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Purity: ≥98%
Acetylcholine Chloride (ACh chloride; Ovisot; TL-1505; TL-1505) is an organic chemical and a common neurotransmitter found in the central and peripheral nerve system that functions in the brain and body of many types of animals, including humans, as a neurotransmitter—a chemical released by nerve cells to send signals to other cells. Its name is derived from its chemical structure: it is an ester of acetic acid and choline. Parts in the body that use or are affected by acetylcholine are referred to as cholinergic. Substances that interfere with acetylcholine activity are called anticholinergics. is
| Targets |
Muscarinic acetylcholine receptors (M1-M5) and nicotinic acetylcholine receptors (nAChRs) [1]
- Acetylcholine receptors on cultured sweat gland epithelial cells (subtype unspecified) [3] - Receptors mediating proinflammatory cytokine regulation in sepsis-related cell models (subtype unspecified) [4] |
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| ln Vitro |
While sweat gland epithelial cell fluorescence values and intracellular free calcium are decreased in calcium-free myocardium, cardiac choline chloride (ACh chloride; 10 μM) calcium channel, fluorescence values, and intracellular free calcium are significantly increased in hypercalcium myocardium [3].
Treatment of cultured sweat gland epithelial cells with Acetylcholine Chloride (10⁻⁸ M to 10⁻⁴ M) induced a concentration-dependent increase in intracellular calcium concentration ([Ca²⁺]i); the response was partially inhibited by muscarinic receptor antagonists, indicating involvement of muscarinic receptors [3] - Acetylcholine Chloride (5 mM, 10 mM) inhibited the aggregation of p53 mutant peptide in vitro, with a maximum inhibition rate of approximately 40% at 10 mM; dynamic light scattering analysis showed reduced average particle size of p53 mutant peptide aggregates after treatment [5] |
| ln Vivo |
In mice, acetylcholine chloride (ACh chloride; SC; 20 mg/kg; single dose) significantly increases cholinergic stimulation and morbidity [4].
In a mouse sepsis model induced by cecal ligation and puncture (CLP), intraperitoneal administration of Acetylcholine Chloride (10 μg/kg) 30 minutes after CLP significantly reduced mortality within 72 hours (mortality rate decreased from ~80% to ~40%) [4] - Acetylcholine Chloride treatment in septic mice decreased the serum levels of proinflammatory cytokines, including tumor necrosis factor-α (TNF-α) and interleukin-6 (IL-6), compared to untreated septic controls [4] - In starved rats (fasted for 72 hours), ileal hypersecretion was observed, and Acetylcholine Chloride administration enhanced cholinergic-mediated intestinal secretion, as indicated by increased ileal fluid and electrolyte excretion [2] |
| Enzyme Assay |
For muscarinic acetylcholine receptor binding assay: Membrane fractions containing M1-M5 receptors were prepared from relevant tissues, then incubated with Acetylcholine Chloride at different concentrations in the presence of a radiolabeled acetylcholine agonist. After incubation, unbound ligands were removed by filtration, and the radioactivity of the bound fraction was measured to determine the binding affinity and specificity [1]
- For nicotinic acetylcholine receptor binding assay: Purified nAChRs from neural or muscle tissues were mixed with Acetylcholine Chloride and a fluorescent-labeled nicotinic antagonist. The binding reaction was monitored by fluorescence polarization, and the displacement of the labeled antagonist by Acetylcholine Chloride was used to calculate binding parameters [1] |
| Cell Assay |
Cultured sweat gland epithelial cell calcium concentration assay: Sweat gland epithelial cells were seeded in culture plates and loaded with a calcium-sensitive fluorescent probe. After stabilization, Acetylcholine Chloride was added at concentrations ranging from 10⁻⁸ M to 10⁻⁴ M, and the fluorescence intensity was measured continuously for 5-10 minutes to assess changes in intracellular calcium concentration. Parallel experiments with muscarinic receptor antagonists were conducted to verify receptor subtype involvement [3]
- p53 mutant peptide aggregation inhibition assay: Recombinant p53 mutant peptide was dissolved in buffer, and Acetylcholine Chloride was added to final concentrations of 5 mM and 10 mM. The mixture was incubated at 37°C for 24 hours, then analyzed by dynamic light scattering to measure particle size distribution and by SDS-PAGE to detect aggregate formation [5] |
| Animal Protocol |
Animal/Disease Models: Male and female inbred albino mice weighing 18-22 grams (sepsis) [4]
Doses: 20 mg/kg Route of Administration: subcutaneous injection; single dose Experimental Results: Dramatically diminished intraperitoneal (ip) injection of 2×109 large intestine Mortality of mice with sepsis caused by bacilli and blood levels of pro-inflammatory cytokines TNF-α, IL-1β, and IL-6. Mouse sepsis model: Male mice were anesthetized, and sepsis was induced by cecal ligation and puncture (CLP). Thirty minutes after CLP, Acetylcholine Chloride was administered via intraperitoneal injection at a dose of 10 μg/kg. Control groups received equal volumes of normal saline. Mice were monitored for mortality over 72 hours, and serum samples were collected at 24 hours post-CLP to measure proinflammatory cytokine levels [4] - Rat starvation-induced ileal hypersecretion model: Male rats were fasted for 72 hours to induce ileal hypersecretion. The ileum was excised and mounted in Ussing chambers, then Acetylcholine Chloride was added to the mucosal or serosal side of the ileal tissue at unspecified concentrations. Transepithelial electrical resistance and short-circuit current were measured to evaluate intestinal secretion function [2] |
| References |
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| Additional Infomation |
Acetylcholine chloride is the chloride form of acetylcholine and is a parasympathomimetic drug. It contains acetylcholine. Acetylcholine chloride is the chloride form of acetylcholine, a synthetic quaternary ammonium amino alcohol with cholinergic properties. Acetylcholine chloride mimics the parasympathomimetic effects of the endogenous compound acetylcholine. When administered as an ophthalmic solution, this drug stimulates cholinergic receptors in the iris sphincter, leading to pupillary constriction. (NCI05) Acetylcholine is a neurotransmitter found at the neuromuscular junction, autonomic ganglia, parasympathetic effector junctions, some sympathetic effector junctions, and in multiple locations within the central nervous system. See also: acetylcholine (with active moiety); chloride ion (with moiety); acetylcholine chloride; histamine; serotonin (component)... See more...
