866927-10-8
866927-10-8 structure
- Name: IC 87201
- Chemical Name: IC87201
- CAS Number: 866927-10-8
- Molecular Formula: C13H10Cl2N4O
- Molecular Weight: 309.151
- Catalog: Signaling Pathways Membrane Transporter/Ion Channel iGluR
- Create Date: 2018-06-25 10:41:54
- Modify Date: 2025-08-27 10:32:11
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IC87201, an inhibitor of PSD95-nNOS protein-protein interactions, suppresses NMDAR-dependent NO and cGMP formation.
| Name | IC87201 |
|---|---|
| Synonyms |
Phenol, 2-[(2H-1,2,3-benzotriazol-5-ylamino)methyl]-4,6-dichloro-
2-[(2H-Benzotriazol-5-ylamino)methyl]-4,6-dichlorophenol |
| Description | IC87201, an inhibitor of PSD95-nNOS protein-protein interactions, suppresses NMDAR-dependent NO and cGMP formation. |
|---|---|
| Related Catalog | |
| In Vitro | 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]. |
| In Vivo | IC87201 (1, 4 and 10 mg/kg, i.p.) does not produce impairment in either spatial working memory or source memory[2]. IC87201 (1 mg/kg) is effective in treating NMDA-induced thermal hyperalgesia in mice, with a corresponding peak plasma level of 55 ng/mL (or 0.2 μM)[3]. |
| Animal Admin | 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]. |
| References |
| Density | 1.6±0.1 g/cm3 |
|---|---|
| Boiling Point | 525.0±60.0 °C at 760 mmHg |
| Molecular Formula | C13H10Cl2N4O |
| Molecular Weight | 309.151 |
| Flash Point | 271.3±32.9 °C |
| Exact Mass | 308.023163 |
| LogP | 2.83 |
| Vapour Pressure | 0.0±1.4 mmHg at 25°C |
| Index of Refraction | 1.786 |