| Size | Price | Stock | Qty |
|---|---|---|---|
| 1mg |
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| 5mg |
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| 10mg |
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| Other Sizes |
| Targets |
AChE
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|---|---|
| ln Vitro |
Zanapezil (TAK-147) has a potent and reversible inhibitory effect on AChE activity in rat cerebral cortex homogenates (IC50=51.2 nM), which is 3.0-fold and 2.4-fold more potent than Tacrine and Physostigmine. Zanapezil is the weakest inhibitor of butyrylcholinesterase activity in rat plasma (IC50=23,500 nM)[1]. Zanapezil moderately inhibits the uptake of norepinephrine and serotonin with IC50 values of 4020 and 1350 nM, respectively[1]. Zanapezil also inhibits ligand binding at α-1, α-2, and serotonin 2 receptors with Ki values of 324, 2330, and 3510 nM, respectively[1].
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| ln Vivo |
Zanapezil (TAK-147) (TAK-147; 3 mg/kg; po) significantly accelerates the turnover rate of dopamine, norepinephrine, and serotonin in the rat brain. In ex vivo experiments, Zanapezil (TAK-147) (1-10 mg/kg; po) caused a statistically significant dose-dependent decrease in cerebral cortical AChE activity [1]. Zanapezil (TAK-147) (TAK-147; 5 and 10 mg/kg; po) significantly increases AChE levels in the ventral hippocampus (VH) for 120 minutes [2].
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| References |
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| Additional Infomation |
Zanapazol fumarate is a polymer.
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| Molecular Formula |
C29H36N2O5
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|---|---|
| Molecular Weight |
492.61
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| Exact Mass |
492.262
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| CAS # |
142852-51-5
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| PubChem CID |
5282215
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| Appearance |
Solid powder
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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 |
O=C(C1C=CC2CCCCNC=2C=1)CCC1CCN(CC2C=CC=CC=2)CC1.OC(/C=C/C(=O)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+
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| 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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| Synonyms |
TAK-147
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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) |
DMSO : 100 mg/mL (203.00 mM; with sonication)
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|---|---|
| Solubility (In Vivo) |
Solubility in Formulation 1: ≥ 2.5 mg/mL (5.08 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, add 100 μL of 25.0 mg/mL clear DMSO stock solution to 400 μL PEG300 and mix well; then add 50 μL Tween-80 to the above system and mix well; then add 450 μL saline to make up 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 (5.08 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, add 100 μL of 25.0 mg/mL clear DMSO stock solution to 900 μL of 20% SBE-β-CD in saline and mix well. *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. Solubility in Formulation 3: ≥ 2.5 mg/mL (5.08 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, add 100 μL of 25.0 mg/mL clear DMSO stock solution 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 | 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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