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| 1mg |
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| 5mg |
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| 10mg |
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| 25mg |
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Purity: ≥98%
Tegoprazan, a novel and potent P-CAB (potassium-competitive acid blocker), is a next-generation therapeutics developed for the treatment of acid-related gastrointestinal diseases such as gastroesophageal reflux disease (GERD) and peptic ulcers, acting by controling gastric acid secretion and motility.
| ln Vitro |
H+/K+-ATPase activity in pigs, dogs, and humans is inhibited by tigeprazan. Tegoprazan inhibits pH+/K+-ATPase in a reversible and potassium-competitive way. At tegoprazan doses up to 0.15 μM, 86% of H+/K+-ATPase activity is inhibited by 3 μM of tegoprazan [1].
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| ln Vivo |
In dogs, egoprazan (1.0 mg/kg, po) effectively prevents stomach acidity brought on by histamine. The neutral range of pH is regained in the stomach after pentagastrin-induced acidification, with a dose of 1.0–3.0 mg/kg, po. In dogs administered with pentagastrin, egoprazan (3 mg/kg, face) causes immediate gastric phase III contractions of the migrating motor complex [1].
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| References |
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| Additional Infomation |
Tegoprazan (also known as CJ-12420) is a novel therapeutic developed by CJ Healthcare Corp for treating acid-related gastrointestinal diseases. This drug is a potent and high-selective potassium-competitive acid blocker (P-CAB) with a fast onset of action and the ability to control gastric pH for a prolonged period of time. Tegoprazan’s strong and sustained effect is due to its ability to be slowly cleared from the gastric glands and exertion of effects independent of acid levels. It has also been observed to be efficacious independent of food intake.
Mechanism of Action Tegoprazan works as a potassium-competitive acid blocker that is potent and highly selective. Its mechanism of action is different from that of the proton-pump inhibitors as this drug does not require conversion into an active form and can directly inhibit H+/K+‐ATPase in a reversible and K+‐competitive way. This is because it is an acid-resistant weak base with the ability to remain in the highly acidic canaliculi of gastric parietal cells. |
| Molecular Formula |
C20H19F2N3O3
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|---|---|
| Molecular Weight |
387.37997174263
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| Exact Mass |
387.139
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| CAS # |
942195-55-3
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| Related CAS # |
Tegoprazan-d6
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| PubChem CID |
23582846
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| Appearance |
Off-white to light yellow solid powder
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| LogP |
3.2
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| Hydrogen Bond Donor Count |
1
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| Hydrogen Bond Acceptor Count |
6
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| Rotatable Bond Count |
3
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| Heavy Atom Count |
28
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| Complexity |
581
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| Defined Atom Stereocenter Count |
1
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| SMILES |
O([C@H]1CCOC2=CC(=CC(=C12)F)F)C1C=C(C(=O)N(C)C)C=C2N=C(NC=12)C
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| InChi Key |
CLIQCDHNPDMGSL-HNNXBMFYSA-N
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| InChi Code |
InChI=1S/C20H19F2N3O3/c1-10-23-14-6-11(20(26)25(2)3)7-17(19(14)24-10)28-15-4-5-27-16-9-12(21)8-13(22)18(15)16/h6-9,15H,4-5H2,1-3H3,(H,23,24)/t15-/m0/s1
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| Chemical Name |
7-[[(4S)-5,7-difluoro-3,4-dihydro-2H-chromen-4-yl]oxy]-N,N,2-trimethyl-3H-benzimidazole-5-carboxamide
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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 : ~100 mg/mL (~258.14 mM)
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|---|---|
| Solubility (In Vivo) |
Solubility in Formulation 1: ≥ 2.5 mg/mL (6.45 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 (6.45 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 (6.45 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 | 2.5814 mL | 12.9072 mL | 25.8144 mL | |
| 5 mM | 0.5163 mL | 2.5814 mL | 5.1629 mL | |
| 10 mM | 0.2581 mL | 1.2907 mL | 2.5814 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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