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Activity Type | Activity Value -log(M) | Mechanism of Action | Activity Reference | Publications (PubMed IDs) |
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SKU | Size | Availability | Price | Qty |
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S655450-1ml | 1ml | Available within 8-12 weeks(?) Production requires sourcing of materials. We appreciate your patience and understanding. | $638.90 |
Specifications & Purity | 10mM in DMSO |
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Storage Temp | Store at -80°C |
Shipped In | Ice chest + Ice pads |
Product Description | 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 ) |
Activity Type | Activity Value -log(M) | Mechanism of Action | Activity Reference | Publications (PubMed IDs) |
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Canonical SMILES | CN1C(=O)C=C(N=C1N2CCOC(C2)C3=CC=C(C=C3)F)C4=NC=NC=C4 |
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Molecular Weight | 367.38 |
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