S80740 |
AZD2858 |
源叶(MedMol) | 98% |
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- 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.
- 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:
1mg 5mg 10mg 1 mM 2.205 ml 11.025 ml 22.05 ml 5 mM 0.441 ml 2.205 ml 4.41 ml 10 mM 0.22 ml 1.102 ml 2.205 ml 50 mM 0.044 ml 0.22 ml 0.441 ml
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本计算器可帮助您计算出特定溶液中溶质的质量、溶液浓度和体积之间的关系,公式为:
质量 (mg) = 浓度 (mM) x 体积 (mL) x 分子摩尔量 (g/mol)