| Size | Price | Stock | Qty |
|---|---|---|---|
| 1mg |
|
||
| 2mg |
|
||
| 5mg |
|
||
| 10mg |
|
||
| 25mg |
|
||
| Other Sizes |
| Targets |
Lansoprazole sulfone is a metabolite of lansoprazole, a proton pump inhibitor that inactivates the hydrogen/potassium-stimulated ATPase pumps in parietal cells, thus inhibiting gastric acid secretion. The compound itself inhibits H⁺,K⁺-ATPase.
|
|---|---|
| ln Vitro |
Lansoprazole sulfone is a phase I metabolite of lansoprazole formed through oxidation of the parent compound. It has potential applications in duodenal ulcer, gastric ulcer, gastroesophageal reflux disease, and Zollinger-Ellison syndrome. The compound is used as a reference standard for lansoprazole metabolism studies.
|
| ln Vivo |
Lansoprazole sulfone is a metabolite of lansoprazole. It is formed in vivo through the oxidation of lansoprazole. The compound has been shown to inhibit H⁺,K⁺-ATPase, suggesting it may contribute to the pharmacological effects of lansoprazole. However, its activity is lower than that of the parent compound.
|
| Enzyme Assay |
In vitro enzyme assays for Lansoprazole sulfone typically involve studying its formation from lansoprazole by CYP450 enzymes. Microsomal preparations or recombinant CYP enzymes are incubated with lansoprazole and NADPH, and the formation of lansoprazole sulfone is measured by HPLC or LC-MS. The compound's ability to inhibit H⁺,K⁺-ATPase can also be assessed in vitro using gastric membrane preparations.
|
| Cell Assay |
Cell-based assays for Lansoprazole sulfone are limited, as the compound is a metabolite rather than a primary therapeutic agent. Its effects on gastric acid secretion can be studied in isolated gastric glands or parietal cells. The compound's ability to inhibit acid secretion is measured by assessing the accumulation of [¹⁴C]-aminopyrine, a marker of acid production. However, the parent compound lansoprazole is typically more potent.
|
| Animal Protocol |
In vivo animal studies for Lansoprazole sulfone are limited, as the compound is a metabolite. Studies typically focus on the pharmacokinetics and metabolism of lansoprazole, with lansoprazole sulfone measured as a metabolite. The compound's contribution to the overall pharmacological effect of lansoprazole can be assessed by comparing the effects of the parent compound and the metabolite.
|
| ADME/Pharmacokinetics |
Metabolism / Metabolites
Lansoprazole sulfone is a known metabolite of lansoprazole in the human body. Pharmacokinetic properties of Lansoprazole sulfone are related to its formation from lansoprazole. The compound is formed in the liver via CYP450-mediated oxidation. It is then excreted in the urine and bile. The compound's half-life is longer than that of lansoprazole. It does not contribute significantly to the therapeutic effect of lansoprazole due to its lower activity. |
| Toxicity/Toxicokinetics |
Toxicological profile of Lansoprazole sulfone is not well-characterized, as the compound is a metabolite. It is generally considered to have low toxicity. The compound is used as an impurity standard for quality control of lansoprazole formulations. Its safety profile is derived from the extensive safety data available for lansoprazole.
|
| References | |
| Additional Infomation |
Lansoprazole sulfone is a phase I metabolite of the proton pump inhibitor lansoprazole. It is used as a reference standard and impurity marker in pharmaceutical quality control. The compound is also used in research to study lansoprazole metabolism and the role of metabolites in drug action. It is not approved for therapeutic use.
|
| Molecular Formula |
C16H14F3N3O3S
|
|---|---|
| Molecular Weight |
385.36
|
| Exact Mass |
385.07
|
| CAS # |
131926-99-3
|
| Related CAS # |
Lansoprazole sulfone-d4;1184999-77-6
|
| PubChem CID |
10385385
|
| Appearance |
White to off-white solid powder
|
| Density |
1.5±0.1 g/cm3
|
| Boiling Point |
555.6±60.0 °C at 760 mmHg
|
| Melting Point |
207ºC(dec.)
