SSR 411298

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

SSR411298 是一种高选择性、脑渗透性和口服活性的 FAAH 抑制剂，IC50 为 62.5 nM（小鼠脑 FAAH）。

SSR411298 is a highly selective, brain penetrant and orally-active inhibitor of FAAH with IC50 of 62.5 nM (mouse brain FAAH); potently increases hippocampal levels of AEA, OEA and PEA in mice, produces robust antidepressant-like activity in the rat forced-swimming test and in the mouse chronic mild stress models.Anxiety Phase 1 Clinical.

SSR411298 (0.1, 1, 10, 100, 1000, 10000 nM) inhibits mouse brain FAAH in a concentration-dependent manner.SSR411298 produces maximal inhibition of FAAH between 0.3 and 30 mg/kg in the ex-vivo experiment.

SSR411298 (0.3, 1, 3 mg/kg; p.o.; twice a day during 2 days; 60 minutes before pretest, immediately after, and 60 minutes before the second session of testing) produces robust antidepressant-like activity in the rat forced-swimming test and in the mouse chronic mild stress model, restoring notably the development of inadequate coping responses to chronic stress in male Wistar rats weighing 235-290 g. SSR411298 (0.3, 1, 3, 10 mg/kg; po; single dose; two hours prior to sacrifice) produces a significant global increase of tissular AEA, PEA and OEA levels in the hippocampus, but not of 2-AG levels.

SSR411298

Metabolic Enzyme/Protease

FAAH

FAAH

Neurological Disease

Anxiety

666860-59-9

402.447

C21H26N2O6

>98% (HPLC)

In Vitro:?DMSO : 100 mg/mL (248.48 mM)

——

2-amino-2-oxoethyl (3-((2r,5r)-5-(6-methoxynaphthalen-1-yl)-1,3-dioxan-2-yl)propyl)carbamate

(-20℃)

With Ice Pack

≥ 2 years