| Size | Price | Stock | Qty |
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| 250mg |
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| 500mg |
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| 1g |
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| 2g |
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| 5g |
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Purity: ≥98%
Pantoprazole Sodium (BY1023; SKF96022; Protonix) is an anti-ulcer drug that acts as a proton pump inhibitor (PPI) and is used for short-term treatment of erosion and ulceration of the esophagus caused by gastroesophageal reflux disease. Pantoprazole inhibits the activity of H+/K+-ATPase proton pumb in the parietal cells of gastric mucosa. This inhibition affects the acid secretion and thus, pantoprazole are used as drugs for the treatment of various acid-related disorders. Pantoprazole is activated slowly. The activated sulfonamide of pantoprazole binds to Cys813 and Cys822 of the pumb and inhibits acid secretion selectively.
| Targets |
Proton pump
|
|---|---|
| ln Vitro |
In EMT-6 and MCF7 cells, pantoprazole sodium (BY1023 sodium; 1–10,000 μM) raises endosomal pH in a concentration-dependent manner [1]. Pantoprazole sodium has the ability to prevent exosome release. Pantoprazole sodium prevents tumor cells (melanoma, adenocarcinoma, and lymphoma cell lines) from acidifying the extracellular media by blocking V-H+-ATPase activity [2].
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| ln Vivo |
In MCF-7 xenografts, the combination of pantoprazole sodium (BY1023 sodium; 200 mg/kg; intraperitoneal injection; once weekly for 3 weeks) and doxorubicin considerably prolonged the tumor development delay [1]. Oral pantoprazole sodium (0.3–3 mg/kg) decreases mepizole-induced stimulated acid secretion in acute fistula rats and basal acid secretion in pyloric ligation rats in a dose-dependent manner [4].
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| Enzyme Assay |
The action of the H+/K(+)-ATPase inhibitors pantoprazole and omeprazole was compared in different in vitro test systems. In gastric membrane vesicles under conditions shown to result in acidification of the vesicle interior, pantoprazole and omeprazole inhibited H+/K(+)-ATPase activity with IC50 values of 6.8 and 2.4 microM, respectively. When intravesicular acidification was reduced by inclusion of imidazole (5 mM), a membrane permeable weak base, the inhibitory action of omeprazole was partially lost (IC50 30 microM) and that of pantoprazole almost completely lost. After incubation for 40 min with pumping membrane vesicles, a half-maximal reduction in intravesicular H+ concentration occurred at pantoprazole and omeprazole concentrations of 1.1 and 0.6 microM, respectively. Again, when the intravesicular H+ concentration was reduced by inclusion of imidazole (2.5 mM), pantoprazole (20 and 60 microM) did not reduce the remaining intravesicular proton concentration, whereas omeprazole (10 and 30 microM) did. Both drugs inhibited, with similar potency, papain activity at pH 3.0 and inactivated the enzyme in a similar time-dependent manner; at pH 5.0 omeprazole (IC50 17 microM) was more potent than pantoprazole (IC50 37 microM) and enzyme inhibition was faster than with pantoprazole. These results indicate that pantoprazole is a potent inhibitor of H+/K(+)-ATPase under highly acidic conditions and that it is more stable than omeprazole at a slightly acidic pH such as pH 5.0[3].
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| Cell Assay |
Murine EMT-6 and human MCF-7 cells were treated with pantoprazole to evaluate changes in endosomal pH using fluorescence spectroscopy, and uptake of doxorubicin using flow cytometry. Effects of pantoprazole on tissue penetration of doxorubicin were evaluated in multilayered cell cultures (MCC). Pantoprazole (>200 μmol/L) increased endosomal pH in cells, and also increased nuclear uptake of doxorubicin. Pretreatment with pantoprazole increased tissue penetration of doxorubicin in MCCs [1].
|
| Animal Protocol |
Animal/Disease Models: Mice bearing MCF-7 or A431 xenografts [1]
Doses: 200 mg/kg Route of Administration: IP; once weekly for 3 weeks; alone or in combination with doxorubicin (6 mg/kg iv) First 2 hour Experimental Results: The growth delay of MCF-7 xenografts with doxorubicin was even greater compared to the single dose combination. A single dose of doxorubicin Dramatically increased tumor growth delay. alone had no effect on growth delay. |
| Toxicity/Toxicokinetics |
Effects During Pregnancy and Lactation
◉ Summary of Use during Lactation Maternal pantoprazole doses of 40 mg daily produce low levels in milk and would not be expected to cause any adverse effects in breastfed infants. ◉ Effects in Breastfed Infants Relevant published information was not found as of the revision date. ◉ Effects on Lactation and Breastmilk A retrospective claims database study in the United States found that users of proton pump inhibitors had an increased risk of gynecomastia. A review article reported that a search of database from the European Pharmacovigilance Centre found 48 cases of gynecomastia, 3 cases of galactorrhea, 14 cases of breast pain and 4 cases of breast enlargement associated with pantoprazole. A search of the WHO global pharmacovigilance database found 97 cases of gynecomastia, 13 cases of galactorrhea, 35 cases of breast pain and 16 cases of breast enlargement associated with pantoprazole. |
| References |
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| Additional Infomation |
Pantoprazole sodium is an organic sodium salt. It has a role as an EC 3.6.3.10 (H(+)/K(+)-exchanging ATPase) inhibitor and an anti-ulcer drug. It contains a pantoprazole(1-).
