| Size | Price | Stock | Qty |
|---|---|---|---|
| 250mg |
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| 500mg |
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| Other Sizes |
| Targets |
Clidinium bromide targets muscarinic acetylcholine receptors. It competitively inhibits acetylcholine or other cholinergic stimuli at autonomic effectors innervated by postganglionic cholinergic nerves. It is a gastrointestinal muscarinic receptor antagonist. By blocking muscarinic receptors, it reduces gastric acid secretion and intestinal motility.
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| ln Vitro |
In vitro, Clidinium bromide is a potent anticholinergic agent. It acts as a muscarinic antagonist, blocking the effects of acetylcholine at muscarinic receptors. Its activity can be measured in receptor binding assays using membrane preparations expressing muscarinic receptors.
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| ln Vivo |
Mice that receive oral gavage (0.25, 0.5, and 1 mg/kg; 3 days) are constipated. Following clidinium administration, mice showed a substantial decrease in % transport [(F(3, 28)=27.405] [1]. The effects of clidinium (oral gavage; 0.25, 0.5, and 1 mg/kg; 3 days) on the PTZ-induced clonic epilepsy threshold were statistically significant [(F(3, 35) = 14.103][1].
In vivo, Clidinium bromide (oral gavage; 0.25, 0.5, and 1 mg/kg; 3 days) causes constipation in mice. It leads to a significant decrease in %transit after treatment. It is used to treat peptic ulcer disease and to relieve cramps or stomach spasms. |
| Enzyme Assay |
Clidinium bromide is evaluated in cell-free receptor binding assays to determine its affinity for muscarinic receptors. Radioligand binding displacement assays are performed using membrane preparations expressing muscarinic receptor subtypes. Competition binding experiments are conducted with increasing concentrations of Clidinium bromide and a fixed concentration of a labeled reference ligand.
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| Cell Assay |
Clidinium bromide is assessed in cell-based functional assays to measure its antagonist activity at muscarinic receptors. Cells expressing muscarinic receptors are treated with Clidinium bromide, and receptor activity is measured by assessing downstream signaling pathways, such as calcium mobilization or inhibition of cAMP accumulation.
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| Animal Protocol |
Animal/Disease Models: Male weighing 20-25 g NMRI mice[1]
Doses: 0.25, 0.5 and 1 mg/kg Route of Administration: po (oral gavage); 0.25, 0.5 and 1 mg/kg; 3 days Experimental Results: diminished clonic seizure latency compared to control animals . Clidinium bromide is administered orally in animal models to evaluate its antispasmodic and antisecretory effects. In mice, it is given at doses of 0.25, 0.5, and 1 mg/kg for 3 days. Efficacy is assessed by measuring intestinal transit time and gastric acid secretion. |
| ADME/Pharmacokinetics |
Clidinium bromide has a molecular weight of 432.35 and a molecular formula of C22H26BrNO3. It has a CAS number of 3485-62-9. The compound is a quaternary ammonium salt. It is soluble in water and should be stored under recommended conditions.
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| Toxicity/Toxicokinetics |
No detailed toxicity data is available for Clidinium bromide beyond its known use as an anticholinergic agent. It is generally well-tolerated but can cause side effects such as dry mouth, constipation, and blurred vision. The compound is a therapeutic agent and is available by prescription only.
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| References | |
| Additional Infomation |
Clidinium bromide is the bromide salt of clidinium. It is used to treat symptoms of peptic ulcers and can also be used to relieve abdominal or gastric cramps or spasms caused by colic, diverticulitis, and irritable bowel syndrome. It has parasympathetic blocking, antispasmodic, and antiarrhythmic effects. It is a quaternary ammonium salt and an organic bromide salt containing a clidinium group. Its structure is similar to that of benzoic acid and 3-quininecyclool.
See also: Chlordiazepoxide hydrochloride; Clidinium bromide (ingredient); Chlordiazepoxide; Clidinium bromide (ingredient). Clidinium bromide is also known as Ro 2-3773. It is a quaternary amine antimuscarinic agent. It is used in combination with chlordiazepoxide for the treatment of peptic ulcer disease and irritable bowel syndrome. The compound is a therapeutic agent. |
| Molecular Formula |
C22H26BRNO3
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|---|---|
| Molecular Weight |
432.35
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| Exact Mass |
431.109
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| CAS # |
3485-62-9
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| Related CAS # |
Clidinium-d5 bromide
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| PubChem CID |
19004
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| Appearance |
White to off-white solid powder
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| Melting Point |
240-241°C
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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 |
27
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| Complexity |
482
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| Defined Atom Stereocenter Count |
0
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| InChi Key |
GKEGFOKQMZHVOW-UHFFFAOYSA-M
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| InChi Code |
InChI=1S/C22H26NO3.BrH/c1-23-14-12-17(13-15-23)20(16-23)26-21(24)22(25,18-8-4-2-5-9-18)19-10-6-3-7-11-19;/h2-11,17,20,25H,12-16H2,1H3;1H/q+1;/p-1
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| Chemical Name |
(1-methyl-1-azoniabicyclo[2.2.2]octan-3-yl) 2-hydroxy-2,2-diphenylacetate;bromide
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| Synonyms |
Clidinii bromidum Quarzan Clidinium 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 : ~125 mg/mL (~289.12 mM)
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| Solubility (In Vivo) |
Solubility in Formulation 1: ≥ 2.08 mg/mL (4.81 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 (4.81 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 (4.81 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 | 2.3129 mL | 11.5647 mL | 23.1294 mL | |
| 5 mM | 0.4626 mL | 2.3129 mL | 4.6259 mL | |
| 10 mM | 0.2313 mL | 1.1565 mL | 2.3129 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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