AZD1080

  • CAS: 612487-72-6
  • MDL:
  • Product number:QC-11776
  • Molecular formula: C19H18N4O2
  • Purity: 98.3%
  • MW: 334.37
Size Price Stock
100mg $595 in stock
250mg $895 in stock
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Brief Description

AZD1080 is a selective, orally active, brain permeable GSK3 inhibitor of GSK3α and GSK3β with Ki of 6.9 nM and 31 nM, respectively, shows >14-fold selectivity against CDK2, CDK5, CDK1 and Erk2.
IC50 Value: 6.9 nM(Ki, GSK3α); 31 nM(Ki, GSK3β)
Target: GSK3α; GSK3β
AZD1080 is a potent and selective GSK3 inhibitor that demonstrates peripheral target engagement in Phase 1 clinical studies.
in vitro: AZD1080 inhibits tau phosphorylation in cells expressing human tau and in intact rat brain. Interestingly, subchronic but not acute administration with AZD1080 reverses MK-801-induced deficits, measured by long-term potentiation in hippocampal slices and in a cognitive test in mice, suggesting that reversal of synaptic plasticity deficits in dysfunctional systems requires longer term modifications of proteins downstream of GSK3β signaling.
in vivo: AZD1080 reverses MK-801-induced impairments in mouse model of cognition. AZD1080 treatment significantly prevents MK-801-induced deficits at both time-points (*p < 0.05; **p < 0.01). Data are presented as mean _ SEM (n = 9-12 subjects/group). Clinical trial: Phase 1

Solubility

DMSO

Melting point

Boiling point

Density

Formula Weight:

Flash point

Storage conditions

Store at -20°C 2 years

Appearance:

Light yellow to yellow solid

All CEG Chemical products are intended for laboratory research use only.

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