| Size | Price | Stock | Qty |
|---|---|---|---|
| 1mg |
|
||
| 50mg | |||
| Other Sizes |
| Targets |
Muscarinic acetylcholine receptors (mAChR). Tridihexethyl chloride is an antagonist of mAChR with antimuscarinic and anticholinergic activities. It effectively blocks acetylcholine receptors.
|
|---|---|
| ln Vitro |
In vitro, Tridihexethyl chloride acts as an mAChR antagonist with antimuscarinic and anticholinergic activities. It effectively blocks acetylcholine receptors, reducing parasympathetic tone. The compound shows pronounced antispasmodic and antisecretory effects on the gastrointestinal tract.
|
| ln Vivo |
In vivo, Tridihexethyl chloride is used to treat acquired nystagmus and peptic ulcer disease. It reduces stomach acid secretion and intestinal spasms. The compound is orally active and shows pronounced antispasmodic and antisecretory effects on the gastrointestinal tract. It has been studied for its effects on gastrointestinal motility and secretion.
|
| Enzyme Assay |
Non-cell receptor binding assays are performed using membrane preparations from cells expressing muscarinic acetylcholine receptor subtypes (M1-M5). Radioligand binding studies are conducted using [³H]N-methylscopolamine or [³H]QNB as tracers. Membranes are incubated with the radioligand and varying concentrations of Tridihexethyl chloride (0.001-100 μM). Nonspecific binding is determined with excess atropine. After incubation at 25°C for 60-90 minutes, filtration and scintillation counting are performed. Ki values are calculated from competition curves.
|
| Cell Assay |
Cellular functional assays are performed using cells expressing muscarinic acetylcholine receptors. Cells are treated with Tridihexethyl chloride at concentrations ranging from 0.01 nM to 100 μM. Inhibition of carbachol-induced calcium mobilization is measured using fluorescent calcium indicators (e.g., Fluo-4). The IC₅₀ for inhibition of receptor activation is calculated from dose-response curves. Alternatively, inhibition of forskolin-stimulated cAMP accumulation is measured for M2/M4 subtypes.
|
| Animal Protocol |
In vivo animal studies are conducted in rodent models of gastrointestinal motility and secretion. Tridihexethyl chloride is administered orally or intraperitoneally at doses ranging from 0.1-10 mg/kg. Gastric acid secretion is measured by pylorus ligation or gastric perfusion. Intestinal motility is assessed by charcoal transit or isolated organ bath studies. Efficacy against nystagmus is evaluated in appropriate animal models.
|
| ADME/Pharmacokinetics |
Tridihexethyl chloride is orally active. The compound is a quaternary ammonium compound with limited central nervous system penetration due to its charged nature. It is absorbed from the gastrointestinal tract and acts systemically on peripheral muscarinic receptors. Further pharmacokinetic parameters such as half-life, clearance, and metabolism are available in the primary literature.
|
| Toxicity/Toxicokinetics |
Common adverse effects of Tridihexethyl chloride include dry mouth, blurred vision, constipation, urinary retention, and tachycardia, consistent with anticholinergic pharmacology. No significant organ-specific toxicity has been reported at therapeutic doses. The compound is contraindicated in patients with glaucoma, obstructive uropathy, and gastrointestinal obstruction.
|
| References |
|
| Additional Infomation |
Tridihexylethyl chloride is an organochloride salt. It contains a tridihexylethyl group.
Tridihexethyl chloride (Pathilon chloride) is an orally active anticholinergic agent and mAChR antagonist used clinically for the treatment of peptic ulcer disease and acquired nystagmus. It shows pronounced antispasmodic and antisecretory effects on the gastrointestinal tract. The compound is a quaternary ammonium compound. It is available as a prescription medication in some countries. |
| Molecular Formula |
C21H36CLNO
|
|---|---|
| Molecular Weight |
353.969645500183
|
| Exact Mass |
353.249
|
| CAS # |
4310-35-4
|
| Related CAS # |
125-99-5 (iodide);4310-35-4 (chloride);60-49-1 (cation);
|
| PubChem CID |
20298
|
| Appearance |
White to off-white solid powder
|
| LogP |
1.725
|
| Hydrogen Bond Donor Count |
1
|
| Hydrogen Bond Acceptor Count |
2
|
| Rotatable Bond Count |
8
|
| Heavy Atom Count |
24
|
| Complexity |
319
|
| Defined Atom Stereocenter Count |
0
|
| SMILES |
[Cl-].OC(C1C=CC=CC=1)(CC[N+](CC)(CC)CC)C1CCCCC1
|
| InChi Key |
XJGONMZLEDGBRM-UHFFFAOYSA-M
|
| InChi Code |
InChI=1S/C21H36NO.ClH/c1-4-22(5-2,6-3)18-17-21(23,19-13-9-7-10-14-19)20-15-11-8-12-16-20/h7,9-10,13-14,20,23H,4-6,8,11-12,15-18H2,1-3H31H/q+1/p-1
|
| Chemical Name |
3-cyclohexyl-N,N,N-triethyl-3-hydroxy-3-phenylpropan-1-aminium chloride
|
| Synonyms |
PathilonPropethonumTridihexethyl Tridihexethyl chloride.
|
| HS Tariff Code |
2934.99.9001
|
| Storage |
Powder -20°C 3 years 4°C 2 years In solvent -80°C 6 months -20°C 1 month Note: (1). This product requires protection from light (avoid light exposure) during transportation and storage. (2). Please store this product in a sealed and protected environment (e.g. under nitrogen), 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)
|
| 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
|
|---|---|
| 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.) |
| Preparing Stock Solutions | 1 mg | 5 mg | 10 mg | |
| 1 mM | 2.8251 mL | 14.1255 mL | 28.2510 mL | |
| 5 mM | 0.5650 mL | 2.8251 mL | 5.6502 mL | |
| 10 mM | 0.2825 mL | 1.4125 mL | 2.8251 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.
Products are for research use only; We do not sell to patients
Copyright 2020 InvivoChem LLC | All Rights Reserved
