ZSET1446
Based on 1 Customer Validation
ZSET1446 is a novel cognitive enhancer that significantly improves learning deficits in various types of Alzheimer disease (AD) models.
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- Pureté: 98.33%
- CAS No.: 887603-94-3
- Formule: C15H12N2O
- Masse moléculaire:236.27
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Stockage:Powder -20°C, 3 years , 4°C, 2 years ; In solvent -80°C, 2 years , -20°C, 1 year
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Activité biologique
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Chemical Information
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Solvant et solubilité
- Protocole
- Pureté et documentation
- Références
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Help & FAQs
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Activité biologique
ZSET1446 (100 pM-10 nM) exerts limited effects on the basal neuronal excitability and synaptic transmission. ZSET1446 potentiates the facilitatory effect of nAChR stimulation on sPSC frequency. ZSET1446 potentiates the increase in sIPSC frequency by local application of nicotine (5 μM; 2 minutes) without affecting the basal sIPSC frequency at the range of 10 pM to 1 nM[1].
MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.
MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.
| NCT Number | Sponsor | Condition | Start Date |
Phase
|
|---|---|---|---|---|
| NCT01329991 | Plexxikon| | 2011-05 | PHASE1 |
Chemical Information
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CAS No. 887603-94-3
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Appearance Solid
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Masse moléculaire 236.27
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Formule C15H12N2O
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Color Light yellow to khaki
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SMILES
O=C1N=C2C=CC=CN2C13CC4=C(C=CC=C4)C3
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Synonyms
ST-101
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Livraison
Room temperature in continental US; may vary elsewhere.
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Stockage
Powder -20°C 3 years 4°C 2 years In solvent -80°C 2 years -20°C 1 year
Solvant et solubilité
DMSO : 50 mg/mL (211.62 mM; Need ultrasonic; Hygroscopic DMSO has a significant impact on the solubility of product, please use newly opened DMSO)
Please refer to the solubility information to select the appropriate solvent. Once prepared, please aliquot and store the solution to prevent product inactivation from repeated freeze-thaw cycles.
Storage method and period of stock solution: -80°C, 2 years; -20°C, 1 year. When stored at -80°C, please use it within 2 years. When stored at -20°C, please use it within 1 year.
Please refer to the solubility information to select the appropriate solvent. Once prepared, please aliquot and store the solution to prevent product inactivation from repeated freeze-thaw cycles.
Storage method and period of stock solution: -80°C, 2 years; -20°C, 1 year. When stored at -80°C, please use it within 2 years. When stored at -20°C, please use it within 1 year.
Concentration (start) × Volume (start) = Concentration (final) × Volume (final)
Select the appropriate dissolution method based on your experimental animal and administration route.
- For the following dissolution methods, please ensure to first prepare a clear stock solution using an In Vitro approach and then sequentially add co-solvents:
- To ensure reliable experimental results, the clarified stock solution can be appropriately stored based on storage conditions. As for the working solution for In Vivo experiments, it is recommended to prepare freshly and use it on the same day.
- The percentages shown for the solvents indicate their volumetric ratio in the final prepared solution. If precipitation or phase separation occurs during preparation, heat and/or sonication can be used to aid dissolution.
Add each solvent one by one: 10% DMSO 40% PEG300 5% Tween-80 45% Saline
Solubility: ≥ 2.5 mg/mL (10.58 mM); Clear solution
This protocol yields a clear solution of ≥ 2.5 mg/mL (saturation unknown).
Taking 1 mL working solution as an example, add 100 μL DMSO stock solution (25.0 mg/mL) to 400 μL PEG300, and mix evenly; then add 50 μL Tween-80 and mix evenly; then add 450 μL Saline to adjust the volume to 1 mL.
Preparation of Saline: Dissolve 0.9 g sodium chloride in ddH₂O and dilute to 100 mL to obtain a clear Saline solution.
Add each solvent one by one: 10% DMSO 90% (20% SBE-β-CD in Saline)
Solubility: ≥ 2.5 mg/mL (10.58 mM); Clear solution
This protocol yields a clear solution of ≥ 2.5 mg/mL (saturation unknown).
Taking 1 mL working solution as an example, add 100 μL DMSO stock solution (25.0 mg/mL) to 900 μL 20% SBE-β-CD in Saline, and mix evenly.
Preparation of 20% SBE-β-CD in Saline (4°C, storage for one week): 2 g SBE-β-CD powder is dissolved in 10 mL Saline, completely dissolve until clear.
Please enter the basic information of animal experiments:
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Recommended: Prepare an additional quantity of animals to account for potential losses during experiments.
Please enter your animal formula composition:
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%DMSO +
Recommended: Keep the proportion of DMSO in working solution below 2% if your animal is weak.
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%+
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+%Tween-80 + +
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%Saline +
The co-solvents required include: DMSO, . All of co-solvents are available by MedChemExpress (MCE). , Tween 80. All of co-solvents are available by MedChemExpress (MCE).
