AZD1080

    • Catalog No.:MC0211
      • CasNo:
      • 612487-72-6
      • MolecularFormula:
      • C19H18N4O2
      • Purity:
      • >98%
      • Target:
      • GSK-3
      • IC50:
      • IC50: 6.9 nM (GSK3α), 31 nM (GSK3β)[1]pKi: 8.2 (GSK3α), 7.5 (GSK3β)[1]
      • In Vitro:
      • AZD1080 shows selectivity against cdk2 (pKi=5.9; 1150 nM; 37-fold), cdk5 (pKi=6.4; 429 nM; 14-fold), cdk1 (pKi=5.7; 1980 nM; 64-fold) and Erk2 (pKi< 5; >10 μM; >323-fold). AZD1080 (at 10 μM) is also evaluated for pan-kinase selectivity and showed good overall selectivity versus 23 kinases, as well as against 65 different receptors, enzymes and ion channels in MDS Pharma screen (< 50% effect at 10 μM AZD1080). Concentration-dependent inhibition of tau phosphorylation is observed for AZD1080 (IC50=324 nM) and the non-selective reference GSK3 inhibitor LiCl (IC50=1.5 mM) indicating that AZD1080 is several orders of magnitude more potent than LiCl[1].
      • In Vivo:
      • The pharmacokinetic analysis in blood after oral administration revealed that AZD1080 has a good oral bioavailability in rats (15-24%) with a half-life of 7.1 h, making AZD1080 attractive for further in vivo testing. The subchronic (3 days) oral treatment with AZD1080 at 4 or 15 μmol/kg significantly blocked the MK-801-induced memory deficit (AZD1080 vs. MK-801, p<0.05 at 4 μmol/kg and p<0.01 at 15 μmol/kg) in mice, raising the hypothesis that longer treatment may be required to prime the synapses to function effectively[1].
      • Fields:
      • AZD1080 is a selective, orally active, brain permeable GSK3 inhibitor, inhibits human GSK3α and GSK3β with Ki of 6.9 nM and 31 nM, respectively, shows >14-fold selectivity against CDK2, CDK5, CDK1 and Erk2. IC50: 6.9 nM (GSK3α), 31 nM (GSK3β)[1]pKi: 8.2 (GSK3α), 7.5 (GSK3β)[1]
      • Specificity:
      • Target: GSK-3. Fields: AZD1080 is a selective, orally active, brain permeable GSK3 inhibitor, inhibits human GSK3α and GSK3β with Ki of 6.9 nM and 31 nM, respectively, shows >14-fold selectivity agai
      • Source:
      • Rabbit
      • Dilution:
      • IC50: 6.9 nM (GSK3α), 31 nM (GSK3β)[1]pKi: 8.2 (GSK3α), 7.5 (GSK3β)[1]
      • Concentration:
      • >98%
      • Storage Stability:
      • 2 years -20°C Powder, 2 weeks4°C in DMSO,6 months-80°C in DMSO
      • Other Name:
      • AZD 1080,AZD-1080
      • MolecularWeight(Da):
      • 334.37
      • References:
      • [1]. Georgievska B, et al. AZD1080, a novel GSK3 inhibitor, rescues synaptic plasticity deficits in rodent brain and exhibits peripheral target engagement in humans. J Neurochem. 2013 May;125(3):446-5
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