IC87201

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Chemical Structure| 866927-10-8 同义名 : -
CAS号 : 866927-10-8
货号 : A880304
分子式 : C13H10Cl2N4O
纯度 : 99%+
分子量 : 309.15
MDL号 : MFCD28160570
存储条件:

Pure form Sealed in dry, 2-8°C

In solvent -20°C:3-6个月-80°C:12个月

溶解度 : -
动物实验配方:
生物活性
描述 IC87201, at concentrations ranging from 500 to 1800 μM, does not block the interactions between the PDZ domains (PDZ1, PDZ2, PDZ3) of PSD-95 and nNOS-PDZ, nor does it attach to the standard PDZ ligand-binding sites. Instead, IC87201 targets the β-finger of nNOS-PDZ, resulting in an allosteric inhibition of the nNOS-PDZ/PSD-95-PDZ interaction. Additionally, when TAMRA-nNOS is used as a probe, IC87201 generates a significant fluorescence-based artefactual signal[1]. IC87201, at a concentration of 20 μM, inhibits the formation of cGMP that is stimulated by NMDA compared to the control, in neurons cultured from the hippocampus[2]. IC87201, at concentrations of 10 and 100 nM, mitigates the reduction in neurite outgrowth induced by NMDA/glycine. It also decreases NMDA-stimulated cGMP production in primary hippocampal neurons (DIV 14-21) in a dose-dependent manner, with an IC50 value of (2.7 \mu M). Furthermore, IC87201 enhances branching in these neurons at concentrations of 10-30 μM compared to neurons treated with the control[3].
实验方案
1mg 5mg 10mg

1 mM

5 mM

10 mM

3.23mL

0.65mL

0.32mL

16.17mL

3.23mL

1.62mL

32.35mL

6.47mL

3.23mL

参考文献

[1]Lee WH, Xu Z, et al. Small molecule inhibitors of PSD95-nNOS protein-protein interactions as novel analgesics. Neuropharmacology. 2015 Oct;97:464-75.

[2]Doucet MV, Levine H, et al. Small-molecule inhibitors at the PSD-95/nNOS interface have antidepressant-like properties in mice. Neuropsychopharmacology. 2013 Jul;38(8):1575-84.