| Size | Price | Stock | Qty |
|---|---|---|---|
| 100mg |
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| 1g |
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| 5g | |||
| Other Sizes |
| Targets |
mAChR
Mepenzolate Bromide targets muscarinic acetylcholine receptors (mAChRs), particularly the M2 and M3 subtypes. It acts as a competitive antagonist, inhibiting the binding of acetylcholine to muscarinic receptors in smooth muscle. This blocks downstream signaling cascades, leading to relaxation of smooth muscle in the gastrointestinal tract and other organs. It is also a GPR109A inhibitor. |
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| ln Vitro |
Mepenzolate not only has a muscarinic absorption mechanism that helps it reduce inflammation, but it also uses the same mechanism to help open up blood vessels. Mepenzoate, a non-muscarinic absorbent subtype, inhibits intestinal motility and dilates blood vessels, which are both attributed to its antagonistic action on M3R [1].
In vitro, mepenzolate bromide is a potent muscarinic antagonist with high affinity for human M2 and M3 receptors. It not only has a muscarinic absorption mechanism that helps it reduce inflammation, but it also uses the same mechanism to help open up blood vessels. It inhibits intestinal motility and dilates blood vessels, attributed to its antagonistic action on M3R. |
| ln Vivo |
Mepenzolate bromide is a GPR109A absorbent that eliminates the beneficial effects of acid on body weight, ductal wet weight, and myeloperoxidase (MPO) and VEGF levels [2]. Mepenzolate bromide is a muscarinic antagonist. Intratracheal inhalation or inhalation of mezoxate bromide reduces the severity of elastic inflation-induced cavity dilation and respiratory dysfunction. Due to its anti-inflammatory and bronchodilator activity, mezofosate may be a promising treatment for chronic obstructive pulmonary disease. Animal Model: Adult male Wistar rat, body weight 150-200 g [2] Dosage: 5 mg/kg Administration: Intraperitoneal injection Results : Eliminates niacin as an effective drug for chronic obstructive pulmonary disease (COPD) caused by iodoacetamide [3]. Colon wet weight and colonic MPO and VEGF levels. Animal models: ICR mice (4-6 weeks old, male) and DBA/2 mice (5 weeks old, female) [3] Doses: 0.04, 0.38, 3.8, 38 μg/kg; 45.2 and 226 μg per chamber Administration: "Intratracheal administration once daily for 14 days 0.04, 0.38, 3.8, 38 μg/kg Inhaled 45.2 and 226 μg per chamber once daily for 14 days" Results: Simultaneous daily intratracheal administration suppressed this This increase occurred in a dose-dependent manner. The inhalation route was similar to that observed with the intratracheal administration mode.
In vivo, mepenzolate bromide is a GPR109A absorbent that eliminates the beneficial effects of acid on body weight, ductal wet weight, and myeloperoxidase (MPO) and VEGF levels. Intratracheal inhalation or inhalation of mepenzolate bromide reduces the severity of elastic inflation-induced cavity dilation and respiratory dysfunction. Due to its anti-inflammatory and bronchodilator activity, it may be a promising treatment for COPD. |
| Enzyme Assay |
In vitro enzyme/receptor binding studies for mepenzolate bromide typically involve radioligand binding assays using membrane preparations from cells expressing human M2 and M3 receptors. Competitive binding experiments with labeled ligands such as [3H]-N-methylscopolamine are performed to determine Ki values. Standard protocols involve incubating membranes with increasing concentrations of mepenzolate in the presence of a fixed concentration of radioligand.
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| Cell Assay |
In vitro cellular assays for mepenzolate bromide involve culturing smooth muscle cells or other cells expressing muscarinic receptors. Cells are treated with serial dilutions of the compound, and receptor-mediated signaling, such as calcium mobilization or contractility, is measured. Anti-inflammatory activity may be assessed by measuring cytokine production. Cytotoxicity is evaluated using standard viability assays.
