| Size | Price | Stock | Qty |
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| 100mg |
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| 500mg |
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| Other Sizes |
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| Targets |
The target of Aceclidine is the muscarinic acetylcholine receptor, particularly the M3 subtype.
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| ln Vivo |
In Vivo: 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 |
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 |
1979 rat LD50 subcutaneous 225 mg/kg Arzneimittel-Forschung. Drug Research., 18(320), 1968
1979 rat LD50 intravenous 45 mg/kg Arzneimittel-Forschung. Drug Research., 18(320), 1968 1979 mouse LD50 oral 165 mg/kg BEHAVIORAL: TREMOR; BEHAVIORAL: CONVULSIONS OR EFFECT ON SEIZURE THRESHOLD; GASTROINTESTINAL: CHANGES IN STRUCTURE OR FUNCTION OF SALIVARY GLANDS Arzneimittel-Forschung. Drug Research., 18(320), 1968 1979 mouse LD50 intraperitoneal 78 mg/kg BEHAVIORAL: TREMOR; BEHAVIORAL: ANALGESIA Archives Internationales de Pharmacodynamie et de Therapie., 189(295), 1971 [PMID:5548767] 1979 mouse LD50 subcutaneous 102 mg/kg BEHAVIORAL: TREMOR; BEHAVIORAL: CONVULSIONS OR EFFECT ON SEIZURE THRESHOLD; GASTROINTESTINAL: CHANGES IN STRUCTURE OR FUNCTION OF SALIVARY GLANDS Arzneimittel-Forschung. Drug Research., 18(320), 1968 |
| References | |
| Additional Infomation |
Acetic acid 1-azabicyclo[2.2.2]octan-3-yl ester is a member of quinuclidines.
Aceclidine has been marketed in Europe but has not been used clinically in the United States. It is used in the treatment of open-angle glaucoma and is a parasympathomimetic agent. 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 |
| Molecular Formula |
C9H15NO2
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|---|---|
| Molecular Weight |
169.22
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| Exact Mass |
169.11
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| Elemental Analysis |
C, 63.88; H, 8.93; N, 8.28; O, 18.91
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| CAS # |
827-61-2
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| Related CAS # |
6109-70-2 (HCl racemic);827-61-2 (free base racemic);59653-40-6 (R-isomer);59653-42-8 (S-isomer);
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| PubChem CID |
1979
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| Appearance |
Off-white to light yellow <34°C powder,>36°C liquid
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| Boiling Point |
221.5ºC at 760 mmHg
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| Flash Point |
85ºC
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| LogP |
0.581
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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 |
2
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| Heavy Atom Count |
12
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| Complexity |
185
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| Defined Atom Stereocenter Count |
0
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| SMILES |
O=C(C)OC1C2CCN(CC2)C1
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| InChi Key |
WRJPSSPFHGNBMG-UHFFFAOYSA-N
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| InChi Code |
InChI=1S/C9H15NO2/c1-7(11)12-9-6-10-4-2-8(9)3-5-10/h8-9H,2-6H2,1H3
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| Chemical Name |
1-Azabicyclo(2.2.2)octan-3-ol, acetate (ester)
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| Synonyms |
Glaucostat; Aceclidine; NSC-657843; aceclidine; 827-61-2; 3-Acetoxyquinuclidine; 3-Quinuclidinol acetate (ester); Aceclidina; Aceclidinum; 3-Quinuclidinol acetate; 1-Azabicyclo(2.2.2)octan-3-ol, acetate (ester); NSC657843; NSC 657843
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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 |
| 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 (~590.95 mM)
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|---|---|
| Solubility (In Vivo) |
Solubility in Formulation 1: ≥ 2.5 mg/mL (14.77 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 25.0 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: ≥ 2.5 mg/mL (14.77 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 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: ≥ 2.5 mg/mL (14.77 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 | 5.9095 mL | 29.5473 mL | 59.0947 mL | |
| 5 mM | 1.1819 mL | 5.9095 mL | 11.8189 mL | |
| 10 mM | 0.5909 mL | 2.9547 mL | 5.9095 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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