| Size | Price | Stock | Qty |
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| 5mg |
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| 10mg |
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| 50mg |
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| 100mg | |||
| Other Sizes |
| Targets |
4-DAMP targets muscarinic acetylcholine receptors. Its affinity profile, determined by recombinant human receptor binding, is M3 (Ki = 0.37 nM) ≈ M1 (Ki = 0.57 nM) ≈ M5 (Ki = 0.55 nM) > M4 (Ki = 0.72 nM) >> M2 (Ki = 7.3 nM). It has a pKi of 9.3 for the M3 receptor. By binding to these receptors, it blocks the action of acetylcholine.
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| ln Vitro |
In vitro, 4-DAMP is characterized by its high affinity and selectivity for muscarinic receptor subtypes. It is a potent antagonist at the M3 receptor (pKi = 9.3) and has high affinity for the M5 receptor (pKi = 8.9). It is routinely used in pharmacological assays to study the regulation and function of the M3 receptor and to differentiate M3/M1-mediated responses from M2-mediated effects in tissue preparations.
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| ln Vivo |
In vivo, 4-DAMP is used as a research tool to study the physiological roles of muscarinic receptors in animal models. By specifically blocking M3 and M1 receptors, it can help elucidate their involvement in various functions such as smooth muscle contraction, glandular secretion, and central nervous system processes. Its selectivity allows for pharmacological dissection of cholinergic pathways in vivo.
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| Enzyme Assay |
The in vitro receptor binding assay for 4-DAMP typically involves radioligand binding studies. A tritiated derivative, [3H]4-DAMP, is available and binds with high affinity (Kd = 0.2 nM) to M1 and M3 receptors. The assay is performed using membrane preparations from cells expressing recombinant human muscarinic receptors. The ability of unlabeled 4-DAMP to compete with the radioligand is measured to calculate its Ki values for different receptor subtypes.
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| Cell Assay |
In vitro cellular studies are conducted using cell lines that express specific muscarinic receptor subtypes, such as CHO-K1 cells transfected with human M1-M5 receptors. Cells are treated with 4-DAMP to measure its functional antagonism, typically by assessing its ability to inhibit agonist-induced intracellular calcium mobilization or other downstream signaling pathways. This allows for detailed pharmacological characterization of the compound.
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| Animal Protocol |
In vivo animal experiments with 4-DAMP are conducted in various research models to study cholinergic function. For example, it may be administered to rodents to investigate its effects on airway constriction, bladder function, or cognitive processes. The route of administration and dosage vary depending on the specific experimental question, and the compound's effects are measured via physiological or behavioral endpoints.
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| ADME/Pharmacokinetics |
4-DAMP has a molecular formula of C21H26INO2 and a molecular weight of 451.34 g/mol. It is soluble in DMSO (100 mM) and ethanol (25 mM). It is typically supplied as a white to off-white solid with ≥98% purity. It is stable at room temperature for shipping and should be stored under standard laboratory conditions.
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| Toxicity/Toxicokinetics |
As a research chemical, 4-DAMP is not intended for human use. Its toxicological profile is primarily known from its use as a pharmacological tool in vitro and in animal models. At high concentrations, it may exhibit effects typical of muscarinic antagonists. Standard laboratory safety precautions should be followed when handling this compound. It is not a drug for therapeutic applications.
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| References | |
| Additional Infomation |
4-DAMP methyl iodide is a quaternary ammonium salt prepared by reacting equimolar amounts of 4-diphenylacetoxy-N-methylpiperidine and iodomethane. It acts as both a muscarinic receptor antagonist and a cholinergic receptor antagonist. It is both a quaternary ammonium salt and an iodide salt. It contains 4-DAMP(1+).
4-DAMP is a standard pharmacological tool for probing muscarinic receptor function. It is available as a tritiated radioligand ([3H]4-DAMP) and as an irreversible alkylating derivative (4-DAMP mustard) for receptor inactivation studies. Its unique selectivity profile makes it a superior choice over other antagonists like pirenzepine or methoctramine for isolating M3 and M1 receptor responses. |
| Molecular Formula |
C21H26NO2+.I-
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|---|---|
| Molecular Weight |
451.34064
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| Exact Mass |
451.1
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| CAS # |
1952-15-4
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| Related CAS # |
81405-11-0 (Parent)
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| PubChem CID |
3014059
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| Appearance |
White to off-white solid powder
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| LogP |
0.563
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| Hydrogen Bond Donor Count |
0
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| Hydrogen Bond Acceptor Count |
3
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| Rotatable Bond Count |
5
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| Heavy Atom Count |
25
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| Complexity |
380
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| Defined Atom Stereocenter Count |
0
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| InChi Key |
WWJHRSCUAQPFQO-UHFFFAOYSA-M
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| InChi Code |
InChI=1S/C21H26NO2.HI/c1-22(2)15-13-19(14-16-22)24-21(23)20(17-9-5-3-6-10-17)18-11-7-4-8-12-18;/h3-12,19-20H,13-16H2,1-2H3;1H/q+1;/p-1
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| Chemical Name |
(1,1-dimethylpiperidin-1-ium-4-yl) 2,2-diphenylacetate;iodide
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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 (e.g. under nitrogen), avoid exposure to moisture and light. |
| 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 (~221.56 mM)
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| Solubility (In Vivo) |
Solubility in Formulation 1: ≥ 5 mg/mL (11.08 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 50.0 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: ≥ 5 mg/mL (11.08 mM) (saturation unknown) in 10% DMSO + 90% Corn Oil (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 50.0 mg/mL clear DMSO stock solution to 900 μL of corn oil and mix evenly. (Please use freshly prepared in vivo formulations for optimal results.) |
| Preparing Stock Solutions | 1 mg | 5 mg | 10 mg | |
| 1 mM | 2.2156 mL | 11.0781 mL | 22.1562 mL | |
| 5 mM | 0.4431 mL | 2.2156 mL | 4.4312 mL | |
| 10 mM | 0.2216 mL | 1.1078 mL | 2.2156 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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