| Size | Price | Stock | Qty |
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| 1mg |
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| 5mg |
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| 10mg | |||
| Other Sizes |
| Targets |
Acetylcholinesterase (AChE)
(R)-Donepezil targets acetylcholinesterase (AChE), acting as a potent and specific inhibitor. It has the R configuration. By inhibiting AChE, it prevents the breakdown of acetylcholine, thereby enhancing cholinergic neurotransmission. Its enantiomeric purity makes it a valuable tool for studying stereospecific interactions with AChE. |
|---|---|
| ln Vitro |
In cell-free enzyme assays, (R)-Donepezil inhibits AChE activity with high potency. It has shown promise in improving cognitive function and mitigating symptoms of Alzheimer's disease in preclinical models. Its potency in inhibiting AChE may be enhanced compared to the racemate. Cellular assays for (R)-Donepezil are conducted using neuronal cell lines. Cells are treated with the compound, and markers of cholinergic function, such as acetylcholine levels, are measured. Its neuroprotective effects can be assessed in models of neurodegeneration. Studies on its stereoselective metabolism and transport have been conducted in vitro.
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| ln Vivo |
In vivo, (R)-Donepezil has shown promise in improving cognitive function in preclinical models of Alzheimer's disease. It is studied in animal models to assess its effects on memory, learning, and neurodegeneration. Its pharmacokinetic and pharmacodynamic properties may differ from those of the (S)-enantiomer.
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| Enzyme Assay |
Cell-free enzyme inhibition assays for (R)-Donepezil are performed using purified AChE enzyme. The enzyme is incubated with varying concentrations of the compound and a chromogenic substrate. The rate of substrate hydrolysis is measured spectrophotometrically, and the IC50 value is determined from the inhibition curve.
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| Cell Assay |
Cellular assays for (R)-Donepezil are conducted using neuronal cell lines. Cells are treated with the compound, and AChE activity is measured. The accumulation of acetylcholine can be quantified. Neuroprotective effects can be assessed in models of neurodegeneration. Studies on its stereoselective transport are also performed.
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| Animal Protocol |
In vivo studies on (R)-Donepezil are conducted in rodent models of cognitive impairment. The compound is administered orally or via injection, and its effects on memory and learning are assessed using behavioral tests. Brain AChE inhibition and acetylcholine levels are also measured.
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| ADME/Pharmacokinetics |
The pharmacokinetic properties of (R)-Donepezil are consistent with those of a central nervous system drug. It is able to cross the blood-brain barrier. Its stereoselective metabolism and transport have been studied in vitro. The (R)-enantiomer may exhibit different PK parameters compared to the (S)-enantiomer.
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| Toxicity/Toxicokinetics |
Preclinical toxicity data for (R)-Donepezil are likely aligned with the safety profile of donepezil. It is generally well-tolerated at therapeutic doses. Comprehensive toxicological studies have been conducted for the racemic mixture.
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| References |
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| Additional Infomation |
(R)-Donepezil is a 2-[(1-benzylpiperidin-4-yl)methyl]-5,6-dimethoxyindan-1-one with the R configuration. It is the conjugate base of (R)-donepezil (1+) and the enantiomer of (S)-donepezil.
(R)-Donepezil is a research compound used to study the stereospecific pharmacology of AChE inhibition. Its enantiomeric purity makes it a valuable tool for understanding the differences between enantiomers in terms of potency, metabolism, and transport. It is not approved for clinical use as a single enantiomer. |
| Molecular Formula |
C24H29NO3
|
|---|---|
| Molecular Weight |
379.491966962814
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| Exact Mass |
379.21475
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| Elemental Analysis |
C, 75.96; H, 7.70; N, 3.69; O, 12.65
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| CAS # |
142698-19-9
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| Related CAS # |
Donepezil;120014-06-4
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| PubChem CID |
1150567
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| Appearance |
White to off-white solid powder
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| LogP |
4.71
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| Hydrogen Bond Donor Count |
0
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| Hydrogen Bond Acceptor Count |
4
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| Rotatable Bond Count |
6
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| Heavy Atom Count |
28
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| Complexity |
510
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| Defined Atom Stereocenter Count |
1
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| SMILES |
C1(=O)C2=C(C=C(OC)C(OC)=C2)C[C@H]1CC1CCN(CC2=CC=CC=C2)CC1
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| InChi Key |
ADEBPBSSDYVVLD-HXUWFJFHSA-N
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| InChi Code |
InChI=1S/C24H29NO3/c1-27-22-14-19-13-20(24(26)21(19)15-23(22)28-2)12-17-8-10-25(11-9-17)16-18-6-4-3-5-7-18/h3-7,14-15,17,20H,8-13,16H2,1-2H3/t20-/m1/s1
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| Chemical Name |
(2R)-2-[(1-benzylpiperidin-4-yl)methyl]-5,6-dimethoxy-2,3-dihydroinden-1-one
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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: 200 mg/mL (527.02 mM)
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|---|---|
| Solubility (In Vivo) |
Solubility in Formulation 1: ≥ 5 mg/mL (13.18 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 (13.18 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 50.0 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: ≥ 5 mg/mL (13.18 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 | 2.6351 mL | 13.1756 mL | 26.3512 mL | |
| 5 mM | 0.5270 mL | 2.6351 mL | 5.2702 mL | |
| 10 mM | 0.2635 mL | 1.3176 mL | 2.6351 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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