SAR502250

小分子

SAR502250

S655450-1ml

1ml

10mM in DMSO

-80℃储存

超低温冰袋运输

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) In Vitro SAR502250 (0.01-1 μM; 36 h) attenuates the Aβ 25-35 -induced cell death in rat embryonic hippocampal neurons. MCE has not independently confirmed the accuracy of these methods. They are for reference only. In Vivo 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. MCE has not independently confirmed the accuracy of these methods. They are for reference only. Animal Model: Female P301L human tau transgenic mice (three-month-old; 32 g)Dosage: 1, 3, 10, 30, 100 mg/kg Administration: A single p.o. Result: Attenuated dose-dependently tau phosphorylation in the cortex and spinal cord, with ED 50 s of 12.5 and 11.5 mg/kg, respectively. IC50& Target:hGSK-3β 12 nM (IC 50 )

SAR502250 是一种强效、选择性、ATP 竞争性、口服活性和脑穿透性 GSK3 抑制剂，对人 GSK-3β 的 IC 50 为 12 nM。SAR502250 具有类似抗抑郁剂的活性。SAR502250 可用于阿尔茨海默病的研究。

503860-57-9(DMSO)

C19H18FN5O2

367.38 g/mol

CN1C(=O)C=C(N=C1N2CCOC(C2)C3=CC=C(C=C3)F)C4=NC=NC=C4