| 货号 | 规格 | 价格 | 上海 | 北京 | 武汉 | 南京 | 购买数量 |
|---|---|---|---|---|---|---|---|
S80740-1mg |
99.9% | ￥232.00 | >10 | - | - | - |
|
S80740-5mg |
99.9% | ￥360.00 | 7 | - | - | - |
|
S80740-10mg |
99.9% | ￥624.00 | 8 | - | - | - |
|
S80740-25mg |
≥98% | ￥1520.00 | 货期：2-3天 | - | - | - |
|
S80740-50mg |
99.9% | ￥2160.00 | 6 | - | - | - |
|
S80740-100mg |
≥98% | ￥4160.00 | 货期：2-3天 | - | - | - |
|
AZD2858 is a potent, orally active GSK-3 inhibitor, with IC50s of 0.9 and 5 nM for GSK-3α and GSK-3β, respectively, used in the research of fracture healing.
| 产品描述： | AZD2858 is a potent, orally active GSK-3 inhibitor, with IC50s of 0.9 and 5 nM for GSK-3α and GSK-3β, respectively, used in the research of fracture healing. | ||||||||||||||||||||
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| 靶点： | GSK-3α：0.9 nM (IC50);GSK-3β:5 nM (IC50);CDK5/p25:356 nM (IC50)；Haspin：366 nM (IC50)；CDK5/p35：387 nM (IC50)；DYRK2：491 nM (IC50)；CDK2/cyclin A：810 nM (IC50)；CDK1/cyclin B：1246 nM (IC50);PIM3:1269 nM (IC50);TLK2:1381 nM (IC50);PKD2:2462 nM (IC50);CDK2/cyclin E:3310 nM (IC50);Aurora-A:4966 nM (IC50);GSK-3 | ||||||||||||||||||||
| 体内研究： | AZD2858 (20 mg/kg) causes a dose-dependent increase in trabecular bone mass compared to control after a two-week treatment with a maximum effect. AZD2858 exhibits a substantial effect on fracture healing. AZD2858 (20 mg/kg) causes an increase in cortical BMC of 9%, cortical area of 10%, and cortical thickness of 11% at 3 weeks in the non-operated right femur of rats. AZD2858 (30 μmol/kg/day) alters the biomarkers of bone turnover with statistically significant increases in P1NP and decreases in TRAcP-5b seen from 3 days of treatment and onwards. AZD2858 demonstrates significant changes in serum bone turnover markers (P1NP and TRAcP-5b) and femur bone formation after only 7 days of daily dosing. AZD2858 (AR28, 30 mg/kg, s.c.) stimulates an increase in an initial wave of mesenchymal progenitors with osteogenic and adipogenic potential and drives their differentiation to the osteogenic lineage in BALB/c mice. AR28 (30 mg/kg, s.c.) enhances the proliferation of committed hematopoietic progenitors and their differentiation to the osteoclast lineage but does not prevent an overall increase in bone mass | ||||||||||||||||||||
| 参考文献： | 1. Marsell R, et al. GSK-3 inhibition by an orally active small molecule increases bone mass in rats. Bone. 2012 Mar;50(3):619-27. 2. Sisask G, et al. Rats treated with AZD2858, a GSK3 inhibitor, heal fractures rapidly without endochondral bone formation. Bone. 2013 May;54(1):126-32. 3. Gilmour PS, et al. Human stem cell osteoblastogenesis mediated by novel glycogen synthase kinase 3 inhibitors induces bone formation and a unique bone turnover biomarker profile in rats. Toxicol Appl Pharmacol. 2013 Oct 15;272(2):399-407. 4. Gambardella A, et al. Glycogen synthase kinase-3α/β inhibition promotes in vivo amplification of endogenous mesenchymal progenitors with osteogenic and adipogenic potential and their differentiation to the osteogenic lineage. J Bone Miner Res. 2011 Apr;26 | ||||||||||||||||||||
| 溶解性： | DMSO : 12.5 mg/mL (27.56 mM; Need ultrasonic) | ||||||||||||||||||||
| 保存条件： | -20℃ | ||||||||||||||||||||
| 配置溶液浓度参考： |
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| 注意： | 部分产品我司仅能提供部分信息，我司不保证所提供信息的权威性，仅供客户参考交流研究之用。 |
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