| Size | Price | Stock | Qty |
|---|---|---|---|
| 5mg |
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| 10mg |
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| 50mg |
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| 100mg | |||
| Other Sizes |
| Targets |
alpha1-adrenergic receptor (indirect). Mebeverine alcohol is a metabolite of Mebeverine. While Mebeverine itself is a potent alpha1 receptor inhibitor that causes relaxation of the gastrointestinal tract, the alcohol metabolite is significantly less active at the target receptor compared to the parent drug. In the context of research, it serves as a negative control or a marker for drug exposure, as its primary role is in drug metabolism studies rather than direct pharmacological activity.
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| ln Vitro |
Specific in vitro potency data for mebeverine alcohol alone is not provided in the search results. It is well-documented that the primary ester hydrolysis product is significantly less potent than the parent drug, Mebeverine, which typically has IC₅0 values in the low nanomolar range for alpha1 receptor antagonism. Its formation is the primary route of clearance for mebeverine, preventing systemic toxicity from the parent compound.
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| ln Vivo |
In vivo, Mebeverine alcohol is formed rapidly and extensively after oral administration of Mebeverine HCl. Its plasma concentration profile is used to characterize the absorption and first-pass metabolism of the parent drug. The area under the curve (AUC) of mebeverine alcohol is much higher than that of the parent drug, confirming its role as the major circulating metabolite. It is not administered for therapeutic effects.
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| Enzyme Assay |
For metabolite stability, a microsomal assay can be used. Mebeverine alcohol (100 microM) is incubated with human liver microsomes (0.5 mg/mL) and NADPH (1 mM) in a 37degC water bath. Aliquots are taken at 0, 15, 30, 60 minutes. The reaction is stopped with cold acetonitrile containing an internal standard. After centrifugation, the supernatant is analyzed by LC-MS/MS to measure the disappearance of the compound and formation of secondary metabolites.
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| Cell Assay |
Human HepG2 hepatocytes or intestinal Caco-2 cells are seeded in 96-well plates and treated with various concentrations of Mebeverine alcohol (e.g., 1-500 microM) for 24-72 hours. Cell viability is assessed using an MTT or WST-1 assay. The culture supernatant is also collected to measure lactate dehydrogenase (LDH) release as a marker of cellular toxicity to determine the safety profile of the circulating metabolite.
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| Animal Protocol |
For pharmacokinetic studies, male Sprague-Dawley rats are cannulated. Mebeverine alcohol (e.g., 5 mg/kg) is dissolved in a vehicle (e.g., 5% DMSO in saline) and administered intravenously via the cannula. Blood samples are collected at timed intervals from the cannula. Plasma is separated and processed by protein precipitation with acetonitrile containing an internal standard. Samples are analyzed by LC-MS/MS.
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| ADME/Pharmacokinetics |
As a metabolite of Mebeverine, its pharmacokinetic profile is characterized by rapid appearance in plasma (Tmax typically < 1 hour) and a higher Cmax and AUC than the parent drug. The compound is lipophilic (LogP ~2.72) and has a molecular weight of 265.39. It is soluble in DMSO (100 mg/mL). The metabolite is eventually eliminated primarily via renal excretion after possible conjugation (glucuronidation).
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| Toxicity/Toxicokinetics |
Specific toxicology data for mebeverine alcohol is not detailed. However, as the primary metabolite of a drug used for gastrointestinal disorders, it is considered to have low inherent toxicity. The rapid metabolism of mebeverine to mebeverine alcohol is actually a detoxification step, as the parent drug can cause side effects. In cell culture assays, it is typically well-tolerated up to high micromolar concentrations.
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| Additional Infomation |
Mebeverine alcohol is a pharmacopoeial impurity standard (specifically EP Impurity C) and a research metabolite. It is not a drug and has no clinical therapeutic use. It is an essential reference standard for quality control of Mebeverine hydrochloride drug products and is used in bioanalytical laboratories to quantify mebeverine exposure in clinical studies and therapeutic drug monitoring (TDM).
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| Molecular Formula |
C16H27NO2
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|---|---|
| Molecular Weight |
265.39108
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| Exact Mass |
265.204
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| CAS # |
14367-47-6
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| Related CAS # |
Mebeverine alcohol-d5;2070015-15-3;Mebeverine-d6 hydrochloride;1329647-20-2
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| PubChem CID |
26649
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| Appearance |
Light yellow to yellow liquid
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| Density |
0.994g/cm3
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| Boiling Point |
386.4ºC at 760mmHg
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| Flash Point |
187.5ºC
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| Vapour Pressure |
1.16E-06mmHg at 25°C
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| Index of Refraction |
1.512
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| LogP |
2.72
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| Hydrogen Bond Donor Count |
1
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| Hydrogen Bond Acceptor Count |
3
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| Rotatable Bond Count |
9
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| Heavy Atom Count |
19
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| Complexity |
215
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| Defined Atom Stereocenter Count |
0
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| SMILES |
CCN(CCCCO)C(C)CC1=CC=C(C=C1)OC
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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 (~376.80 mM)
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|---|---|
| Solubility (In Vivo) |
Solubility in Formulation 1: ≥ 2.5 mg/mL (9.42 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 (9.42 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 (9.42 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 | 3.7680 mL | 18.8402 mL | 37.6804 mL | |
| 5 mM | 0.7536 mL | 3.7680 mL | 7.5361 mL | |
| 10 mM | 0.3768 mL | 1.8840 mL | 3.7680 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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