IC87201
Based on 2 publication(s) in Google Scholar
IC87201, an inhibitor of PSD95-nNOS protein-protein interactions, suppresses NMDAR-dependent NO and cGMP formation.
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- Pureza: 97.24%
- No. CAS: 866927-10-8
- Fòrmula: C13H10Cl2N4O
- Peso molecular:309.15
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Almacenamiento:Powder -20°C, 3 years , 4°C, 2 years ; In solvent -80°C, 2 years , -20°C, 1 year
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Actividad biológica
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Chemical Information
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Solvente y solubilidad
- Protocolo
- Pureza y Documentación
- Referencias
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Publications Citing Use of MedChemExpress (MCE) IC87201
MoreVer todos los productos específicos de isoformas iGluR
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Actividad biológica
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NMDA Receptor |
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Cell Line
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Type | Value | Description | References |
|---|---|---|---|---|
| Hippocampal neurone | IC50 |
2.7 μM
Compound: 46; IC87201
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Neuroprotective activity in rat hippocampal neuron cells assessed as NMDA-induced cGMP production
Neuroprotective activity in rat hippocampal neuron cells assessed as NMDA-induced cGMP production
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[PMID: 37931330] |
IC87201 (500-1800 μM) does not inhibit any of the probe-PDZ interactions involving PDZ1, PDZ2, PDZ3 of PSD-95 or nNOS-PDZ, or bind the canonical PDZ ligand binding sites. IC87201 binds to the β-finger of nNOS-PDZ and allosterically inhibits the nNOS-PDZ/PSD-95-PDZ interactions. IC87201 shows high degree of fluorescence-based artefactual signal when using TAMRA-nNOS as probe[1]. IC87201 (20 μM) suppresses NMDA-stimulated cGMP formation relative to vehicle, in cultured hippocampal neurons[2]. IC87201 (10 and 100 nM) attenuats NMDA/glycine-induced decreases in neurite outgrowth. IC87201 dose-dependently reduces NMDA-induced cGMP production in primary hippocampal neurons (DIV 14-21) with an IC50 of 2.7 μM. IC87201 increases the number of branches at 10-30 μM when compared to control-treated neurons[3].
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.
Chemical Information
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No. CAS 866927-10-8
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Appearance Solid
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Peso molecular 309.15
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Fòrmula C13H10Cl2N4O
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Color Pink to red
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SMILES
OC1=C(Cl)C=C(Cl)C=C1CNC2=CC=C3N=NNC3=C2
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Envío
Room temperature in continental US; may vary elsewhere.
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Almacenamiento
Powder -20°C 3 years 4°C 2 years In solvent -80°C 2 years -20°C 1 year
Publications (2)
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Journal Impact Factor
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Most Recent
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Neurochem Int
Downregulation of Preso protects against ischemic/reperfusion-mediated neuronal injury through regulating PSD95-nNOS/YAP pathways. [Abstract]2023 Oct:169:105586. PMID: 37442439 -
Neurosci Lett
nNOS-PSD95 interactions activate the PKC-ε isoform leading to increased GluN1 phosphorylation and the development of neuropathic mechanical allodynia in mice. [Abstract]2019 Jun 11:703:156-161. PMID: 30926374
Solvente y solubilidad
DMSO : ≥ 100 mg/mL (323.47 mM; Hygroscopic DMSO has a significant impact on the solubility of product, please use newly opened DMSO)
* "≥" means soluble, but saturation unknown.
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 (8.09 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 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 (8.09 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.
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.
Protocolo
MK-801 is dissolved in saline and administered intraperitoneally (i.p.) in a within subjects dosing paradigm in order of increasing dose (0.1, 0.2, and 0.3 mg/kg). IC87201 (1, 4 and 10 mg/kg) and ZL006 (10 mg/kg) are dissolved in a vehicle containing 3% DMSO with the remaining 97% comprised of 1:1:18 of emulphor:ethanol:0.9% NaCl. Active compounds are compared with equivalent volumes of the appropriate vehicle in each case. MK-801, IC87201, and ZL006 are administered 30 min prior to behavioral testing. All drugs are administered intraperitoneally (i.p.) in a volume of 1 mL/kg[2].
MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.
Pureza y Documentación
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Ficha de datos (276 KB)
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SDS (393 KB)
- English - EN (393 KB)
- Français - FR (393 KB)
- Deutsch - DE (393 KB)
- Norwegian - NO (393 KB)
- Español - ES (393 KB)
- Swedish - SV (393 KB)
- Italian - IT (393 KB)
- Korean - KR (393 KB)
- Portuguese - PT (393 KB)
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Instrucciones de manejo (2659 KB)
Referencias
[1]. Bach A, et al. Biochemical investigations of the mechanism of action of small molecules ZL006 and IC87201 as potential inhibitors of the nNOS-PDZ/PSD-95-PDZ interactions. Sci Rep. 2015 Jul 16;5:12157. [Content Brief]
[2]. Smith AE, et al. Source memory in rats is impaired by an NMDA receptor antagonist but not by PSD95-nNOS protein-protein interaction inhibitors. Behav Brain Res. 2016 May 15;305:23-9. [Content Brief]
[3]. Doucet MV, et al. Small-molecule inhibitors at the PSD-95/nNOS interface protect against glutamate-induced neuronal atrophy in primary cortical neurons. Neuroscience. 2015 Aug 20;301:421-38. [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 | 3.2347 mL | 16.1734 mL | 32.3468 mL | 80.8669 mL |
| 5 mM | 0.6469 mL | 3.2347 mL | 6.4694 mL | 16.1734 mL | |
| 10 mM | 0.3235 mL | 1.6173 mL | 3.2347 mL | 8.0867 mL | |
| 15 mM | 0.2156 mL | 1.0782 mL | 2.1565 mL | 5.3911 mL | |
| 20 mM | 0.1617 mL | 0.8087 mL | 1.6173 mL | 4.0433 mL | |
| 25 mM | 0.1294 mL | 0.6469 mL | 1.2939 mL | 3.2347 mL | |
| 30 mM | 0.1078 mL | 0.5391 mL | 1.0782 mL | 2.6956 mL | |
| 40 mM | 0.0809 mL | 0.4043 mL | 0.8087 mL | 2.0217 mL | |
| 50 mM | 0.0647 mL | 0.3235 mL | 0.6469 mL | 1.6173 mL | |
| 60 mM | 0.0539 mL | 0.2696 mL | 0.5391 mL | 1.3478 mL | |
| 80 mM | 0.0404 mL | 0.2022 mL | 0.4043 mL | 1.0108 mL | |
| 100 mM | 0.0323 mL | 0.1617 mL | 0.3235 mL | 0.8087 mL |
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