AZD-2858
AZD-2858 Basic information
- Product Name:
- AZD-2858
- Synonyms:
-
- AZD 2858
- AZD2858
- AZD-2858
- 3-Amino-6-[4-[(4-methyl-1-piperazinyl)sulfonyl]phenyl]-N-3-pyridinyl-pyrazinecarboxamide
- 2-Pyrazinecarboxamide, 3-amino-6-[4-[(4-methyl-1-piperazinyl)sulfonyl]phenyl]-N-3-pyridinyl-
- 3-Amino-6-[4-[(4-methyl-1-piperazinyl)sulfonyl]phenyl]-N-3-pyridinyl-pyrazinecarboxamide AZD2858
- 3-Amino-6-(4-((4-methylpiperazin-1-yl)sulfonyl)phenyl)-N-(pyridin-3-yl)pyrazine-2-carboxamide
- 3-Amino-6-{4-[(4-methyl-1-piperazinyl)sulfonyl]phenyl}-N-(3-pyridinyl)-2-pyrazinecarboxamide
- CAS:
- 486424-20-8
- MF:
- C21H23N7O3S
- MW:
- 453.52
- Product Categories:
-
- Inhibitors
- Akt
- mTOR
- PI3K
- Mol File:
- 486424-20-8.mol
AZD-2858 Chemical Properties
- Density
- 1.408±0.06 g/cm3(Predicted)
- storage temp.
- Store at -20° C
- solubility
- DMSO:8.0(Max Conc. mg/mL);17.64(Max Conc. mM)
- form
- A crystalline solid
- pka
- 7.17±0.70(Predicted)
- color
- Green to khaki
AZD-2858 Usage And Synthesis
Description
AZD2858 is a selective GSK-3 inhibitor with an IC50 of 68 nM, activating Wnt signaling, increases bone mass in rats.
In vitro
AZD2858 is a selective GSK-3 inhibitor with an IC50 of 68 nM, inhibits tau phosphorylation at the S396 site, activates Wnt signaling pathway. AZD2858 treatment (1 μM, 12 h) on primary isolated human osteoblast-like cells results in a 3-fold increase of β-catenin levels. AZD2858 causes β-catenin stabilisation in human and rat mesenchymal stem cells, stimulates hADSC commitment towards osteoblasts and osteogenic mineralisation in vitro.
In vivo
In rats, oral AZD2858 treatment causes a dose-dependent increase in trabecular bone mass compared to control after a two-week treatment with a maximum effect at a dose of 20 mg/kg once daily (total BMC: 172% of control). A small but significant effect is also seen at cortical sites (total BMC: 111% of control). AZD285 treatment (30 μmol/kg) on rats daily for up to 3 weeks shows an increase in both mineral density (of 28% at 2 weeks and 38% at 3 weeks) and mineral content (of 81% at 2 weeks and 93% at 3 weeks) in the calluses. AZD285 treatment makes the fractures heals more rapidly, with a bony callus without an obvious endochondral component. AZD2858 produces time-dependent changes in serum bone turnover biomarkers and increases bone mass over 28 days exposure in rats. After 7 days, AZD2858 increases the bone formation biomarker P1NP, and reduces the resorption biomarker TRAcP-5b, indicating increased bone anabolism and reduced resorption in rats.
Uses
AZD 2858 is a highly selective glycogen synthase kinase-3β (GSK3β) inhibitor used in the treatment of neurological diseases such as Alzheimer’s (1).
Definition
ChEBI: AZD2858 is a member of the class of pyrazines that is pyrazine substituted by (pyridin-3-yl)aminocarbonyl, amino, and 4-(4-methylpiperazine-1-sulfonyl)phenyl groups at positions 2, 3 and 6, respectively. It is a potent inhibitor of GSK3alpha and GSK3beta (IC50 values of 0.9 and 4.9 nM, respectively) and increases bone mass (via Wnt activation) in rats. It has a role as an EC 2.7.11.26 (tau-protein kinase) inhibitor, an antineoplastic agent, a bone density conservation agent and a Wnt signalling activator. It is a member of pyrazines, a secondary carboxamide, a member of pyridines, a N-methylpiperazine, a sulfonamide and an aromatic amine.
storage
Store at -20°C
AZD-2858Supplier
- Tel
- sales@boylechem.com
- Products Intro
- Product Name:AZD-2858
CAS:486424-20-8
Purity:98% Package:1g,10g,100g,1kg
- Tel
- +86 (531) 88811783
- sales@trio-pharmatech.com (International market)
- Products Intro
- Product Name:AZD2858
CAS:486424-20-8
Purity:99% Package:5Mg, 10Mg, 20Mg, 50Mg
- Tel
- 0411-62910999 13889544652
- meilunui@163.com
- Products Intro
- Product Name:AZD-2858
CAS:486424-20-8
Purity:>98% Package:100MG Remarks:4870
- Tel
- 021-58950125
- info@chemexpress.com
- Products Intro
- Product Name:AZD2858
CAS:486424-20-8
Purity:>98% Package:1116RMB/10mg
- Tel
- 400-400-6206333 18521732826
- market@aladdin-e.com
- Products Intro
- Product Name:AZD2858
CAS:486424-20-8
Purity:10mM in DMSO Package:1ml/RMB 720.90
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