Pantoprazole Sodium is the sodium salt form of a substituted benzimidazole with proton pump inhibitor activity. Pantoprazole is a lipophilic, weak base that crosses the parietal cell membrane and enters the acidic parietal cell canaliculus where it becomes protonated, producing the active metabolite sulfenamide, which forms an irreversible covalent bond with two sites of the H+/K+-ATPase enzyme located on the gastric parietal cell, thereby inhibiting both basal and stimulated gastric acid production. 2-pyridinylmethylsulfinylbenzimidazole proton pump inhibitor that is used in the treatment of GASTROESOPHAGEAL REFLUX and PEPTIC ULCER. See also: Pantoprazole (has active moiety). Drug Indication Short-term treatment of reflux symptoms (e. g. heartburn, acid regurgitation) in adults. |
| Molecular Formula |
C16H14F2N3NAO4S
|
|---|---|
| Molecular Weight |
405.35
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| Exact Mass |
405.057
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| Elemental Analysis |
C, 47.41; H, 3.48; F, 9.37; N, 10.37; Na, 5.67; O, 15.79; S, 7.91
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| CAS # |
138786-67-1
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| Related CAS # |
Pantoprazole;102625-70-7;Pantoprazole sodium hydrate;164579-32-2;S-Pantoprazole sodium trihydrate;1416988-58-3
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| PubChem CID |
15008962
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| Appearance |
Typically exists as white to off-white solids at room temperature
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| Boiling Point |
586.9ºC at 760 mmHg
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| Melting Point |
199-202ºC
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| Flash Point |
308.7ºC
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| LogP |
3.535
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| Hydrogen Bond Donor Count |
0
|
| Hydrogen Bond Acceptor Count |
10
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| Rotatable Bond Count |
7
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| Heavy Atom Count |
27
|
| Complexity |
497
|
| Defined Atom Stereocenter Count |
0
|
| SMILES |
S(C([H])([H])C1C(=C(C([H])=C([H])N=1)OC([H])([H])[H])OC([H])([H])[H])(C1=NC2C([H])=C(C([H])=C([H])C=2[N-]1)OC([H])(F)F)=O.[Na+]
|
| InChi Key |
YNWDKZIIWCEDEE-UHFFFAOYSA-N
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| InChi Code |
InChI=1S/C16H14F2N3O4S.Na/c1-23-13-5-6-19-12(14(13)24-2)8-26(22)16-20-10-4-3-9(25-15(17)18)7-11(10)21-16/h3-7,15H,8H2,1-2H3/q-1+1
|
| Chemical Name |
sodium5-(difluoromethoxy)-2-[(3,4-dimethoxypyridin-2-yl)methylsulfinyl]benzimidazol-1-ide
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| Synonyms |
BY1023; SKF96022; Protonix; BY 1023; BY-1023; SKF 96022; SKF-96022; Pantoloc; Controloc; Pantecta; Zurcal; Protonix; SK and F-96022; SKF-96022
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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 (e.g. under nitrogen), avoid exposure to moisture and light. |
| 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 (~246.70 mM)
H2O : ~3.85 mg/mL (~9.50 mM) |
|---|---|
| Solubility (In Vivo) |
Solubility in Formulation 1: ≥ 2.5 mg/mL (6.17 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 (6.17 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 (6.17 mM) (saturation unknown) in 10% DMSO + 90% Corn Oil (add these co-solvents sequentially from left to right, and one by one), clear solution. Solubility in Formulation 4: 8.33 mg/mL (20.55 mM) in PBS (add these co-solvents sequentially from left to right, and one by one), clear solution; with ultrasonication (<60°C). |
| Preparing Stock Solutions | 1 mg | 5 mg | 10 mg | |
| 1 mM | 2.4670 mL | 12.3350 mL | 24.6700 mL | |
| 5 mM | 0.4934 mL | 2.4670 mL | 4.9340 mL | |
| 10 mM | 0.2467 mL | 1.2335 mL | 2.4670 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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