1. Membrane Transporter/Ion Channel Neuronal Signaling
  2. Calcium Channel nAChR
  3. ZSET1446

ZSET1446 is a novel cognitive enhancer that significantly improves learning deficits in various types of Alzheimer disease (AD) models.

For research use only. We do not sell to patients.

ZSET1446 Chemical Structure

ZSET1446 Chemical Structure

CAS No. : 887603-94-3

Size Price Stock Quantity
Solid + Solvent
10 mM * 1 mL in DMSO
ready for reconstitution
USD 260 In-stock
Solution
10 mM * 1 mL in DMSO USD 260 In-stock
Solid
1 mg USD 100 In-stock
5 mg USD 225 In-stock
10 mg USD 315 In-stock
25 mg USD 630 In-stock
50 mg USD 1050 In-stock
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Customer Review

Based on 1 publication(s) in Google Scholar

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  • Biological Activity

  • Protocol

  • Purity & Documentation

  • References

  • Customer Review

Description

ZSET1446 is a novel cognitive enhancer that significantly improves learning deficits in various types of Alzheimer disease (AD) models.

In Vitro

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.

In Vivo

ZSET1446 enhances object recognition memory in mice and ameliorates cognitive impairment caused by scopolamine in rats. Concomitant administration of subeffective doses of ZSET1446 and memantine significantly ameliorates the cognitive performance in the novel object recognition task in both mice and rats. Moreover, oral administration of ZSET1446 or memantine increases the extracellular level of ACh in the hippocampus as compared with the control. Further, concomitant administration of subeffective doses of ZSET1446 and memantine significantly increases the extracellular level of ACh as compared with the group of ZSET1446 or memantine alone[2]. ZSET1446 (0.002, 0.01, and 0.1 mg/kg, p.o.) ameliorates cognitive deficits of SAMP8 after 4, 8, 12, and 16 weeks of treatment in a novel object recognition test. ZSET1446 also reduces grading scores of SAMP8 after 16 weeks of treatment. Further, 8-week treatment of ZSET1446 significantly reduces the total number of Aβ-positive granules in the hippocampus[3].

MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.

Clinical Trial
Molecular Weight

236.27

Formula

C15H12N2O

CAS No.
Appearance

Solid

Color

Light yellow to khaki

SMILES

O=C1N=C2C=CC=CN2C13CC4=C(C=CC=C4)C3

Shipping

Room temperature in continental US; may vary elsewhere.

Storage
Powder -20°C 3 years
4°C 2 years
In solvent -80°C 2 years
-20°C 1 year
Solvent & Solubility
In Vitro: 

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)

Preparing
Stock Solutions
Concentration Solvent Mass 1 mg 5 mg 10 mg
1 mM 4.2324 mL 21.1622 mL 42.3245 mL
5 mM 0.8465 mL 4.2324 mL 8.4649 mL
View the 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.

  • Molarity Calculator

  • Dilution Calculator

Mass (g) = Concentration (mol/L) × Volume (L) × Molecular Weight (g/mol)

Mass
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Volume
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Molecular Weight *

Concentration (start) × Volume (start) = Concentration (final) × Volume (final)

This equation is commonly abbreviated as: C1V1 = C2V2

Concentration (start)

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In Vivo:

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.

  • Protocol 1

    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.
  • Protocol 2

    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.
In Vivo Dissolution Calculator
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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%
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Recommended: Keep the proportion of DMSO in working solution below 2% if your animal is weak.
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).
Calculation results:
Working solution concentration: mg/mL
Method for preparing stock solution: mg drug dissolved in μL  DMSO (Stock solution concentration: mg/mL).
The concentration of the stock solution you require exceeds the measured solubility. The following solution is for reference only. If necessary, please contact MedChemExpress (MCE).
Method for preparing in vivo working solution for animal experiments: Take μL DMSO stock solution, add μL . μL , mix evenly, next add μL Tween 80, mix evenly, then add μL Saline.
 If the continuous dosing period exceeds half a month, please choose this protocol carefully.
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.
Purity & Documentation
References
Animal Administration
[2]

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.

MCE has not independently confirmed the accuracy of these methods. They are for reference only.

References

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 21.1622 mL 42.3245 mL 105.8111 mL
5 mM 0.8465 mL 4.2324 mL 8.4649 mL 21.1622 mL
10 mM 0.4232 mL 2.1162 mL 4.2324 mL 10.5811 mL
15 mM 0.2822 mL 1.4108 mL 2.8216 mL 7.0541 mL
20 mM 0.2116 mL 1.0581 mL 2.1162 mL 5.2906 mL
25 mM 0.1693 mL 0.8465 mL 1.6930 mL 4.2324 mL
30 mM 0.1411 mL 0.7054 mL 1.4108 mL 3.5270 mL
40 mM 0.1058 mL 0.5291 mL 1.0581 mL 2.6453 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 0.5291 mL 1.3226 mL
100 mM 0.0423 mL 0.2116 mL 0.4232 mL 1.0581 mL
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  • Do most proteins show cross-species activity?

    Species cross-reactivity must be investigated individually for each product. Many human cytokines will produce a nice response in mouse cell lines, and many mouse proteins will show activity on human cells. Other proteins may have a lower specific activity when used in the opposite species.

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ZSET1446
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