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1mg |
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5mg |
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10mg |
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Other Sizes |
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ln Vitro |
In homogenates of the rat cerebral cortex, zanapezil (TAK-147) free base exhibits a strong and reversible suppression of AChE activity (IC50=51.2 nM). Its potency is 3.0- and 2.4-fold greater than that of tacrine and physostigmine, respectively. The least effective inhibitor of butyrylcholinesterase activity in rat plasma is zanapezil free base (IC50=23,500 nM)[1]. Noradrenaline and serotonin absorption is considerably inhibited by zanapezil free base, with IC50 values of 4020 and 1350 nM, respectively[1]. With Ki values of 324, 2330, and 3510 nM, respectively, zanapezil free base also inhibits ligand binding to alpha-1, alpha-2, and serotonin 2 receptors[1].
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ln Vivo |
In the rat brain, oral treatment of Zanapezil (TAK-147; 3 mg/kg) free base markedly increased the rates of dopamine, noradrenaline, and serotonin turnover. In ex vivo investigations, oral injection of 1–10 mg/kg of Zanapezil free base causes a statistically significant and dose-dependent decrease in AChE activity in the cerebral cortex[1]. For 120 minutes, the ventral hippocampus (VH) considerably raises its ACh level when zanapezil (TAK-147; 5 and 10 mg/kg) is given free base[2].
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Animal Protocol |
Animal/Disease Models: Male Wistar rats 7 weeks in age (230-240 g)[2]
Doses: 5 and 10 mg/kg Route of Administration: Oral administration Experimental Results: Increased acetylcholine (ACh) level in the VH for 120 min. |
References |
[1]. K Hirai, et al. Neurochemical effects of 3-[1-(phenylmethyl)-4-piperidinyl]-1-(2,3,4,5-tetrahydro-1H-1-b enzazepin-8-yl)-1-propanone fumarate (TAK-147), a novel acetylcholinesterase inhibitor, in rats. J Pharmacol Exp Ther. 1997 Mar;280(3):1261-9.
[2]. Izzettin Hatip-Al-Khatib,et al. Comparison of the effect of TAK-147 (zanapezil) and E-2020 (donepezil) on extracellular acetylcholine level and blood flow in the ventral hippocampus of freely moving rats. Brain Res. 2004 Jun 25;1012(1-2):169-76. |
Molecular Formula |
C25H32N2O
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Molecular Weight |
376.53
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CAS # |
142852-50-4
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Related CAS # |
Zanapezil fumarate;263248-42-6
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Appearance |
Typically exists as solids (or liquids in special cases) at room temperature
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SMILES |
C1=CC=C(CN2CCC(CCC(C3=CC=C4CCCCNC4=C3)=O)CC2)C=C1
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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) |
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 | 2.6558 mL | 13.2792 mL | 26.5583 mL | |
5 mM | 0.5312 mL | 2.6558 mL | 5.3117 mL | |
10 mM | 0.2656 mL | 1.3279 mL | 2.6558 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.