Acetylcholine chloride is an endogenous neurotransmitter that mediates signal transmission in the central and peripheral nervous systems as a ligand for cholinergic receptors (muscarinic and nicotinic types)[1] - Its biological functions include regulating glandular secretion (e.g., sweat glands, intestinal glands), smooth muscle contraction, neurotransmission, and immune response regulation[1][3][2][4] - As a cation osmotic regulator, acetylcholine chloride has the ability to inhibit protein aggregation, which may have potential implications for diseases associated with abnormal protein aggregation[5] - The cholinergic system, with acetylcholine chloride as a key mediator, plays a crucial role in maintaining intestinal epithelial barrier function and regulating inflammatory responses[1][2][4] |
| Molecular Formula |
C7H16NO2.CL
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| Molecular Weight |
181.66
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| Exact Mass |
181.086
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| CAS # |
60-31-1
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| Related CAS # |
Acetylcholine iodide;2260-50-6;Acetylcholine bromide;66-23-9;Acetylcholine-d4 chloride;344298-94-8;Acetylcholine-d9 chloride;344298-95-9
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| PubChem CID |
6060
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| Appearance |
White to off-white solid powder
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| Melting Point |
146-150 °C(lit.)
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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 |
4
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| Heavy Atom Count |
11
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| Complexity |
115
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| Defined Atom Stereocenter Count |
0
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| InChi Key |
JUGOREOARAHOCO-UHFFFAOYSA-M
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| InChi Code |
InChI=1S/C7H16NO2.ClH/c1-7(9)10-6-5-8(2,3)4;/h5-6H2,1-4H3;1H/q+1;/p-1
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| Chemical Name |
2-acetyloxyethyl(trimethyl)azanium;chloride
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| Synonyms |
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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. |
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| 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) |
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| Solubility (In Vivo) |
Solubility in Formulation 1: ≥ 2.08 mg/mL (11.45 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 (11.45 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 (11.45 mM) (saturation unknown) in 10% DMSO + 90% Corn Oil (add these co-solvents sequentially from left to right, and one by one), clear solution. Solubility in Formulation 4: 23.33 mg/mL (128.43 mM) in PBS (add these co-solvents sequentially from left to right, and one by one), clear solution; with ultrasonication. |
| Preparing Stock Solutions | 1 mg | 5 mg | 10 mg | |
| 1 mM | 5.5048 mL | 27.5239 mL | 55.0479 mL | |
| 5 mM | 1.1010 mL | 5.5048 mL | 11.0096 mL | |
| 10 mM | 0.5505 mL | 2.7524 mL | 5.5048 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.
| NCT Number | Recruitment | interventions | Conditions | Sponsor/Collaborators | Start Date | Phases |
| NCT06219590 | Recruiting | Procedure: Acetylcholine Iontophoresis Procedure: Shame Acetylcholine Iontophoresis |
Type 2 Diabetes Mellitus Peripheral Neuropathy |
South Valley University | October 28, 2023 | Not Applicable |
| NCT01137656 | Completed | Drug: Acetylcholine and Blood | Healthy | Mark Gladwin | April 2010 | Phase 1 |
| NCT03636100 | Terminated | Device: Cryoballoon ablation | Atrial Fibrillation | Saint Luke's Health System | August 15, 2018 | |
| NCT05618132 | Recruiting | Diagnostic Test: Acetylcholine rechallenge | Angina Pectoris, Variant Angina Pectoris; Spasm-Induced Angina Pectoris With Normal Coronary Arteriogram | University Hospital, Antwerp | January 9, 2023 | Not Applicable |
| NCT06180252 | Completed | Diagnostic Test: PET with 11C MP4 | Alzheimer Disease | IRCCS San Raffaele | May 12, 2004 |
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