ChemicalBook CAS DataBase List 503860-57-9

503860-57-9

Name	[4,4'-Bipyrimidin]-6(1H)-one, 2-[(2S)-2-(4-fluorophenyl)-4-morpholinyl]-1-methyl-
CAS	503860-57-9
Molecular Formula	C19 H18 F N5 O2
MDL Number	MFCD33023233
Molecular Weight	367.38
MOL File	503860-57-9.mol

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)
form	Solid
pka	2.90±0.19(Predicted)
color	White to off-white

Hazard Information

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 Aβ_25-35^[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].

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 11.5?mg/kg, respectively.

IC 50

hGSK-3β: 12 nM (IC₅₀)

storage

Store at -20°C

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

Supplier

Send Inquriy