866927-10-8

866927-10-8化学性质

储存条件 :Store at -20°C
溶解度 :DMF:30.0(Max Conc. mg/mL);97.04(Max Conc. mM)
DMSO:29.0(Max Conc. mg/mL);93.81(Max Conc. mM)
DMSO:PBS (pH 7.2) (1:3):0.25(Max Conc. mg/mL);0.81(Max Conc. mM)
Ethanol:1.0(Max Conc. mg/mL);3.23(Max Conc. mM)
形态 :A solid
颜色 :Pink to red

866927-10-8性质、用途与生产工艺

生物活性 IC87201 是 PSD95-nNOS 相互作用的抑制剂，可抑制 nMDAR 诱导的一氧化氮和 cGMP 的形成。
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).

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866927-10-8 试剂级价格

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