ZL-006

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

ZL-006 (ZL 006, ZL006) 是一种 PSD-95/nNOS 相互作用的脑渗透性小分子抑制剂，可预防谷氨酸诱导的兴奋性毒性和体内脑缺血损伤。

ZL-006 (ZL 006, ZL006) is a brain penetrant small molecule inhibitor of PSD-95/nNOS interaction that prevents glutamate-induced excitotoxicity and cerebral ischemic damage in vivo; selectively blocks the ischemia-induced nNOS-PSD-95 association, shows potent neuroprotective activity in vitro and ameliorates focal cerebral ischemic damage in mice and rats subjected to middle cerebral artery occlusion (MCAO) and reperfusio; does not inhibit NMDAR function, catalytic activity of nNOS or spatial memory, and has no effect on aggressive behaviors.

ZL006 presents little cytotoxicity, and a growth inhibition of BCECs is not found at low concentration of 0.001, 0.01, 0.1, 1 and 10 μg/mL. The cytotoxicity of T7-P-LPs/ZL006 is significantly enhanced at the concentration of 10 μg/mL. Cellular uptake of ZL006 loads P-LPs and T7-P-LPs after incubation for 0.5 h at the concentrations range from 100 μg/mL to 600 μg/mL in BCECs. ZL006 does not inhibit the nNOS-PDZ/PSD-95-PDZ interaction, or perturb the nNOS β-finger.

Compared with P-LPs/ZL006 and free ZL006, T7-P-LPs/ZL006 exhibits a significant increase of drug accumulation in the brain tissue due to its better brain targeting delivery. Compared with free ZL006, P-LPs/ZL006 and T7-P-LPs/ZL006 exhibit a significant decrease of drug accumulation in the liver and kidney.

ZL 006 | ZL006

Immunology/Inflammation

NOS

NOS

Neurological Disease

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1181226-02-7

328.1474

C14H11Cl2NO4

>98% (HPLC)

DMSO: ≥ 29 mg/mL

O=C(O)C1=CC=C(NCC2=CC(Cl)=CC(Cl)=C2O)C=C1O

Benzoic acid, 4-[[(3,5-dichloro-2-hydroxyphenyl)methyl]amino]-2-hydroxy-

(-20℃)

With Ice Pack

≥ 2 years