| Size | Price | Stock | Qty |
|---|---|---|---|
| 100mg |
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| Other Sizes |
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| Targets |
mAChR1; mAChR3; muscarinic acetylcholine receptor, particularly the M3 subtype. No specific IC50, Ki, or EC50 values were reported [2]
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|---|---|
| ln Vivo |
Aceclidine (1-10 mg/kg, subcutaneous injection) hydrochloride can reverse hemicholinium-3-induced spatial learning deficits in rats[4].
Aceclidine was evaluated for its effect on refractive errors of the eye. In animal models, topical administration of formulations containing Aceclidine resulted in a reduction of myopia, as measured by changes in refractive error. The effect was observed to be dose-dependent, with higher concentrations of the compound leading to more significant improvements in refractive status [1] In experiments where spatial learning was impaired by hemicholinium-3, administration of Aceclidine reversed the deficit. This reversal was demonstrated through improved performance in spatial learning tasks, indicating a role in enhancing cholinergic neurotransmission related to memory and learning [4] |
| Animal Protocol |
For assessing effects on refractive errors, animals with induced myopia were treated with topical ophthalmic formulations containing Aceclidine. The formulations were applied to the eye(s) at specified frequencies (e.g., once or twice daily) for a defined period. Refractive error was measured using retinoscopy or similar techniques before and after treatment to evaluate efficacy [1]
In studies on spatial learning, animals were first administered hemicholinium-3 to impair spatial learning. Subsequently, Aceclidine was administered via a specified route (e.g., intraperitoneal injection) at a defined dose. Animals were then tested in spatial learning tasks (e.g., maze tests) to assess reversal of the impairment, with performance metrics recorded and compared to controls [4] |
| Toxicity/Toxicokinetics |
170367 rat LD50 intraperitoneal 105 mg/kg AUTONOMIC NERVOUS SYSTEM: OTHER (DIRECT) PARASYMPATHOMIMETIC Arzneimittel-Forschung. Drug Research., 18(322), 1968 [PMID:5696008]
170367 rat LD50 subcutaneous 225 mg/kg Farmakologiya i Toksikologiya, 23(398), 1960 [PMID:13767763] 170367 rat LD50 intravenous 45 mg/kg Farmakologiya i Toksikologiya, 23(398), 1960 [PMID:13767763] 170367 mouse LD50 oral 165 mg/kg Farmakologiya i Toksikologiya, 23(398), 1960 [PMID:13767763] 170367 mouse LD50 intraperitoneal 116 mg/kg AUTONOMIC NERVOUS SYSTEM: OTHER (DIRECT) PARASYMPATHOMIMETIC Arzneimittel-Forschung. Drug Research., 18(322), 1968 [PMID:5696008] |
| References | |
| Additional Infomation |
Aceclidine is a cholinergic agent that acts as a modulator of muscarinic acetylcholine receptors, with a focus on the M3 subtype. It is formulated in storage-stable compositions, often with other excipients to enhance stability and efficacy, for topical ophthalmic use in treating refractive errors such as myopia [1]
[2] Its ability to reverse hemicholinium-3-induced spatial learning deficits suggests it enhances cholinergic function, which is critical for memory and cognitive processes [4] |
| Molecular Formula |
C9H16CLNO2
|
|---|---|
| Molecular Weight |
205.68
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| Exact Mass |
205.08695
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| Elemental Analysis |
, 52.56; H, 7.84; Cl, 17.24; N, 6.81; O, 15.56
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| CAS # |
6109-70-2
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| Related CAS # |
Aceclidine;827-61-2;Aceclidine-d3 hydrochloride;2713384-81-5
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| Appearance |
White to off-white solid powder
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| SMILES |
CC(=O)OC1CN2CCC1CC2.Cl
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| Synonyms |
Quinuclidin-3-yl acetate hydrochloride; Aceclidine hydrochloride; 6109-70-2; Aceclidine HCl; 3-Acetoxyquinuclidine hydrochloride; C 162 D; 3B22O325Q6; 1-Azabicyclo(2.2.2)octan-3-ol, acetate (ester), hydrochloride; 1-Azabicyclo(2.2.2)octan-3-ol, 3-acetate, hydrochloride (1:1);
|
| 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 : ~100 mg/mL (~486.19 mM; with ultrasonication)
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|---|---|
| Solubility (In Vivo) |
Solubility in Formulation 1: ≥ 2.5 mg/mL (12.15 mM)(saturation unknown) in 10% DMSO 40% PEG300 5% Tween-80 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 25.0 mg/mL clear DMSO stock solution and add it to 400 μL PEG300, mix well; then add 50 μL Tween-80 to the above system, mix well; then continue to add 450 μL of normal saline to make up to 1 mL. Preparation of normal saline: Dissolve 0.9 g of sodium chloride in ddH₂O and make up to 100 mL to obtain a clear and transparent normal saline solution. Solubility in Formulation 2: ≥ 2.5 mg/mL (12.15 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 25.0 mg/mL clear DMSO stock solution and add it to 900 μL of 20% SBE-β-CD saline solution and mix well. 2 g SBE-β-CD (sulfobutyl ether β-cyclodextrin) powder is diluted to 10 mL of saline and completely dissolved until clear and transparent. Solubility in Formulation 3: ≥ 2.5 mg/mL (12.15 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 25.0 mg/mL clear DMSO stock solution and add it to 900 μL corn oil and mix well. (Please use freshly prepared in vivo formulations for optimal results.) |
| Preparing Stock Solutions | 1 mg | 5 mg | 10 mg | |
| 1 mM | 4.8619 mL | 24.3096 mL | 48.6192 mL | |
| 5 mM | 0.9724 mL | 4.8619 mL | 9.7238 mL | |
| 10 mM | 0.4862 mL | 2.4310 mL | 4.8619 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 |
| NCT05431543 | Completed | Drug: Aceclidine+Brimonidine combination ophthalmic solution |
Presbyopia Refractive Errors |
Alisyn Facemire | August 6, 2022 | Phase 2 |
| NCT05294328 | Completed | Drug: Aceclidine+Brimonidine combination ophthalmic solution |
Presbyopia Refractive Errors |
LENZ Therapeutics, Inc | May 5, 2022 | Phase 2 |
| NCT05936489 | Completed | Drug: Aceclidine + Brimonidine Drug: Aceclidine |
Eye Diseases Presbyopia |
LENZ Therapeutics, Inc | July 6, 2023 | Phase 1 |
| NCT03201562 | Completed Has Results | Drug: Aceclidine+tropicamide combination |
Presbyopia | LENZ Therapeutics, Inc | April 30, 2017 | Phase 2 |
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