Molecular Formula | C13H10Cl2N4O |
Molar Mass | 309.15 |
Solubility | DMSO: ≥ 28 mg/mL |
Storage Condition | -20℃ |
In vitro study | 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. IC87201 (20 μM) suppresses NMDA-stimulated cGMP formation relative to vehicle, in cultured hippocampal neurons. 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 IC 50 of 2.7 μM. IC87201 increases the number of branches at 10-30 μM when compared to control-treated neurons. |
In vivo study | IC87201 (1, 4 and 10 mg/kg, i.p.) does not produce impairment in either spatial working memory or source memory. 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). |
1mg | 5mg | 10mg | |
---|---|---|---|
1 mM | 3.235 ml | 16.173 ml | 32.347 ml |
5 mM | 0.647 ml | 3.235 ml | 6.469 ml |
10 mM | 0.323 ml | 1.617 ml | 3.235 ml |
5 mM | 0.065 ml | 0.323 ml | 0.647 ml |
biological activity | IC87201 is a PSD95-nNOS interacting inhibitor that inhibits nMDAR-induced formation of nitric oxide and cGMP. |