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Purity: ≥98%
IC87201 is an inhibitor of PSD95-nNOS protein-protein interactions. It suppresses NMDAR-dependent NO and cGMP formation. In vitro, IC87201 does not interact with the PDZ domains of nNOS or PSD-95, nor inhibit the nNOS-PDZ/PSD-95-PDZ interface by interacting with the β-finger of nNOS-PDZ. IC87201 binds to the β-finger of nNOS-PDZ and allosterically inhibits the nNOS-PDZ/PSD-95-PDZ interactions. IC87201 also shows high degree of fluorescence-based artefactual signal when using TAMRA-nNOS as probe. 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.
| ln Vitro |
IC87201 (500-1800 μM) does not bind the canonical PDZ ligand binding sites or inhibit any of the probe-PDZ interactions involving PSD-95's PDZ1, PDZ2, or PDZ3 or nNOS-PDZ. By binding to the β-finger of nNOS-PDZ, IC87201 allosterically inhibits the interactions between nNOS-PDZ and PSD-95-PDZ. When TAMRA-nNOS is used as the probe, IC87201 exhibits a high degree of fluorescence-based artefactual signal[1]. In cultured hippocampal neurons, IC87201 (20 μM) suppresses NMDA-stimulated cGMP formation in comparison to vehicle[2]. Ten and 100 nM of IC87201 attenuate decreases in neurite outgrowth caused by NMDA and glycine. With an IC50 of 2.7 μM, IC87201 dose-dependently lowers the production of cGMP induced by NMDA in primary hippocampal neurons (DIV 14-21). Compared to neurons treated with control, IC87201 causes an increase in branches at concentrations of 10–30 μM[3].
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| ln Vivo |
Neither spatial working memory nor source memory are affected by IC87201 (1, 4 and 10 mg/kg, ip)[2]. Mice with NMDA-induced thermal hyperalgesia can be effectively treated with IC87201 (1 mg/kg), which has a corresponding peak plasma level of 55 ng/mL (or 0.2 μM)[3].
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| References |
[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.
[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. [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 |
| Molecular Formula |
C₁₃H₁₀CL₂N₄O
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| Molecular Weight |
309.15
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| CAS # |
866927-10-8
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| SMILES |
OC1=C(Cl)C=C(Cl)C=C1CNC2=CC=C(NN=N3)C3=C2
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| Storage |
Powder -20°C 3 years 4°C 2 years In solvent -80°C 6 months -20°C 1 month |
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| Shipping Condition |
Room temperature (This product is stable at ambient temperature for a few days during ordinary shipping and time spent in Customs)
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| Solubility (In Vitro) |
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| Solubility (In Vivo) |
Solubility in Formulation 1: 2.5 mg/mL (8.09 mM) in 10% DMSO + 40% PEG300 + 5% Tween80 + 45% Saline (add these co-solvents sequentially from left to right, and one by one), suspension solution; with sonication.
For example, if 1 mL of working solution is to be prepared, you can add 100 μL of 25.0 mg/mL clear DMSO stock solution to 400 μL PEG300 and mix evenly; then add 50 μL Tween-80 to the above solution and mix evenly; then add 450 μL normal saline to adjust the volume to 1 mL. Preparation of saline: Dissolve 0.9 g of sodium chloride in 100 mL ddH₂ O to obtain a clear solution. Solubility in Formulation 2: 2.5 mg/mL (8.09 mM) in 10% DMSO + 90% (20% SBE-β-CD in Saline) (add these co-solvents sequentially from left to right, and one by one), suspension solution; with ultrasonication. For example, if 1 mL of working solution is to be prepared, you can add 100 μL of 25.0 mg/mL clear DMSO stock solution to 900 μL of 20% SBE-β-CD physiological saline solution and mix evenly. Preparation of 20% SBE-β-CD in Saline (4°C，1 week): Dissolve 2 g SBE-β-CD in 10 mL saline to obtain a clear solution. (Please use freshly prepared in vivo formulations for optimal results.) |
| Preparing Stock Solutions | 1 mg | 5 mg | 10 mg | |
| 1 mM | 3.2347 mL | 16.1734 mL | 32.3468 mL | |
| 5 mM | 0.6469 mL | 3.2347 mL | 6.4694 mL | |
| 10 mM | 0.3235 mL | 1.6173 mL | 3.2347 mL |
*Note: Please select an appropriate solvent for the preparation of stock solution based on your experiment needs. For most products, DMSO can be used for preparing stock solutions (e.g. 5 mM, 10 mM, or 20 mM concentration); some products with high aqueous solubility may be dissolved in water directly. Solubility information is available at the above Solubility Data section. Once the stock solution is prepared, aliquot it to routine usage volumes and store at -20°C or -80°C. Avoid repeated freeze and thaw cycles.
Calculation results
Working concentration： mg/mL；
Method for preparing DMSO stock solution： mg drug pre-dissolved in μL DMSO (stock solution concentration mg/mL). Please contact us first if the concentration exceeds the DMSO solubility of the batch of drug.
Method for preparing in vivo formulation:：Take μL DMSO stock solution, next add μL PEG300, mix and clarify, next addμL Tween 80, mix and clarify, next add μL ddH2O，mix and clarify.
(1) Please be sure that the solution is clear before the addition of next solvent. Dissolution methods like vortex, ultrasound or warming and heat may be used to aid dissolving.
(2) Be sure to add the solvent(s) in order.
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