AZD-2858
Description In vitro In vivo- Product Name
- AZD-2858
- CAS No.
- 486424-20-8
- Chemical Name
- AZD-2858
- Synonyms
- CS-980;AZD2858;AZD 2858;AZD-2858;AZD-2858;AZD 2858;AZD-2858 USP/EP/BP;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)-2-pyrazinecarboxamide;3-Amino-6-(4-((4-methylpiperazin-1-yl)sulfonyl)phenyl)-N-(pyridin-3-yl)pyrazine-2-carboxamide
- CBNumber
- CB32668221
- Molecular Formula
- C21H23N7O3S
- Formula Weight
- 453.52
- MOL File
- 486424-20-8.mol
AZD-2858 Property
- 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)
Hazard and Precautionary Statements (GHS)
- Symbol(GHS)
-
- Signal word
- Danger
- Hazard statements
-
H301Toxic if swalloed
H341Suspected of causing genetic defects
H372Causes damage to organs through prolonged or repeated exposure
- Precautionary statements
-
P201Obtain special instructions before use.
P202Do not handle until all safety precautions have been read and understood.
P260Do not breathe dust/fume/gas/mist/vapours/spray.
P264Wash hands thoroughly after handling.
P264Wash skin thouroughly after handling.
P270Do not eat, drink or smoke when using this product.
P281Use personal protective equipment as required.
P301+P310IF SWALLOWED: Immediately call a POISON CENTER or doctor/physician.
P308+P313IF exposed or concerned: Get medical advice/attention.
P314Get medical advice/attention if you feel unwell.
P321Specific treatment (see … on this label).
P330Rinse mouth.
P405Store locked up.
P501Dispose of contents/container to..…
N-Bromosuccinimide Price
- Product number
- 16728
- Product name
- AZD 2858
- Purity
- ≥98%
- Packaging
- 1mg
- Price
- $33
- Updated
- 2024/03/01
- Product number
- 16728
- Product name
- AZD 2858
- Purity
- ≥98%
- Packaging
- 5mg
- Price
- $120
- Updated
- 2024/03/01
- Product number
- 16728
- Product name
- AZD 2858
- Purity
- ≥98%
- Packaging
- 10mg
- Price
- $176
- Updated
- 2024/03/01
- Product number
- A808095
- Product name
- AZD2858
- Packaging
- 25mg
- Price
- $345
- Updated
- 2021/12/16
- Product number
- CS-1672
- Product name
- AZD2858
- Purity
- 99.42%
- Packaging
- 10mg
- Price
- $144
- Updated
- 2021/12/16
AZD-2858 Chemical Properties,Usage,Production
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-2858 Preparation Products And Raw materials
Raw materials
Preparation Products
AZD-2858 Suppliers
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View Lastest Price from AZD-2858 manufacturers
- Product
- AZD-2858 486424-20-8
- Price
- US $2.00/kg
- Min. Order
- 1kg
- Purity
- 99%
- Supply Ability
- 100kg
- Release date
- 2018-12-24