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).

Product information

CAS Number: 503860-57-9

Molecular Weight: 367.38

Formula: C19H18FN5O2

Chemical Name: 2-[(2S)-2-(4-fluorophenyl)morpholin-4-yl]-1-methyl-1,6-dihydro-[4,4'-bipyrimidin]-6-one

Smiles: CN1C(=NC(=CC1=O)C1=CC=NC=N1)N1CCO[C@H](C1)C1C=CC(F)=CC=1

InChiKey: NKUNFNVAHJNALA-QGZVFWFLSA-N

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

Technical Data

Appearance: Solid Power

Purity: ≥98% (or refer to the Certificate of Analysis)

Solubility: DMSO : 100 mg/mL (272.20 mM; Need ultrasonic).

Shipping Condition: Shipped under ambient temperature as non-hazardous chemical or refer to Certificate of Analysis

Storage Condition: Dry, dark and -20 ^oC for 1 year or refer to the Certificate of Analysis.

Shelf Life: ≥12 months if stored properly.

Stock Solution Storage: 0 - 4 ^oC for 1 month or refer to the Certificate of Analysis.

Drug Formulation: To be determined

HS Tariff Code: 382200

How to use

In Vitro:

SAR502250 (0.01-1 μM; 36 h) attenuates the Aβ25-35-induced cell death in rat embryonic hippocampal neurons.

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 Aβ25-35. 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.

Products are for research use only. Not for human use.