2. Membrane Transporter/Ion Channel Neuronal Signaling
  3. iGluR
  4. Zonampanel

Zonampanel (YM 872) is a selective antagonist of the glutamate receptor subtype, α-amino-3-hydroxy-5-methylisoxazole-4-propionic acid (AMPA) receptor.

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Zonampanel Chemical Structure

Zonampanel Chemical Structure

CAS No. : 210245-80-0

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1 mg USD 200 In-stock
5 mg USD 500 In-stock
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Zonampanel Related Antibodies

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  • Biological Activity

  • Protocol

  • Purity & Documentation

  • References

  • Customer Review

Description

Zonampanel (YM 872) is a selective antagonist of the glutamate receptor subtype, α-amino-3-hydroxy-5-methylisoxazole-4-propionic acid (AMPA) receptor.

In Vitro

Zonampanel inhibits the human MRP4-mediated transport of [3H]oestradiol 17-D-glucuronide in a concentration-dependent manner. In contrast, Zonampanel (up to 1000 mM) does not inhibit the human MRP2- or BCRP-mediated transport of [3H]oestradiol 17-D-glucuronide or [3H]methotrexate[1]. Zonampanel inhibits the uptake of typical substrates by Oat1, Oat2, and Oat3 with inhibition constant (Ki) values of 7.02 to 10.4 μM. A time- and saturable concentration-dependent increase in [14C]Zonampanel uptake is observed in these cells [Km values: 13.4 to 53.6 μM][2].

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

Zonampanel Related Antibodies
In Vivo

In in vivo experiments, probenecid and cimetidine decrease intrinsic clearance for both the renal secretion and biliary excretion of Zonampanel[2].

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

331.24

Formula

C13H9N5O6
CAS No.
Appearance

Solid

Color

Yellow to brown

SMILES

O=C(N1CC(O)=O)C(NC(C1=C2)=CC([N+]([O-])=O)=C2N3C=CN=C3)=O
Shipping

Room temperature in continental US; may vary elsewhere.
Storage

4°C, sealed storage, away from moisture and light

*In solvent : -80°C, 6 months; -20°C, 1 month (sealed storage, away from moisture and light)

Solvent & Solubility
In Vitro: 

DMSO : 50 mg/mL (150.95 mM; ultrasonic and warming and heat to 60°C; 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 3.0190 mL 15.0948 mL 30.1896 mL
5 mM 0.6038 mL 3.0190 mL 6.0379 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, 6 months; -20°C, 1 month (sealed storage, away from moisture and light). When stored at -80°C, please use it within 6 months. When stored at -20°C, please use it within 1 month.

  • Molarity Calculator

  • Dilution Calculator

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

Mass
=
Concentration
×
Volume
×
Molecular Weight *

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

This equation is commonly abbreviated as: C1V1 = C2V2

Concentration (start)

C1

×
Volume (start)

V1

=
Concentration (final)

C2

×
Volume (final)

V2

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 (7.55 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 (7.55 mM); Suspended solution; Need ultrasonic

    This protocol yields a suspended solution of 2.5 mg/mL. Suspended solution can be used for oral and intraperitoneal injection.

    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:

Dosage

mg/kg

Animal weight
(per animal)

g

Dosing volume
(per animal)

μL

Number of animals

Recommended: Prepare an additional quantity of animals to account for potential losses during experiments.
Please enter your animal formula composition:
%
DMSO +
% 
+
%
Tween-80 +
%
Saline
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).

*In solvent : -80°C, 6 months; -20°C, 1 month (sealed storage, away from moisture and light)

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]

Seven-week-old male Sprague-Dawley rats are used at 8 weeks after acclimatization for at least 1 week. During acclimatization, the rats are kept in an air-conditioned room with temperature and humidity controlled at 22.9 to 23.3°C and 50 to 78%; the room is lit for 12 h 30 min from 7:30 AM to 8:00 PM. Rats are given free access to solid food and water until just before drug administration. YM 872 (15 mg/kg) is administered at a single bolus dose into the rat tail vein with or without probenecid (50 mg/kg) or cimetidine (40 mg/kg). At 5, 15, and 30 min and 1, 2, 3, 4, and 6 h after dosing, blood is sampled under ether anesthesia via the inferior vena cava using a heparinized syringe and immediately stored on ice using four rats each per sampling time point per administration group (total of 128 rats for 8 sampling time points and 4 administration groups). Plasma is obtained by centrifugation at 4°C, 1870 g for 15 min and kept frozen at -20°C. Rats for plasma sampling at 3 and 6 h after administration are housed in metabolic cages after administration, spontaneously excreted urine is collected, and the cages are washed using water. Regarding specific gravity as 1, urine volume (including the cage-wash water) is calculated according to differences in the weight of the sampling tube before and after sampling. Urine samples are kept frozen at -20°C until assay as described below. All plasma and urine samples are protected from light throughout the sampling, storage, and assay procedures.

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, 6 months; -20°C, 1 month (sealed storage, away from moisture and light). When stored at -80°C, please use it within 6 months. When stored at -20°C, please use it within 1 month.

Optional Solvent Concentration Solvent Mass 1 mg 5 mg 10 mg 25 mg
DMSO 1 mM 3.0190 mL 15.0948 mL 30.1896 mL 75.4740 mL
5 mM 0.6038 mL 3.0190 mL 6.0379 mL 15.0948 mL
10 mM 0.3019 mL 1.5095 mL 3.0190 mL 7.5474 mL
15 mM 0.2013 mL 1.0063 mL 2.0126 mL 5.0316 mL
20 mM 0.1509 mL 0.7547 mL 1.5095 mL 3.7737 mL
25 mM 0.1208 mL 0.6038 mL 1.2076 mL 3.0190 mL
30 mM 0.1006 mL 0.5032 mL 1.0063 mL 2.5158 mL
40 mM 0.0755 mL 0.3774 mL 0.7547 mL 1.8868 mL
50 mM 0.0604 mL 0.3019 mL 0.6038 mL 1.5095 mL
60 mM 0.0503 mL 0.2516 mL 0.5032 mL 1.2579 mL
80 mM 0.0377 mL 0.1887 mL 0.3774 mL 0.9434 mL
100 mM 0.0302 mL 0.1509 mL 0.3019 mL 0.7547 mL
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Zonampanel Related Classifications

Help & FAQs
  • 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.

Keywords:

Zonampanel210245-80-0YM 872YM872YM-872iGluRIonotropic glutamate receptorsInhibitorinhibitorinhibit

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