| Size | Price | |
|---|---|---|
| Other Sizes |
Purity: =99.9%
| 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 subcutaneous LD50 225 mg/kg Arzneimittel-Forschung. Drug Research., 18(320), 1968
1979 rat LD50 intravenous injection 45 mg/kg Arzneimittel-Forschung. Drug Research., 18(320), 1968 1979 mouse oral LD50 165 mg/kg Behavior: tremor; Behavior: convulsions or effects on epileptic threshold; Gastrointestinal: changes in salivary gland structure or function Arzneimittel-Forschung. Drug Research, 18(320), 1968 1979 mouse intraperitoneal injection LD50 78 mg/kg, behavioral manifestations: tremor; behavioral manifestations: analgesia. International Archives of Pharmacodynamics and Therapeutics, 189(295), 1971 [PMID:5548767] In 1979, the subcutaneous LD50 in mice was 102 mg/kg. Behavioral manifestations included tremor; seizures or effects on the epilepsy threshold; and gastrointestinal changes such as altered salivary gland structure or function. Drug Research, 18(320), 1968 |
| References | |
| Additional Infomation |
1-azabicyclo[2.2.2]oct-3-yl acetate belongs to the quinine ring class of compounds. Aceclidin is marketed in Europe but not yet clinically used in the United States. It is used to treat open-angle glaucoma and is a parasympathomimetic drug. Aceclidin is a cholinergic drug that acts as a modulator of muscarinic acetylcholine receptors, primarily targeting the M3 subtype. It is formulated into storage-stable preparations, often with the addition of other excipients to improve stability and efficacy, and is used in topical ophthalmic treatment of refractive errors such as myopia.
|
| Molecular Formula |
C9H15NO2
|
|---|---|
| Molecular Weight |
169.22
|
| Exact Mass |
169.11
|
| Elemental Analysis |
C, 63.88; H, 8.93; N, 8.28; O, 18.91
|
| CAS # |
827-61-2
|
| Related CAS # |
6109-70-2 (HCl racemic);827-61-2 (free base racemic);59653-40-6 (R-isomer);59653-42-8 (S-isomer);
|
| PubChem CID |
1979
|
| Appearance |
Off-white to light yellow <34°C powder,>36°C liquid
|
| Boiling Point |
221.5ºC at 760 mmHg
|
| Flash Point |
85ºC
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| LogP |
0.581
|
| Hydrogen Bond Donor Count |
0
|
| Hydrogen Bond Acceptor Count |
3
|
| Rotatable Bond Count |
2
|
| Heavy Atom Count |
12
|
| Complexity |
185
|
| Defined Atom Stereocenter Count |
0
|
| SMILES |
O=C(C)OC1C2CCN(CC2)C1
|
| InChi Key |
WRJPSSPFHGNBMG-UHFFFAOYSA-N
|
| InChi Code |
InChI=1S/C9H15NO2/c1-7(11)12-9-6-10-4-2-8(9)3-5-10/h8-9H,2-6H2,1H3
|
| Chemical Name |
1-Azabicyclo(2.2.2)octan-3-ol, acetate (ester)
|
| 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
|
| 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)
|
| 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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