| Size | Price | Stock | Qty |
|---|---|---|---|
| 5mg |
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| 10mg |
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| 50mg |
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| Other Sizes |
| Targets |
α1 repector
alpha1 receptor (inhibitor/antagonist) |
|---|---|
| ln Vitro |
No specific in vitro assays for the metabolite are provided. The parent compound Mebeverine is a potent alpha1 receptor inhibitor that causes relaxation of the gastrointestinal tract. O-Desmethyl Mebeverine alcohol is a major metabolite formed by O-demethylation, contributing to the pharmacological activity of the parent drug.
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| ln Vivo |
Cellular activity data for the metabolite are not specifically reported. Mebeverine and its metabolites act on alpha1-adrenergic receptors on gastrointestinal smooth muscle cells, blocking receptor-mediated contraction and promoting smooth muscle relaxation. This spasmolytic effect is clinically useful for treating irritable bowel syndrome (IBS) and other functional GI disorders.
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| Enzyme Assay |
Radioligand binding assays for alpha1-adrenergic receptors are performed using membrane preparations from rat brain cortex or transfected cells. [3H]-prazosin is used as the radioligand. Test compound (the metabolite or parent Mebeverine) is incubated with membranes at varying concentrations. Bound radioligand is separated by filtration and counted by scintillation. Ki values are calculated from competition curves to determine alpha1 receptor binding affinity.
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| Cell Assay |
Cell-based functional assays for alpha1-adrenergic antagonism use HEK-293 cells expressing human alpha1A receptors with calcium-sensitive fluorescent dye. Cells are seeded in 96-well plates and treated with serial dilutions of O-Desmethyl Mebeverine alcohol hydrochloride. Phenylephrine is added to activate the receptor, and intracellular calcium increase is measured by fluorescence. Antagonist potency (IC50) is determined from concentration-response curves.
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| Animal Protocol |
In vivo animal studies for Mebeverine and its metabolites typically involve oral administration to rats or dogs, followed by blood and tissue collection at multiple time points. HPLC or LC-MS/MS analysis quantifies both parent drug and metabolites including O-Desmethyl Mebeverine alcohol. The metabolite may be identified as a major circulating species contributing to pharmacological activity.
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| ADME/Pharmacokinetics |
O-Desmethyl Mebeverine alcohol is a Phase I metabolite formed via O-demethylation of Mebeverine, likely by cytochrome P450 enzymes (e.g., CYP2D6 or CYP3A4). It is expected to contribute to the pharmacological effects of Mebeverine as an alpha1 receptor inhibitor. The metabolite shows measurable plasma exposure following oral administration of the parent drug.
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| Toxicity/Toxicokinetics |
As a research standard and metabolite, O-Desmethyl Mebeverine alcohol hydrochloride is not intended for therapeutic use. The parent drug Mebeverine has an established clinical safety profile as an approved spasmolytic agent for irritable bowel syndrome, with common side effects including mild gastrointestinal disturbances, dizziness, and headache.
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| Additional Infomation |
O-Desmethyl Mebeverine alcohol hydrochloride is a key metabolite reference standard for pharmacokinetic and metabolic studies of Mebeverine. The parent drug Mebeverine was first approved in Europe for the treatment of IBS and other functional GI disorders. This metabolite is essential for identifying major metabolic pathways and for bioanalytical method development to quantitate both parent drug and metabolites in biological samples.
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| Molecular Formula |
C15H26CLNO2
|
|---|---|
| Molecular Weight |
287.825443744659
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| Exact Mass |
287.165
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| CAS # |
856620-39-8
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| Related CAS # |
Mebeverine-d6 hydrochloride;1329647-20-2;O-Desmethyl Mebeverine alcohol;155172-67-1
|
| PubChem CID |
129012195
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| Appearance |
White to off-white solid powder
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| Hydrogen Bond Donor Count |
3
|
| Hydrogen Bond Acceptor Count |
3
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| Rotatable Bond Count |
8
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| Heavy Atom Count |
19
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| Complexity |
203
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| Defined Atom Stereocenter Count |
0
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| SMILES |
CCN(CCCCO)C(C)CC1=CC=C(C=C1)O.Cl
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| InChi Key |
BWCVTLCWTXRTLL-UHFFFAOYSA-N
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| InChi Code |
InChI=1S/C15H25NO2.ClH/c1-3-16(10-4-5-11-17)13(2)12-14-6-8-15(18)9-7-14;/h6-9,13,17-18H,3-5,10-12H2,1-2H3;1H
|
| Chemical Name |
4-[2-[ethyl(4-hydroxybutyl)amino]propyl]phenol;hydrochloride
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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, 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)
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| Solubility (In Vitro) |
H2O: ≥ 75 mg/mL (260.57 mM)
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|---|---|
| Solubility (In Vivo) |
Solubility in Formulation 1: 100 mg/mL (347.43 mM) in PBS (add these co-solvents sequentially from left to right, and one by one), clear solution; with sonication.
(Please use freshly prepared in vivo formulations for optimal results.) |
| Preparing Stock Solutions | 1 mg | 5 mg | 10 mg | |
| 1 mM | 3.4743 mL | 17.3714 mL | 34.7427 mL | |
| 5 mM | 0.6949 mL | 3.4743 mL | 6.9485 mL | |
| 10 mM | 0.3474 mL | 1.7371 mL | 3.4743 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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