IC-87201

本公司产品仅用于科研实验，不得用于人体或动物的临床与诊断

PSD-95/nNOS 相互作用的小分子抑制剂，IC50 为 31 uM。

A small molecule inhibitor of PSD-95/nNOS interaction with IC50 of 31 uM, without inhibiting nNOS catalytic activity; dose-dependently blocks NMDA-induced increase in cGMP production in hippocampal cultures with IC50 of 2.7 uM; inhibits NMDA-induced thermal hyperalgesia in mice with no effect on acute pain thresholds or motor coordination, also reverses mechanical allodynia induced by chronic constriction of the sciatic nerve.(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. 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 IC50 of 2.7 μM. IC87201 increases the number of branches at 10-30 μM when compared to control-treated neurons.(In Vivo):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).

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 IC50 of 2.7 μM. IC87201 increases the number of branches at 10-30 μM when compared to control-treated neurons.

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).

IC87201 | IC 87201

Immunology/Inflammation

NOS

NOS

Neurological Disease

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866927-10-8

309.1507

C13H10Cl2N4O

>98% (HPLC)

DMSO: ≥ 28 mg/mL

OC1=C(Cl)C=C(Cl)C=C1CNC2=CC=C(NN=N3)C3=C2

Phenol, 2-[(1H-benzotriazol-6-ylamino)methyl]-4,6-dichloro-

(-20℃)

With Ice Pack

≥ 2 years