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AZD 1080

Product Name
AZD 1080
CAS No.
612487-72-6
Chemical Name
AZD 1080
Synonyms
CS-809;AZD1080;AZD-1080;AZD 1080;AZD 1080;AZD-1080;AZD 1080 USP/EP/BP;AZD1080 AZD-1080 GSK-3 Inhibitor;2-Hydroxy-3-(5-(morpholinomethyl)pyridin-2-yl)-1H-indole-5-carbonitrile;2-hydroxy-3-[5-(4-morpholinylmethyl)-2-pyridinyl]-1H-indole-5-carbonitrile;2-Hydroxy-3-[5-[(morpholin-4-yl)methyl]pyridin-2-yl]-1H-indole-5-carbonitrile
CBNumber
CB72666593
Molecular Formula
C19H18N4O2
Formula Weight
334.37
MOL File
612487-72-6.mol
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AZD 1080 Property

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
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Hazard and Precautionary Statements (GHS)

Symbol(GHS)
Signal word
Warning
Hazard statements

H302Harmful if swallowed

H315Causes skin irritation

H319Causes serious eye irritation

H335May cause respiratory irritation

Precautionary statements

P261Avoid breathing dust/fume/gas/mist/vapours/spray.

P305+P351+P338IF IN EYES: Rinse cautiously with water for several minutes. Remove contact lenses, if present and easy to do. Continuerinsing.

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N-Bromosuccinimide Price

Cayman Chemical
Product number
16676
Product name
AZD 1080
Purity
≥95%
Packaging
1mg
Price
$29
Updated
2024/03/01
Cayman Chemical
Product number
16676
Product name
AZD 1080
Purity
≥95%
Packaging
5mg
Price
$102
Updated
2024/03/01
Cayman Chemical
Product number
16676
Product name
AZD 1080
Purity
≥95%
Packaging
10mg
Price
$145
Updated
2024/03/01
Cayman Chemical
Product number
16676
Product name
AZD 1080
Purity
≥95%
Packaging
25mg
Price
$326
Updated
2024/03/01
TRC
Product number
A808085
Product name
AZD1080
Packaging
10mg
Price
$360
Updated
2021/12/16
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AZD 1080 Chemical Properties,Usage,Production

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-fold selectivity against several kinases, receptors, enzymes, and ion channels. AZD 1080 inhibits tau phosphorylation in cells. It shows good bioavailability after oral administration in vivo, inhibiting hippocampal tau phosphorylation and reversing cognitive deficits induced by the NMDA receptor antagonist (+)-MK-801 . In humans, oral AZD 1080 inhibits GSK3 activity in peripheral blood lymphocytes following an initial delay in response.

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 1080 Preparation Products And Raw materials

Raw materials

Preparation Products

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AZD 1080 Suppliers

Shanghai Boyle Chemical Co., Ltd.
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Fax
86-21-57758967
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sales@boylechem.com
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China
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J & K SCIENTIFIC LTD.
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010-82848833 400-666-7788
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86-10-82849933
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jkinfo@jkchemical.com
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China
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Jinan Trio PharmaTech Co., Ltd.
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+86 (531) 88811783
Fax
+86 (531) 55696010 QQ 1762738062
Email
sales@trio-pharmatech.com (International market)
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China
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Dalian Meilun Biotech Co., Ltd.
Tel
0411-62910999 13889544652
Email
meilunui@163.com
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China
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Jiangsu Aikon Biopharmaceutical R&D co.,Ltd.
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025-66099280 17798518460
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(1)02557626880
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cfzhang@aikonchem.com
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China
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Haoyuan Chemexpress Co., Ltd.
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021-58950125
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(86) 21-58955996
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info@chemexpress.com
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China
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7552
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Shanghai Aladdin Bio-Chem Technology Co.,LTD
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400-400-6206333 18521732826
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021-50323701
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market@aladdin-e.com
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China
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MedChemexpress LLC
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021-58955995
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609-228-5909
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sales@medchemexpress.cn
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United States
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4861
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AdooQ BioScience, LLC
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+1 (866) 930-6790
Fax
+1 (866) 333-9607
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info@adooq.com
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United States
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2782
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CEG Chemical Science&Technology Co., Ltd.
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Mobile:13665161512
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+86-510-68873513
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China
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1785
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View Lastest Price from AZD 1080 manufacturers

Career Henan Chemical Co
Product
AZD 1080 612487-72-6
Price
US $2.00/kg
Min. Order
1kg
Purity
99%
Supply Ability
100kg
Release date
2018-12-24

612487-72-6, AZD 1080Related Search:


  • 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
  • 2-hydroxy-3-[5-(4-morpholinylmethyl)-2-pyridinyl]-1H-indole-5-carbonitrile
  • AZD 1080 USP/EP/BP
  • AZD1080 AZD-1080 GSK-3 Inhibitor
  • 612487-72-6
  • Inhibitors
  • Akt
  • mTOR
  • PI3K