| Size | Price | |
|---|---|---|
| 500mg | ||
| 1g | ||
| Other Sizes |
| Targets |
The primary molecular target of Zanapezil is acetylcholinesterase (AChE), the enzyme responsible for hydrolyzing acetylcholine in the synaptic cleft. By inhibiting AChE, Zanapezil increases acetylcholine levels and enhances cholinergic transmission in brain regions involved in memory and cognition. The compound may also inhibit butyrylcholinesterase with lower potency.
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|---|---|
| ln Vitro |
In vitro, Zanapezil fumarate inhibits acetylcholinesterase with IC50 values in the nanomolar range, as determined by Ellman's assay using purified enzyme or brain homogenates. It demonstrates selectivity for AChE over BuChE and exhibits competitive or mixed-type inhibition kinetics.
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| ln Vivo |
In vivo, Zanapezil fumarate improves cognitive performance in animal models of cholinergic deficit. In rats with scopolamine-induced memory impairment, Zanapezil reverses deficits in passive avoidance and Morris water maze tasks. The compound also increases brain acetylcholine levels as measured by microdialysis.
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| Enzyme Assay |
For AChE inhibition assays, purified human or rat brain AChE is incubated with Zanapezil fumarate at various concentrations in phosphate buffer. Acetylthiocholine is added as substrate, and thiocholine production is measured by reaction with DTNB at 412 nm. IC50 values are calculated from dose-response curves.
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| Cell Assay |
For in vitro neuroprotection assays, primary cortical neurons or SH-SY5Y cells are treated with amyloid-beta or glutamate in the presence or absence of Zanapezil fumarate. Cell viability is assessed by MTT or LDH release assays. For cholinergic function, acetylcholine release from brain slices is measured by HPLC.
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| Animal Protocol |
For in vivo cognitive studies, rats receive scopolamine to induce memory impairment, followed by Zanapezil fumarate by oral gavage. Passive avoidance and Morris water maze tests are performed. For neurochemical studies, brain microdialysis is used to measure extracellular acetylcholine levels. In clinical trials, patients with Alzheimer's disease receive Zanapezil fumarate, and cognitive function is assessed by ADAS-cog and MMSE.
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| References |
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| Additional Infomation |
Zanapezil fumarate is a polymer.
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| Molecular Formula |
C29H36N2O5
|
|---|---|
| Molecular Weight |
492.606548309326
|
| Exact Mass |
492.262
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| CAS # |
263248-42-6
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| Related CAS # |
Zanapezil free base;142852-50-4
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| PubChem CID |
5282215
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| Appearance |
White to off-white solid powder
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| Boiling Point |
547ºC at 760mmHg
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| Flash Point |
284.6ºC
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| LogP |
5.097
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| Hydrogen Bond Donor Count |
3
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| Hydrogen Bond Acceptor Count |
7
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| Rotatable Bond Count |
8
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| Heavy Atom Count |
36
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| Complexity |
598
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| Defined Atom Stereocenter Count |
0
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| SMILES |
C1CCNC2=C(C1)C=CC(=C2)C(=O)CCC3CCN(CC3)CC4=CC=CC=C4.C(=C/C(=O)O)\C(=O)O
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| InChi Key |
CWEHWZPCDBRUNO-WLHGVMLRSA-N
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| InChi Code |
InChI=1S/C25H32N2O.C4H4O4/c28-25(23-11-10-22-8-4-5-15-26-24(22)18-23)12-9-20-13-16-27(17-14-20)19-21-6-2-1-3-7-21;5-3(6)1-2-4(7)8/h1-3,6-7,10-11,18,20,26H,4-5,8-9,12-17,19H2;1-2H,(H,5,6)(H,7,8)/b;2-1+
|
| Chemical Name |
3-(1-benzylpiperidin-4-yl)-1-(2,3,4,5-tetrahydro-1H-1-benzazepin-8-yl)propan-1-one;(E)-but-2-enedioic acid
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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, 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) |
May dissolve in DMSO (in most cases), if not, try other solvents such as H2O, Ethanol, or DMF with a minute amount of products to avoid loss of samples
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|---|---|
| Solubility (In Vivo) |
Note: Listed below are some common formulations that may be used to formulate products with low water solubility (e.g. < 1 mg/mL), you may test these formulations using a minute amount of products to avoid loss of samples.
Injection Formulations
Injection Formulation 1: DMSO : Tween 80： Saline = 10 : 5 : 85 (i.e. 100 μL DMSO stock solution → 50 μL Tween 80 → 850 μL Saline)(e.g. IP/IV/IM/SC) *Preparation of saline: Dissolve 0.9 g of sodium chloride in 100 mL ddH ₂ O to obtain a clear solution. Injection Formulation 2: DMSO : PEG300 ：Tween 80 : Saline = 10 : 40 : 5 : 45 (i.e. 100 μL DMSO → 400 μLPEG300 → 50 μL Tween 80 → 450 μL Saline) Injection Formulation 3: DMSO : Corn oil = 10 : 90 (i.e. 100 μL DMSO → 900 μL Corn oil) Example: Take the Injection Formulation 3 (DMSO : Corn oil = 10 : 90) as an example, if 1 mL of 2.5 mg/mL working solution is to be prepared, you can take 100 μL 25 mg/mL DMSO stock solution and add to 900 μL corn oil, mix well to obtain a clear or suspension solution (2.5 mg/mL, ready for use in animals). View More
Injection Formulation 4: DMSO : 20% SBE-β-CD in saline = 10 : 90 [i.e. 100 μL DMSO → 900 μL (20% SBE-β-CD in saline)] Oral Formulations
Oral Formulation 1: Suspend in 0.5% CMC Na (carboxymethylcellulose sodium) Oral Formulation 2: Suspend in 0.5% Carboxymethyl cellulose Example: Take the Oral Formulation 1 (Suspend in 0.5% CMC Na) as an example, if 100 mL of 2.5 mg/mL working solution is to be prepared, you can first prepare 0.5% CMC Na solution by measuring 0.5 g CMC Na and dissolve it in 100 mL ddH2O to obtain a clear solution; then add 250 mg of the product to 100 mL 0.5% CMC Na solution, to make the suspension solution (2.5 mg/mL, ready for use in animals). View More
Oral Formulation 3: Dissolved in PEG400 (Please use freshly prepared in vivo formulations for optimal results.) |
| Preparing Stock Solutions | 1 mg | 5 mg | 10 mg | |
| 1 mM | 2.0300 mL | 10.1500 mL | 20.3000 mL | |
| 5 mM | 0.4060 mL | 2.0300 mL | 4.0600 mL | |
| 10 mM | 0.2030 mL | 1.0150 mL | 2.0300 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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