SAR502250 是一种有效的，选择性的，ATP竞争性，具有口服活性和可透过血脑屏障的 GSK3 抑制剂，对人 GSK-3β 的 IC₅₀ 值为 12 nM。SAR502250 显示出抗抑郁样活性。SAR502250 可用于研究阿尔茨海默症 (AD)。

SAR502250 is a potent, selective, ATP competitive, orally active and brain-penetrant inhibitor of GSK3, with an IC 50 of 12 nM for human GSK-3β. SAR502250 displays antidepressant-like activity. SAR502250 can be used for the research of Alzheimer’s disease (AD).

Solid

hGSK-3β 12 nM (IC50)

SAR502250 (0.01-1 μM; 36 h) attenuates the Aβ25-35-induced cell death in rat embryonic hippocampal neurons.
has not independently confirmed the accuracy of these methods. They are for reference only.

SAR502250 (1-100 mg/kg; a single p.o,) attenuates tau hyperphosphorylation in the cortex and spinal cord of transgenic mice expressing P301L tau.
SAR502250 (10-30 mg/kg; p.o. once daily for 7 weeks) improves the cognitive deficit in transgenic APP(SW)/Tau(VLW) mice after infusion of Aβ 25-35 .
SAR502250 (10-30?mg/kg; a single p.o.) significantly increases the percentage of lever-presses in the inter-response time (IRT) bin (49-96?s), with a significant augmentation of the percentage of reinforced responses.
SAR502250 (30?mg/kg; i.p. once daily for 28 d) ameliorates chronic stress-induced degradation of the physical state of the mice coat.
SAR502250 (10-60 mg/kg; a single p.o.) decreases hyperactivity produced by psychostimulantsin mice.

Room temperature in continental US; may vary elsewhere.

Powder -20°C 3 years；4°C 2 years

[1]. Fukunaga K, et, al. 2-(2-Phenylmorpholin-4-yl)pyrimidin-4(3H)-ones; a new class of potent, selective and orally active glycogen synthase kinase-3β inhibitors. Bioorg Med Chem Lett. 2013 Dec 15;23(24):6933-7.
[2]. Griebel G, et, al. The selective GSK3 inhibitor, SAR502250, displays neuroprotective activity and attenuates behavioral impairments in models of neuropsychiatric symptoms of Alzheimers disease in rodents. Sci Rep. 2019 Dec 2;9(1):18045.

In Vitro: DMSO : 100 mg/mL (272.20 mM; Need ultrasonic)配制储备液