For research use only. Not for therapeutic Use.
SAR502250 is a potent, selective, ATP competitive, orally active and brain-penetrant inhibitor of GSK3, with an IC50 of 12 nM for human GSK-3β. SAR502250 displays antidepressant-like activity. SAR502250 can be used for the research of Alzheimer’s disease (AD)[1][2].
SAR502250 (0.01-1 μM; 36 h) attenuates the Aβ25-35-induced cell death in rat embryonic hippocampal neurons[2].
SAR502250 (1-100 mg/kg; a single p.o,) attenuates tau hyperphosphorylation in the cortex and spinal cord of transgenic mice expressing P301L tau[2].
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 Aβ25-35[2].
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[2].
SAR502250 (30 mg/kg; i.p. once daily for 28 d) ameliorates chronic stress-induced degradation of the physical state of the mice coat[2].
SAR502250 (10-60 mg/kg; a single p.o.) decreases hyperactivity produced by psychostimulantsin mice[2].
| Catalog Number | I044667 |
| CAS Number | 503860-57-9 |
| Synonyms | 2-[(2S)-2-(4-fluorophenyl)morpholin-4-yl]-3-methyl-6-pyrimidin-4-ylpyrimidin-4-one |
| Molecular Formula | C19H18FN5O2 |
| Purity | ≥95% |
| InChI | InChI=1S/C19H18FN5O2/c1-24-18(26)10-16(15-6-7-21-12-22-15)23-19(24)25-8-9-27-17(11-25)13-2-4-14(20)5-3-13/h2-7,10,12,17H,8-9,11H2,1H3/t17-/m1/s1 |
| InChIKey | NKUNFNVAHJNALA-QGZVFWFLSA-N |
| SMILES | CN1C(=O)C=C(N=C1N2CCOC(C2)C3=CC=C(C=C3)F)C4=NC=NC=C4 |
| Reference | [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 Alzheimer’s disease in rodents. Sci Rep. 2019 Dec 2;9(1):18045. |