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| Animal Protocol |
Adult male Wistar rats, weighing 150-200 g
5 mg/kg Intraperitoneal injection In vivo animal studies for mepenzolate bromide include models of COPD, such as elastase-induced airspace enlargement in mice. Animals are treated with mepenzolate via intratracheal administration or inhalation. Endpoints include respiratory function, airspace enlargement, and inflammatory markers such as MPO and VEGF levels. Standard protocols include dose-response assessment and comparison to vehicle or reference treatments. |
| ADME/Pharmacokinetics |
Pharmacokinetic properties of mepenzolate bromide include a molecular weight of 420.34 and a molecular formula of C₂₁H₂₆BrNO₃. It is a quaternary ammonium compound. It is a solid powder. Detailed pharmacokinetic parameters such as half-life and bioavailability are available from preclinical studies. It is soluble in DMSO and other organic solvents.
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| Toxicity/Toxicokinetics |
Toxicological data for mepenzolate bromide indicate that it is generally well-tolerated at therapeutic doses. As an anticholinergic agent, it may cause side effects such as dry mouth, blurred vision, constipation, and urinary retention. It is contraindicated in patients with glaucoma, obstructive uropathy, and gastrointestinal obstruction. Overdose can lead to severe anticholinergic toxicity.
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| References |
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| Additional Infomation |
Mefenazole bromide is a diarylmethane.
Mepenzolate Bromide is a muscarinic antagonist used to treat gastrointestinal disorders. It is also known as Cantil. It is a post-ganglionic parasympathetic inhibitor that decreases gastric acid and pepsin secretion and suppresses spontaneous contractions of the colon. Its anti-inflammatory and bronchodilator activity has generated interest in its potential for treating COPD. It is not approved for human therapeutic use in many jurisdictions. |
| Molecular Formula |
C21H26BRNO3
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|---|---|
| Molecular Weight |
420.3400
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| Exact Mass |
419.11
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| Elemental Analysis |
C, 60.00; H, 6.23; Br, 19.01; N, 3.33; O, 11.42
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| CAS # |
76-90-4
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| Related CAS # |
25990-43-6 (Parent)
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| PubChem CID |
6461
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| Appearance |
White to off-white solid powder
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| Melting Point |
228-229ºC dec.
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| Hydrogen Bond Donor Count |
1
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| Hydrogen Bond Acceptor Count |
4
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| Rotatable Bond Count |
5
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| Heavy Atom Count |
26
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| Complexity |
432
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| Defined Atom Stereocenter Count |
0
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| SMILES |
[Br-].O(C(C(C1C([H])=C([H])C([H])=C([H])C=1[H])(C1C([H])=C([H])C([H])=C([H])C=1[H])O[H])=O)C1([H])C([H])([H])C([H])([H])C([H])([H])[N+](C([H])([H])[H])(C([H])([H])[H])C1([H])[H]
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| InChi Key |
JRRNZNSGDSFFIR-UHFFFAOYSA-M
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| InChi Code |
InChI=1S/C21H26NO3.BrH/c1-22(2)15-9-14-19(16-22)25-20(23)21(24,17-10-5-3-6-11-17)18-12-7-4-8-13-18;/h3-8,10-13,19,24H,9,14-16H2,1-2H3;1H/q+1;/p-1
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| Chemical Name |
(1,1-dimethylpiperidin-1-ium-3-yl) 2-hydroxy-2,2-diphenylacetate;bromide
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| Synonyms |
Cantil; Gastropidil; Cantilaque; Cantilon; mepenzolate iodide; mepenzolic acid; Mepenzolate Bromide
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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) |
DMSO: ~250 mg/mL (~594.8 mM)
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|---|---|
| Solubility (In Vivo) |
Solubility in Formulation 1: ≥ 2.08 mg/mL (4.95 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 20.8 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: ≥ 2.08 mg/mL (4.95 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 20.8 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: ≥ 2.08 mg/mL (4.95 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 | 2.3790 mL | 11.8951 mL | 23.7903 mL | |
| 5 mM | 0.4758 mL | 2.3790 mL | 4.7581 mL | |
| 10 mM | 0.2379 mL | 1.1895 mL | 2.3790 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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