首页 工具
登录
购物车
WAY 316606

WAY 316606

产品编号 T4468   CAS 915759-45-4

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。

TargetMol的所有产品和服务仅用于科学研究,不能被用于人体,我们也不向个人提供产品和服务。
WAY 316606 Chemical Structure
WAY 316606, CAS 915759-45-4
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
其他形式的 WAY 316606:
产品目录号及名称: WAY 316606 (T4468)
点击图片重新获取验证码
选择批次  
纯度: 100%
更多批次查询请联系客服
生物活性
化学信息
存储 & 溶解度
参考文献
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

存储

Powder: -20°C for 3 years | In solvent: -80°C for 1 year

溶解度

DMSO: 50 mg/mL (111.49 mM)

溶液配制表

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

计算器

摩尔浓度计算器
稀释计算器
配液计算器
分子量计算器
=
X
X
X
=
X
=
/
g/mol

输入分子式,点击计算,可计算出产品的分子量。

参考文献

1. Moore, WJ, et al. Modulation of Wnt Signaling Through Inhibition of Secreted Frizzled-Related Protein I (sFRP-1) with N-Substituted Piperidinyl Diphenylsulfonyl Sulfonamides. Journal of Medicinal Chemistry (2009), 52(1), 105-116. 2. Bodine PV, et al. A small molecule inhibitor of the Wnt antagonist secreted frizzled-related protein-1 stimulates bone formation. Bone. 2009 Jun;44(6):1063-8.
Urea N-(3-Methoxybenzyl)-(9Z,12Z,15Z)-octadecatrienamide Adavivint JW74 Salinomycin sodium salt Ginkgetin Isoquercetin G007-LK

相关化合物库

该产品包含在如下化合物库中:
抑制剂库 经典已知活性库 Wnt/Hedgehog/Notch 通路化合物库 抗前列腺癌化合物库 细胞重编程化合物库 抗结直肠癌化合物库 抗癌细胞代谢库 抗衰老化合物库 干细胞分化化合物库 成骨分子库

剂量换算

对于不同动物的给药剂量换算,您也可以参考 更多...

体内实验配液计算器

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。

第一步:请输入动物实验的基本信息
剂量
mg/kg
每只动物体重
g
给药体积
μL
动物数量
第二步:请输入动物体内配方组成,不同的产品配方组成不同,如有配方需求,可先联系我们提供正确的体内配方。
% DMSO
%
% Tween 80
% ddH2O
计算 重置

技术支持

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。

Keywords

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

 

陶术
生物
TargetMol®中国区唯一合作伙伴
点击进入陶术生物官网陶术生物
联系我们
400-820-0310

上海市静安区江场三路238号8楼