中文名 | IC87201 |
英文名 | IC87201 |
别名 | 化合物IC87201 2-(((1H-苯并[D][1,2,3]三唑-6-基)氨基)甲基)-4,6-二氯苯酚 |
英文别名 | IC87201 IC-87201(IC87201 2-[(1H-Benzotriazol-6-ylamino)methyl]-4,6-dichlorophenol Phenol, 2-[(1H-benzotriazol-6-ylamino)methyl]-4,6-dichloro- 2-(((1H-Benzo[d][1,2,3]triazol-6-yl)amino)methyl)-4,6-dichlorophenol |
CAS | 866927-10-8 |
化学式 | C13H10Cl2N4O |
分子量 | 309.15 |
溶解度 | DMSO: ≥ 28 mg/mL |
存储条件 | -20℃ |
体外研究 | 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. |
体内研究 | 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 |
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