Working solution concentration: 0.22 mg/mL
Method for preparing stock solution: mg drug dissolved in μL DMSO. Stock solution concentration: mg/mL.
1. Take μL DMSO stock solution;
2. Add μL .
μL , mix evenly;
3. Then add μL Tween 80, mix evenly;
4. Then add μL
Please ensure that the stock solution in the first step is dissolved to a clear state, and add co-solvents in sequence. You can use ultrasonic heating (ultrasonic cleaner, recommended frequency 20-40 kHz), vortexing, etc. to assist dissolution.
Protocole
The experimental apparatus consists of a Plexiglas open-field box [25 cm (width) × 41 cm (length) × 17 cm (depth), model TP-105], the floor of which is covered with sawdust. The apparatus is located in a sound-attenuated room. The procedure for the novel object recognition task consists of three different sessions: habituation, training, and retention sessions. Each mouse is individually habituated to the box, with 10 min of exploration in the absence of objects (day 1: habituation session). ZSET1446 at doses of 0.001, 0.003, 0.01, and 0.03 mg/kg and/or memantine at doses of 3 and 10 mg/kg is orally administered 60 min before the training trial. In the experiment of injection of nicotinic receptor antagonists, oral administration of ZSET1446 and i.p. injection of mechamylamine or DHbE at each dose of 1 mg/kg are given 60 min before the training trial. During the training session, two different novel objects are symmetrically fixed to the floor in the box, and each animal is allowed to explore in the box for 10 min (day 2: training session). These objects are different in shape and color but similar in size. The mice are considered to be exploring the object when the mouse is facing, touching, or sniffing the object. The time spent for exploring each object is manuallymeasured by a stopwatch. In the training session, locomotor activity is simultaneously measured for a period of 10 min automatically, using an Animex Auto placed under the open-field box. After the training trial, mice are immediately returned to their home cages.
MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.
Pureté et documentation
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Fiche technique (284 KB)
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SDS (251 KB)
- English - EN (251 KB)
- Français - FR (251 KB)
- Deutsch - DE (251 KB)
- Norwegian - NO (251 KB)
- Español - ES (251 KB)
- Swedish - SV (251 KB)
- Italian - IT (251 KB)
- Portuguese - PT (251 KB)
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Instruction de manipulation (2659 KB)
Références
[1]. Takeda K, et al. Potentiation of Acetylcholine-Mediated Facilitation of Inhibitory Synaptic Transmission by an Azaindolizione Derivative, ZSET1446 (ST101), in the Rat Hippocampus. J Pharmacol Exp Ther. 2016 Feb;356(2):445-55 [Content Brief]
[2]. Yamaguchi Y, et al. Combination effects of ZSET1446/ST101 with memantine on cognitive function and extracellular acetylcholine in the hippocampus. J Pharmacol Sci. 2013;123(4):347-55. Epub 2013 Nov 29. [Content Brief]
[3]. Yamaguchi Y, et al. Effects of ZSET1446/ST101 on cognitive deficits and amyloid β deposition in the senescence accelerated prone mouse brain. J Pharmacol Sci. 2012;119(2):160-6. [Content Brief]
Complete Stock Solution Preparation Table
Please refer to the solubility information to select the appropriate solvent. Once prepared, please aliquot and store the solution to prevent product inactivation from repeated freeze-thaw cycles.
Storage method and period of stock solution: -80°C, 2 years; -20°C, 1 year. When stored at -80°C, please use it within 2 years. When stored at -20°C, please use it within 1 year.
| Optional Solvent | Concentration Solvent Mass | 1 mg | 5 mg | 10 mg | 25 mg |
|---|---|---|---|---|---|
| DMSO | 1 mM | 4.2324 mL | 21.1619 mL | 42.3237 mL | 105.8094 mL |
| 5 mM | 0.8465 mL | 4.2324 mL | 8.4647 mL | 21.1619 mL | |
| 10 mM | 0.4232 mL | 2.1162 mL | 4.2324 mL | 10.5809 mL | |
| 15 mM | 0.2822 mL | 1.4108 mL | 2.8216 mL | 7.0540 mL | |
| 20 mM | 0.2116 mL | 1.0581 mL | 2.1162 mL | 5.2905 mL | |
| 25 mM | 0.1693 mL | 0.8465 mL | 1.6929 mL | 4.2324 mL | |
| 30 mM | 0.1411 mL | 0.7054 mL | 1.4108 mL | 3.5270 mL | |
| 40 mM | 0.1058 mL | 0.5290 mL | 1.0581 mL | 2.6452 mL | |
| 50 mM | 0.0846 mL | 0.4232 mL | 0.8465 mL | 2.1162 mL | |
| 60 mM | 0.0705 mL | 0.3527 mL | 0.7054 mL | 1.7635 mL | |
| 80 mM | 0.0529 mL | 0.2645 mL | 0.5290 mL | 1.3226 mL | |
| 100 mM | 0.0423 mL | 0.2116 mL | 0.4232 mL | 1.0581 mL |
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