|
| Flash Point |
289.8±32.9 °C
|
| Vapour Pressure |
0.0±1.5 mmHg at 25°C
|
| Index of Refraction |
1.581
|
| LogP |
4.46
|
| Hydrogen Bond Donor Count |
1
|
| Hydrogen Bond Acceptor Count |
8
|
| Rotatable Bond Count |
5
|
| Heavy Atom Count |
26
|
| Complexity |
582
|
| Defined Atom Stereocenter Count |
0
|
| InChi Key |
TVMJMCGRSSSSDJ-UHFFFAOYSA-N
|
| InChi Code |
InChI=1S/C16H14F3N3O3S/c1-10-13(20-7-6-14(10)25-9-16(17,18)19)8-26(23,24)15-21-11-4-2-3-5-12(11)22-15/h2-7H,8-9H2,1H3,(H,21,22)
|
| Chemical Name |
2-[[3-methyl-4-(2,2,2-trifluoroethoxy)pyridin-2-yl]methylsulfonyl]-1H-benzimidazole
|
| Synonyms |
Lansoprazole sulfone
|
| HS Tariff Code |
2934.99.9001
|
| 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)
|
| Solubility (In Vitro) |
DMSO : ~250 mg/mL (~648.74 mM)
|
|---|---|
| Solubility (In Vivo) |
Note: Listed below are some common formulations that may be used to formulate products with low water solubility (e.g. < 1 mg/mL), you may test these formulations using a minute amount of products to avoid loss of samples.
Injection Formulations
Injection Formulation 1: DMSO : Tween 80： Saline = 10 : 5 : 85 (i.e. 100 μL DMSO stock solution → 50 μL Tween 80 → 850 μL Saline)(e.g. IP/IV/IM/SC) *Preparation of saline: Dissolve 0.9 g of sodium chloride in 100 mL ddH ₂ O to obtain a clear solution. Injection Formulation 2: DMSO : PEG300 ：Tween 80 : Saline = 10 : 40 : 5 : 45 (i.e. 100 μL DMSO → 400 μLPEG300 → 50 μL Tween 80 → 450 μL Saline) Injection Formulation 3: DMSO : Corn oil = 10 : 90 (i.e. 100 μL DMSO → 900 μL Corn oil) Example: Take the Injection Formulation 3 (DMSO : Corn oil = 10 : 90) as an example, if 1 mL of 2.5 mg/mL working solution is to be prepared, you can take 100 μL 25 mg/mL DMSO stock solution and add to 900 μL corn oil, mix well to obtain a clear or suspension solution (2.5 mg/mL, ready for use in animals). View More
Injection Formulation 4: DMSO : 20% SBE-β-CD in saline = 10 : 90 [i.e. 100 μL DMSO → 900 μL (20% SBE-β-CD in saline)] Oral Formulations
Oral Formulation 1: Suspend in 0.5% CMC Na (carboxymethylcellulose sodium) Oral Formulation 2: Suspend in 0.5% Carboxymethyl cellulose Example: Take the Oral Formulation 1 (Suspend in 0.5% CMC Na) as an example, if 100 mL of 2.5 mg/mL working solution is to be prepared, you can first prepare 0.5% CMC Na solution by measuring 0.5 g CMC Na and dissolve it in 100 mL ddH2O to obtain a clear solution; then add 250 mg of the product to 100 mL 0.5% CMC Na solution, to make the suspension solution (2.5 mg/mL, ready for use in animals). View More
Oral Formulation 3: Dissolved in PEG400 (Please use freshly prepared in vivo formulations for optimal results.) |
| Preparing Stock Solutions | 1 mg | 5 mg | 10 mg | |
| 1 mM | 2.5950 mL | 12.9749 mL | 25.9498 mL | |
| 5 mM | 0.5190 mL | 2.5950 mL | 5.1900 mL | |
| 10 mM | 0.2595 mL | 1.2975 mL | 2.5950 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.
Products are for research use only; We do not sell to patients
Copyright 2020 InvivoChem LLC | All Rights Reserved
