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| 5mg |
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| 10mg |
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| 25mg |
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Abeprazan HCl (DWP14012; DWP-14012) hydrochlorideis a novel and potent potassium acid blocker or a potassium-competitive acid blocker, with the potential to be used as a potential alternative to proton pump inhibitor for the treatment of acid-related disease. Abeprazan hydrochloride inhibits H+, K+- ATPase by reversible potassium-competitive ionic binding with no acid activation required.
| ln Vitro |
Unlike proton pump inhibitors, abelazam hydrochloride acts by reversibly binding to H+ and K+-ATPases, meaning that an acidic environment is not necessary for drug activation [1].
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|---|---|
| ln Vivo |
In several in vivo experiments employing pyloric ligated rats, belazan hydrochloride (DWP14012 hydrochloride) decreases stomach acid secretion in a dose-dependent manner, with suppression of gastric acid secretion equal to or greater than that of the previously approved P-CAB Vono. Heidenhan bag dog model, vonoprazan, and intraluminal perfusion rat model [1].
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| References |
| Molecular Formula |
C19H18CLF3N2O3S
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|---|---|
| Molecular Weight |
446.8710
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| Exact Mass |
446.067
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| CAS # |
1902954-87-3
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| Related CAS # |
Abeprazan;1902954-60-2
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| PubChem CID |
130454904
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| Appearance |
White to light yellow solid powder
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| Hydrogen Bond Donor Count |
2
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| Hydrogen Bond Acceptor Count |
7
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| Rotatable Bond Count |
6
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| Heavy Atom Count |
29
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| Complexity |
618
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| Defined Atom Stereocenter Count |
0
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| SMILES |
Cl[H].S(C1=C([H])C([H])=C([H])C(=C1[H])F)(N1C([H])=C(C([H])([H])N([H])C([H])([H])[H])C(=C1C1C([H])=C([H])C(=C([H])C=1F)F)OC([H])([H])[H])(=O)=O
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| InChi Key |
BOHTZYBQQDVIRI-UHFFFAOYSA-N
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| InChi Code |
InChI=1S/C19H17F3N2O3S.ClH/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;1H
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| Chemical Name |
1-[5-(2,4-difluorophenyl)-1-(3-fluorophenyl)sulfonyl-4-methoxypyrrol-3-yl]-N-methylmethanamine;hydrochloride
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| Synonyms |
Abeprazan HClDWP14012DWP-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 Note: Please store this product in a sealed and protected environment, avoid exposure to moisture. |
| 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 : ~25 mg/mL (~55.94 mM)
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| Solubility (In Vivo) |
Solubility in Formulation 1: ≥ 2.5 mg/mL (5.59 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 (5.59 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 (5.59 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 | 2.2378 mL | 11.1889 mL | 22.3779 mL | |
| 5 mM | 0.4476 mL | 2.2378 mL | 4.4756 mL | |
| 10 mM | 0.2238 mL | 1.1189 mL | 2.2378 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.
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