| Size | Price | |
|---|---|---|
| 500mg | ||
| 1g | ||
| Other Sizes |
| Targets |
5-Hydroxylansoprazole sulfone targets the cytochrome P450 enzyme CYP2C19, a key enzyme involved in the metabolism of many clinically used drugs. It acts as a metabolism-dependent inhibitor, meaning that its inhibitory activity requires metabolic transformation. By inhibiting CYP2C19, it can affect the clearance of other drugs that are substrates of this enzyme.
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|---|---|
| ln Vitro |
In vitro, 5-Hydroxylansoprazole sulfone acts as a potent inhibitor of CYP2C19. Its activity is measured in liver microsome or recombinant enzyme assays. The compound's ability to inhibit CYP2C19-mediated metabolism of a probe substrate is used to calculate its half-maximal inhibitory concentration (IC50), demonstrating its potency as a metabolism-dependent inhibitor.
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| ln Vivo |
In vivo, 5-Hydroxylansoprazole sulfone is not a therapeutic agent but a metabolite. Its formation in the body contributes to the overall drug interaction profile of lansoprazole. By inhibiting CYP2C19, it can potentially alter the pharmacokinetics of other co-administered drugs that are metabolized by this enzyme, although its in vivo significance may be limited.
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| Enzyme Assay |
The in vitro enzyme assay for 5-Hydroxylansoprazole sulfone involves a CYP2C19 inhibition assay using human liver microsomes or recombinant CYP2C19 enzyme. The compound is pre-incubated with the enzyme and NADPH to allow for metabolism-dependent inhibition. Then, a probe substrate (e.g., omeprazole or S-mephenytoin) is added, and the formation of its metabolite is measured by LC-MS/MS. The decrease in metabolite formation indicates CYP2C19 inhibition.
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| Cell Assay |
Cellular in vitro experiments for this compound are not typically performed, as its primary use is in biochemical enzyme assays. It is a metabolite used to study enzyme kinetics and drug interactions in cell-free systems, not to assess cellular effects like cytotoxicity or proliferation.
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| Animal Protocol |
In vivo animal experiments are not conducted with this compound as a primary test agent. Instead, it is studied as a metabolite formed after administration of lansoprazole. The formation and disposition of 5-Hydroxylansoprazole sulfone are measured in pharmacokinetic studies to understand the metabolism of the parent drug.
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| References |
| CAS # |
131927-00-9
|
|---|---|
| PubChem CID |
90478568
|
| Appearance |
Typically exists as solid at room temperature
|
| Hydrogen Bond Donor Count |
2
|
| Hydrogen Bond Acceptor Count |
9
|
| Rotatable Bond Count |
5
|
| Heavy Atom Count |
27
|
| Complexity |
613
|
| Defined Atom Stereocenter Count |
0
|
| SMILES |
OC1=CC=C2N=C(S(=O)(CC3=NC=CC(OCC(F)(F)F)=C3C)=O)NC2=C1
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| Synonyms |
AG1909 AG-1909 AG 1909
|
| 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) |
May dissolve in DMSO (in most cases), if not, try other solvents such as H2O, Ethanol, or DMF with a minute amount of products to avoid loss of samples
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|---|---|
| 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.) |
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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