Powder: -20°C for 3 years | In solvent: -80°C for 1 year
WAY 316606 是一种分泌性糖蛋白Wnt 的拮抗剂,是一种分泌蛋白sFRP-1抑制剂,在 FP 结合检测使用中,它作用于 sFRP-1 的IC50为 0.5 μM。
规格 | 价格/CNY | 货期 | 数量 | |
---|---|---|---|---|
1 mg | ¥ 315 | 现货 | ||
5 mg | ¥ 747 | 现货 | ||
10 mg | ¥ 1,180 | 现货 | ||
25 mg | ¥ 2,170 | 现货 | ||
50 mg | ¥ 3,620 | 现货 | ||
100 mg | ¥ 5,280 | 现货 | ||
1 mL * 10 mM (in DMSO) | ¥ 828 | 现货 |
产品描述 | WAY 316606 is an inhibitor of the secreted protein sFRP-1, an endogenous antagonist of the secreted glycoprotein Wnt. |
靶点活性 | sFRP-1:0.5 μM |
体外活性 | The EC50 of WAY-316606 for Wnt-Luciferase Activity from U2-OS Cells is 0.65 μM[1]. WAY-316606 binds to the secreted frizzled-related protein (sFRP)-1 inhibitor with a KD of 0.08 μM and inhibits sFRP-1 with an EC50 of 0.65 μM. WAY-316606 also binds to sFRP-2, albeit over 10 times weaker with a KD of 1 μM. Using a fluorescence polarization binding assay that employs a fluorescent probe compound and purified human sFRP-1 protein in a competitive-binding format, the IC50 for WAY-316606 is 0.5 μM [2]. |
体内活性 | WAY-316606 increases bone formation when tested in a neonatal murine calvarial assay. WAY-316606 increases total bone area by up to 60% in a dose-dependent manner with an EC50 of about 1 nM. WAY-316606 has a good aqueous solubility, moderate to low inhibition of cytochrome p450 isozymes (3A4, 2D6, 2C9) and good stability in rat and human liver microsomes (t1/2>60 min in each species). In female Sprague-Dawley rats, WAY-316606 exhibits high plasma clearance (77 mL/min/kg, greater than hepatic blood flow) following a single intravenous bolus dose (2 mg/kg), which results in a rapid decline of drug exposure in the plasma despite the route of administration [2]. |
激酶实验 | WAY-316606 binding to purified sFRP is determined by spectroscopy methods. The sFRP-1 or -2 stock solutions are diluted to 1 μM in a buffered solution and the initial fluorescence is measured. Increasing concentrations of WAY-316606 (0 to 50 μM) are added to the protein in the cuvette and incubated for 5 min prior to assessing fluorescence intensity using a Fluoromax-2 fluorometer. In control experiments, the DMSO (vehicle control)-matched buffer solution is used. Fluorescence spectra are scanned in the ratio mode (S/R, signal/reference) to compensate for variations in lamp output as a function of wavelength [2]. |
细胞实验 | U2OS bone cells are infected with recombinant adenovirus 5 (Ad5)?WNT3 at a multiplicity of infection (MOI) of 2, followed by infection with Ad5-sFRP-1 and Ad5-16xTCF-luciferase, each at an MOI of 10. Four hours after infection, the cells are frozen in sterile cryogenic vials at a cell density of 9×106 cells/mL and stored in a ?150°C freezer. For the assay, a vial of frozen cells is thawed, and the cells are resuspended in plating medium [phenol red-free RPMI 1640 medium containing 5% fetal calf serum, 2 mM GlutaMAX-l, and 1% (v/v) penicillin-streptomycin] to a final cell density of 1.5×105 cells/mL. The resuspended cells are then plated in 96-well tissue culture treated plates at a volume of 100 μL of cell suspension/well (i.e., 1.5×104 cells/well). The plates are incubated at 37°C inside a 5% CO2/ 95% humidified air incubator for 5 h or until the cells have attached and started to spread. Prior to the addition of WAY-316606, the medium is replaced with 50 μL/well of phenol red-free RPMI 1640 containing 10% fetal calf serum, 2 mM GlutaMAX-l, and 1% (v/v) penicillin-streptomycin. WAY-316606, or vehicle (typically DMSO), diluted in phenol red-free RPMI 1640 containing 2 mM GlutaMAX-l, and l % (v/v) penicillin-streptomycin are then added to the wells in replicates of 4 wells/dilution and the plates are incubated at 37°C overnight. Dose?response experiments are performed with the compounds in 2-fold serial dilutions from 10000?4.9 nM. After the overnight incubation, the cells are washed twice with 150 uL/well of PBS w/o calcium or magnesium and lysed with 50 μL/well of 1× cell culture lysis reagent on a shaker at room temperature for 30 min. Aliquots of the cell lysates (30 μL) are transferred to 96-well luminometer plates, and the luciferase activity is measured in a MicroLumat PLUS luminometer using 100 μL/well of a luciferase substrate. |
分子量 | 448.48 |
分子式 | C18H19F3N2O4S2 |
CAS No. | 915759-45-4 |
Powder: -20°C for 3 years | In solvent: -80°C for 1 year
DMSO: 50 mg/mL (111.49 mM)
可选溶剂 | 浓度 体积 质量 | 1 mg | 5 mg | 10 mg | 25 mg |
DMSO | 1 mM | 2.2298 mL | 11.1488 mL | 22.2975 mL | 55.7438 mL |
5 mM | 0.446 mL | 2.2298 mL | 4.4595 mL | 11.1488 mL | |
10 mM | 0.223 mL | 1.1149 mL | 2.2298 mL | 5.5744 mL | |
20 mM | 0.1115 mL | 0.5574 mL | 1.1149 mL | 2.7872 mL | |
50 mM | 0.0446 mL | 0.223 mL | 0.446 mL | 1.1149 mL | |
100 mM | 0.0223 mL | 0.1115 mL | 0.223 mL | 0.5574 mL |
对于不同动物的给药剂量换算,您也可以参考 更多...
请在以下方框中输入您的动物实验信息后点击计算,可以得到母液配置方法和体内配方的制备方法: 比如您的给药剂量是10 mg/kg,每只动物体重20 g,给药体积100 μL,一共给药动物10 只,您使用的配方为5% DMSO+30% PEG300+5% Tween 80+60% ddH2O。那么您的工作液浓度为2 mg/mL。
母液配置方法:2 mg 药物溶于 50 μL DMSO (母液浓度为 40 mg/mL), 如您需要配置的浓度超过该产品的溶解度,请先与我们联系。
体内配方的制备方法:取 50 μL DMSO 主液,加入 300 μL PEG300, 混匀澄清,再加 50 μL Tween 80,混匀澄清,再加 600 μL ddH2O, 混匀澄清。
您可能有的问题的答案可以在抑制剂处理说明中找到,包括如何准备库存溶液,如何存储产品,以及基于细胞的分析和动物实验需要特别注意的问题。
WAY 316606 915759-45-4 Cytoskeletal Signaling Stem Cells Wnt/beta-catenin FrzA Secreted frizzled related protein 1 WAY316606 WAY-316606 sFRP-1 SARP-2 Inhibitor inhibit inhibitor