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S80740

AZD2858

源叶(MedMol) 98%
  • 英文名:
  • AZD2858
  • 别名:
  • 3-氨基-6-[4-(4-甲基哌嗪-1-基)磺酰基苯基]-N-吡啶-3-基吡嗪-2-羧酰胺
  • CAS号:
  • 486424-20-8
  • 分子式:
  • C21H23N7O3S
  • 分子量:
  • 453.52
  • 核磁/质谱:
品牌货号产品规格价格(RMB) 库存(上海) 北京 武汉 南京 数量计量单位 加入购物车...
源叶(MedMol) S80740-1mg 98% ¥232.00元 >10 - - - EA 加入购物车
源叶(MedMol) S80740-5mg 98% ¥360.00元 7 - - - EA 加入购物车
源叶(MedMol) S80740-10mg 98% ¥624.00元 8 - - - EA 加入购物车
源叶(MedMol) S80740-25mg 98% ¥1520.00元 预计交期:2-3天 - - - EA 加入购物车
源叶(MedMol) S80740-50mg 98% ¥2160.00元 6 - - - EA 加入购物车
源叶(MedMol) S80740-100mg 98% ¥4160.00元 预计交期:2-3天 - - - EA 加入购物车
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  • 提示:详情请下载说明书。
  • 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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