AZD 1080
AZD 1080 Basic information
- Product Name:
- AZD 1080
- Synonyms:
-
- CS-809
- AZD 1080;AZD-1080
- AZD 1080
- AZD1080
- AZD-1080
- 2-Hydroxy-3-(5-(morpholinomethyl)pyridin-2-yl)-1H-indole-5-carbonitrile
- 2-Hydroxy-3-[5-[(morpholin-4-yl)methyl]pyridin-2-yl]-1H-indole-5-carbonitrile
- 2-Hydroxy-3-[5-[(morpholin-4-yl)methyl]pyridin-2-yl]-1H-indole-5-carbonitrile AZD1080
- CAS:
- 612487-72-6
- MF:
- C19H18N4O2
- MW:
- 334.37
- Product Categories:
-
- Inhibitors
- Akt
- mTOR
- PI3K
- Mol File:
- 612487-72-6.mol
AZD 1080 Chemical Properties
- Boiling point:
- 594.0±50.0 °C(Predicted)
- Density
- 1.40±0.1 g/cm3(Predicted)
- storage temp.
- Store at -20°C
- solubility
- insoluble in H2O; insoluble in EtOH; ≥16.7 mg/mL in DMSO
- form
- solid
- pka
- 8.32±0.50(Predicted)
- color
- Light yellow to orange
AZD 1080 Usage And Synthesis
Description
The two isoforms of glycogen synthase kinase 3, GSK3α and GSK3β, constitutively phosphorylate and inactivate glycogen synthase, preventing glycogen synthesis. They also phosphorylate proteins that are relevant to Alzheimer’s disease and osteogenesis. AZD 1080 is a potent, brain permeable inhibitor of GSK3α and GSK3β (Kis = 6.9 and 31 nM, respectively). It shows >14-
Uses
AZD1080 is a selective, orally active, brain permeable glycogen synthase kinase-3 (GSK3) inhibitor (1,2). AZD1080 has shown to rescue synaptic plasticity deficits in rodent brain and exhibit peripheral target engagement in humans.
Definition
ChEBI: AZD1080 is a member of the class of hydroxyindoles that is 1H-indole substituted by hydroxy, 5-(morpholin-4-ylmethyl)pyridin-2-yl, and cyano groups at positions 2, 3 and 5, respectively. It is a potent, brain permeable inhibitor of human GSK3alpha and GSK3beta with Ki of 6.9 nM and 31 nM, respectively. The drug was being developed by AstraZeneca for the treatment of Alzheimer's disease (clinical trial now discontinued). It has a role as an EC 2.7.11.26 (tau-protein kinase) inhibitor, a tau aggregation inhibitor, an antineoplastic agent and an apoptosis inducer. It is a member of morpholines, a member of pyridines, a member of hydroxyindoles, a nitrile and a tertiary amino compound.
target
GSK-3α
References
[1] georgievska b1, sandin j, doherty j, mörtberg a, neelissen j, andersson a, gruber s, nilsson y, schött p, arvidsson pi, hellberg s, osswald g, berg s, fälting j, bhat rv. 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):446-56.
AZD 1080Supplier
- Tel
- sales@boylechem.com
- Tel
- 010-82848833 400-666-7788
- jkinfo@jkchemical.com
- Tel
- +86 (531) 88811783
- sales@trio-pharmatech.com (International market)
- Tel
- 0411-62910999 13889544652
- meilunui@163.com
- Tel
- 025-66099280 17798518460
- cfzhang@aikonchem.com