[4,4'-Bipyrimidin]-6(1H)-one, 2-[(2S)-2-(4-fluorophenyl)-4-morpholinyl]-1-methyl- manufacturers
- SAR502250
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- $1970.00
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2026-07-27
- CAS:503860-57-9
- Purity:
- Supply Ability: 10g
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| | [4,4'-Bipyrimidin]-6(1H)-one, 2-[(2S)-2-(4-fluorophenyl)-4-morpholinyl]-1-methyl- Basic information |
| | [4,4'-Bipyrimidin]-6(1H)-one, 2-[(2S)-2-(4-fluorophenyl)-4-morpholinyl]-1-methyl- Chemical Properties |
| Boiling point | 547.2±60.0 °C(Predicted) | | density | 1.38±0.1 g/cm3(Predicted) | | storage temp. | Store at -20°C | | solubility | DMSO : 100 mg/mL (272.20 mM; Need ultrasonic) | | pka | 2.90±0.19(Predicted) | | form | Solid | | color | White to off-white |
| | [4,4'-Bipyrimidin]-6(1H)-one, 2-[(2S)-2-(4-fluorophenyl)-4-morpholinyl]-1-methyl- Usage And Synthesis |
| Uses | 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]. | | 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[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 (10-30mg/kg; a single p.o.) significantly increases the percentage of lever-presses in the inter-response time (IRT) bin (49-96s), with a significant augmentation of the percentage of reinforced responses[2].
SAR502250 (30mg/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]. | Animal Model: | Female P301L human tau transgenic mice (three-month-old; 32 g)[2] | | 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 ED50s of 12.5 and 11.5mg/kg, respectively. |
| | IC 50 | hGSK-3β: 12 nM (IC50) | | References | [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. DOI:10.1016/j.bmcl.2013.09.020 [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. DOI:10.1038/s41598-019-54557-5 |
| | [4,4'-Bipyrimidin]-6(1H)-one, 2-[(2S)-2-(4-fluorophenyl)-4-morpholinyl]-1-methyl- Preparation Products And Raw materials |
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