2.5 mg/mL (6.09 mM) (saturation unknown) in 10% DMSO + 40% PEG300 + 5% Tween80 + 45% Saline (add these co-solvents sequentially from left to right, and one by one), clear solution.
For example, if 1 mL of working solution is to be prepared, you can add 100 μL of 25.0 mg/mL clear DMSO stock solution to 400 μL PEG300 and mix evenly; then add 50 μL Tween-80 to the above solution and mix evenly; then add 450 μL normal saline to adjust the volume to 1 mL. Preparation of saline: Dissolve 0.9 g of sodium chloride in 100 mL ddH₂ O to obtain a clear solution. Solubility in Formulation 2: ≥ 2.5 mg/mL (6.09 mM) (saturation unknown) in 10% DMSO + 90% (20% SBE-β-CD in Saline) (add these co-solvents sequentially from left to right, and one by one), clear solution. For example, if 1 mL of working solution is to be prepared, you can add 100 μL of 25.0 mg/mL clear DMSO stock solution to 900 μL of 20% SBE-β-CD physiological saline solution and mix evenly. Preparation of 20% SBE-β-CD in Saline (4°C，1 week): Dissolve 2 g SBE-β-CD in 10 mL saline to obtain a clear solution. View More
Solubility in Formulation 3: ≥ 2.5 mg/mL (6.09 mM) (saturation unknown) in 10% DMSO + 90% Corn Oil (add these co-solvents sequentially from left to right, and one by one), clear solution. |
| Preparing Stock Solutions | 1 mg | 5 mg | 10 mg | |
| 1 mM | 2.4366 mL | 12.1829 mL | 24.3659 mL | |
| 5 mM | 0.4873 mL | 2.4366 mL | 4.8732 mL | |
| 10 mM | 0.2437 mL | 1.2183 mL | 2.4366 mL |
*Note: Please select an appropriate solvent for the preparation of stock solution based on your experiment needs. For most products, DMSO can be used for preparing stock solutions (e.g. 5 mM, 10 mM, or 20 mM concentration); some products with high aqueous solubility may be dissolved in water directly. Solubility information is available at the above Solubility Data section. Once the stock solution is prepared, aliquot it to routine usage volumes and store at -20°C or -80°C. Avoid repeated freeze and thaw cycles.
Calculation results
Working concentration： mg/mL；
Method for preparing DMSO stock solution： mg drug pre-dissolved in μL DMSO (stock solution concentration mg/mL). Please contact us first if the concentration exceeds the DMSO solubility of the batch of drug.
Method for preparing in vivo formulation:：Take μL DMSO stock solution, next add μL PEG300, mix and clarify, next addμL Tween 80, mix and clarify, next add μL ddH2O，mix and clarify.
(1) Please be sure that the solution is clear before the addition of next solvent. Dissolution methods like vortex, ultrasound or warming and heat may be used to aid dissolving.
(2) Be sure to add the solvent(s) in order.
| NCT Number | Recruitment | interventions | Conditions | Sponsor/Collaborators | Start Date | Phases |
| NCT06437951 | NOT YET RECRUITING | Drug: Fexuprazan Injection Drug: Fexuprazan Injection placebo Drug: Fexuprazan Injection_part 2 |
Erosive Gastroesophageal Reflux Disease | Daewoong Pharmaceutical Co. LTD. | 2024-07 | Phase 1 |
| NCT06508645 | COMPLETED | Drug: DWP14012 injection | Healthy Volunteers | Daewoong Pharmaceutical Co. LTD. | 2022-01-10 | Phase 1 |
| NCT05614752 | ACTIVE, NOT RECRUITING | Drug: Fexuprazan | Gastroesophageal Reflux Disease | Daewoong Pharmaceutical Co. LTD. | 2022-07-06 | |
| NCT05886933 | ACTIVE, NOT RECRUITING | Drug: Fexuprazan Hydrochloride | Gastroesophageal Reflux Disease | Daewoong Pharmaceutical Co. LTD. | 2023-05-22 | |
| NCT05946135 | NOT YET RECRUITING | Drug: Lansoprazole Drug: Fexuprazan Hydrochloride |
Patients on Treatment With Systemic Steroids | Yonsei University | 2023-07 | Phase 4 |
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