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| 品牌 | absin | CAS | 486424-20-8 |
|---|---|---|---|
| 分子式 | C21H23N7O3S | 纯度 | ＞98% |
| 分子量 | 453.52 | 货号 | abs810773 |
| 规格 | 10mg | 供货周期 | 现货 |
| 主要用途 | is a selective GSK-3 inhibitor with an I | 应用领域 | 化工,生物产业,农林牧渔,制药/生物制药,综合 |
AZD2858 486424-20-8
| 产品描述 | |
| 描述 | AZD2858 is a selective GSK-3 inhibitor with an IC50 of 68 nM, activating Wnt signaling, increases bone mass in rats. |
| 纯度 | >98% |
| 储存/保存方法 | Store at -20℃ for one year（Powder）；Store at 2-4℃ for two weeks；Store at -20℃ for six months after dissolution. |
| 基本信息 | |
| 别名 | AZD-2858；AZD 2858 |
| 外观 | Green to khaki Powder |
| 可溶性/溶解性 | DMSO : 7 mg/mL (15.43 mM) |
| 生物活性 | |
| 靶点 | GSK-3 |
| In vitro(体外研究) | 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(体内研究) | 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. |
| 研究领域 | |
| 研究领域 | EpigeneticsChromatin Modifying EnzymesPhosphorylation Drug DiscoverySmall Molecule DrugLead Compound Discovery |
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