• 提示：详情请下载说明书。

• 产品描述： WAY-262611 (BML-WN110, Compound 5) 是一种 beta-catenin (β-Catenin) 的激动剂，可增加骨形成速率，在TCF-荧光素酶测定中的EC50值为0.63 μM。WAY-262611 也是一种 dickkopf 1 (DKK1) 的抑制剂

• 靶点： DKK1;β-Catenin(TCF-Luciferase assay):0.63 μM(EC50)

• 体外研究： WAY-262611, the DKK1 inhibitor, blocks DKK1 and restores the GDF5 reduced MMP13 gene expression

• 体内研究： WAY-262611 has excellent pharmacokinetic properties and shows a dose dependent increase in the trabecular bone formation rate in ovariectomized rats following oral administration

• 细胞实验： Cell lines: Surplus human chondrocytes Concentrations: 0.01 μM, 0.1 μM, 1 μM Incubation Time: 21 days Method: Chondrocytes are resuspended at 1.25×106 cells/ml in basic differentiation media (BDM) consisting of DMEM high glucose supplemented with 100 nM dexamethasone, 1× insulin-transferrin-selenous acid premix (ITS), 1.0 mg/ml human serum albumin supplemented with 5.0 μg/ml linoleic acid, 14 μg/ml L-ascorbic acid 2-phosphate and 1× Penicilline-Streptomycin. The cell suspension is divided into aliquots of 200 μl to each well of an uncoated flat bottom 96-well plate. The plate is centrifuged at 1,500 rpm for 5 min and incubated for 48 h at 37°C in 5% CO2 and 90% relative humidity to allow for pellet formation. After 48 h the culture medium is changed to BDM supplemented with appropriate growth factors (GFs); 2, 10, 100 or 200 ng/ml recombinant GDF5, 50 ng/ml recombinant Wnt3a, 0.5 μM GSK3b inhibitor CHIR-99021, 0.01, 0.1 or 1 μM DKK1 inhibitor WAY-262611. Medium is changed three times per week for 21 days,

• 动物实验： Animal Models: OVX rats Dosages: 0.3 mg/kg, 1 mg/kg, 3 mg/kg, 10 mg/kg; 2 mg/kg Administration: Oral gavage; IV

• 参考文献：
  1. Jeffrey C Pelletier, et al. (1-(4-(Naphthalen-2-yl)pyrimidin-2-yl)piperidin-4-yl)methanamine: a wingless beta-catenin agonist that increases bone formation rate. J Med Chem. 2009 Nov 26;52(22):6962-5. 2. L Enochson, et al. GDF5 reduces MMP13 expression in human chondrocytes via DKK1 mediated canonical Wnt signaling inhibition. Osteoarthritis Cartilage. 2014 Apr;22(4):566-77.

• 溶解性： Soluble  in  DMSO、Ethanol、H2O

• 保存条件： -20℃

• 配置溶液浓度参考：
  

  	1mg	5mg	10mg
  1 mM	3.141 ml	15.703 ml	31.406 ml
  5 mM	0.628 ml	3.141 ml	6.281 ml
  10 mM	0.314 ml	1.57 ml	3.141 ml
  50 mM	0.063 ml	0.314 ml	0.628 ml

• 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。

输入产品批号：

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 分子量 (g/mol)

• pg ng μg mg g kg =
  fM pM nM μM mM M *
  nL μL mL L *