1. Membrane Transporter/Ion Channel Neuronal Signaling
  2. iGluR
  3. ZL006

ZL006 is a potent inhibitor of nNOS/PSD-95 interaction, and inhibits NMDA receptor-mediated NO synthesis.

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ZL006 Chemical Structure

ZL006 Chemical Structure

CAS No. : 1181226-02-7

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10 mM * 1 mL in DMSO
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Based on 1 publication(s) in Google Scholar

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  • Purity & Documentation

  • References

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Description

ZL006 is a potent inhibitor of nNOS/PSD-95 interaction, and inhibits NMDA receptor-mediated NO synthesis.

IC50 & Target

NMDA Receptor

 

In Vitro

ZL006 presents little cytotoxicity, and a growth inhibition of BCECs is not found at low concentration of 0.001, 0.01, 0.1, 1 and 10 μg/mL. The cytotoxicity of T7-P-LPs/ZL006 is significantly enhanced at the concentration of 10 μg/mL. Cellular uptake of ZL006 loads P-LPs and T7-P-LPs after incubation for 0.5 h at the concentrations range from 100 μg/mL to 600 μg/mL in BCECs[1]. ZL006 does not inhibit the nNOS-PDZ/PSD-95-PDZ interaction, or perturb the nNOS β-finger[2].

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

In Vivo

Compared with P-LPs/ZL006 and free ZL006, T7-P-LPs/ZL006 exhibits a significant increase of drug accumulation in the brain tissue due to its better brain targeting delivery. Compared with free ZL006, P-LPs/ZL006 and T7-P-LPs/ZL006 exhibit a significant decrease of drug accumulation in the liver and kidney[1].

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

Molecular Weight

328.15

Formula

C14H11Cl2NO4

CAS No.
Appearance

Solid

Color

Light yellow to khaki

SMILES

O=C(O)C1=CC=C(NCC2=CC(Cl)=CC(Cl)=C2O)C=C1O

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 : 25 mg/mL (76.18 mM; Need ultrasonic; Hygroscopic DMSO has a significant impact on the solubility of product, please use newly opened DMSO)

H2O : < 0.1 mg/mL (insoluble)

Preparing
Stock Solutions
Concentration Solvent Mass 1 mg 5 mg 10 mg
1 mM 3.0474 mL 15.2369 mL 30.4739 mL
5 mM 0.6095 mL 3.0474 mL 6.0948 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
=
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 (7.62 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 (7.62 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:

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).
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
Cell Assay
[1]

BCECs are seeded in 96-well plates in 200 μL of DMEM medium to obtain a concentration of 2000 cells per well, and incubated for 24 h. The medium in each well is then incubated for 72 h with 200 μL medium containing blank vehicle, P-LPs/ZL006, T7-P-LPs/ZL006 and ZL006 (free drug dissolved in DMSO) with a series of concentrations ranging from 0.001 to 100 μg/mL. The MTT absorbance at 570 nm of each well is measured by a microplate reader.

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

Animal Administration
[1]

ICR mice weighting 20 ± 2 g are divided into three groups at random (n=12). Free ZL006, P-LPs/ZL006 and T7-P-LPs/ZL006 (all containing ZL006 4 mg/kg) are administered to each group through intravenous route, respectively. At designated time intervals (0.5, 1 and 2 h), the mice are executed and the major organs samples including brain, heart, liver, spleen, lung and kidney are collected. Before pretreatment, these tissues are rinsed with cold saline solution to remove the blood and then blotted with paper towel. Protein precipitation of the samples is performed before analysis. Then the samples are injected into the LC-MS/MS systems for analysis. The LC-MS/MS system consists of an Agilent Series 1200 HPLC system and a 6410 Triple Quad LC/MS mass spectrometer. The data is collected and processed using the Agilent MassHunter Workstation Software.

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 3.0474 mL 15.2369 mL 30.4739 mL 76.1847 mL
5 mM 0.6095 mL 3.0474 mL 6.0948 mL 15.2369 mL
10 mM 0.3047 mL 1.5237 mL 3.0474 mL 7.6185 mL
15 mM 0.2032 mL 1.0158 mL 2.0316 mL 5.0790 mL
20 mM 0.1524 mL 0.7618 mL 1.5237 mL 3.8092 mL
25 mM 0.1219 mL 0.6095 mL 1.2190 mL 3.0474 mL
30 mM 0.1016 mL 0.5079 mL 1.0158 mL 2.5395 mL
40 mM 0.0762 mL 0.3809 mL 0.7618 mL 1.9046 mL
50 mM 0.0609 mL 0.3047 mL 0.6095 mL 1.5237 mL
60 mM 0.0508 mL 0.2539 mL 0.5079 mL 1.2697 mL
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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.

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Product Name:
ZL006
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HY-100456
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