中文名称: WAY 316606
英文名称: WAY 316606
CAS No: 915759-45-4
分子式: C18H19F3N2O4S2
分子量: 448.47967
W10063 WAY 316606 ≥98% (psaitong)
包装规格:
5mg 25mg 50mg 100mg in glass bottle
溶解性:
溶于DMSO(≥100mg/mL)
产品描述:

基本信息

产品编号:

W10063 

产品名称:

WAY 316606

CAS:

915759-45-4

 

储存条件

粉末

-20℃

四年

 

 

分子式:

C18H19F3N2O4S2

溶于液体

-80℃

两年

分子量

448.48

-20℃

1个月

化学名: 

5-(Phenylsulfonyl)-N-(piperidin-4-yl)-2-(trifluoromethyl)benzenesulfonamide

Solubility (25°C):

 

体外:

 

DMSO

90 mg/mL (200.67 mM)

Ethanol

7 mg/mL (15.6 mM)

Water

Insoluble

体内(现配现用):

1.请依序添加每种溶剂: 10% DMSO→90% (20% SBE-β-CD in saline)

Solubility: ≥ 2.5 mg/mL (5.57 mM); Clear solution

此方案可获得 ≥ 2.5 mg/mL (5.57 mM,饱和度未知) 的澄清溶液。

1 mL 工作液为例,取 100 μL 25.0 mg/mL 的澄清 DMSO 储备液加到 900 μL 20% 的 SBE-β-CD 生理盐水水溶液中,混合均匀。

2.请依序添加每种溶剂: 10% DMSO→90% corn oil

Solubility: ≥ 2.5 mg/mL (5.57 mM); Clear solution

此方案可获得 ≥ 2.5 mg/mL (5.57 mM,饱和度未知) 的澄清溶液,此方案不适用于实验周期在半个月以上的实验。

1 mL 工作液为例,取 100 μL 25.0 mg/mL 的澄清 DMSO 储备液加到 900 μL玉米油中,混合均匀。

1mg/ml表示微溶或不溶。

普西唐提供的所有化合物浓度为内部测试所得,实际溶液度可能与公布值有所偏差,属于正常的批间细微差异现象。

请根据产品在不同溶剂中的溶解度选择合适的溶剂配制储备液;⼀旦配成溶液,请分装保存,避免反复冻融造成的产品失效。

 

制备储备液

 

浓度

 

溶液体积

质量

 

1mg

 

5mg

 

10mg

1 mM

2.2298 mL

11.1488 mL

22.2975 mL

5 mM

0.4460 mL

2.2298 mL

4.4595 mL

10 mM

0.2230 mL

1.1149 mL

2.2298 mL

50 mM

0.0446 mL

0.2230 mL

0.4460 mL

 

生物活性

产品描述

一种分泌蛋白 sFRP-1 抑制剂,是分泌性糖蛋白 Wnt 的拮抗剂,在 FP 结合检测使用中,WAY-316606 作用于 sFRP-1 的 IC50 为 0.5 μM。

靶点

IC50: 0.5 μM (sFRP-1)

体外研究

The EC50 of WAY-316606 for Wnt-Luciferase Activity from U2-OS Cells is 0.65 μM. WAY-316606 binds to secreted frizzledrelated 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.

体内研究

WAY-316606 increases bone formation when tested in a neonatal murine calvarial assay. WAY-316606 increases total bone area up to 60% in a dose-dependent manner with an EC50 of about 1 nM. WAY-316606 has 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

特征

 

 

推荐实验方法(仅供参考)

Kinase Assay

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. Fluorescence changes are fitted to a quadratic equation to obtain apparent dissociation constants

 

Cell Assay

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 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. WAY-316606, or vehicle (typically DMSO), diluted in phenol red-free RPMI 1640 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 luciferase substrate.

保存条件:
-20℃
UN码:
HazardClass:
危害声明:
安全说明:
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参考文献 & 客户发表文献

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 (g) = 浓度 (mol/L) x 体积 (L) x 分子量 (g/mol)

摩尔浓度计算公式

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开始浓度 x 开始体积 = 最终浓度 x 最终体积

稀释公式

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  • 计算结果

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    C2=C1/X C2: LOG(C2):
    C3=C2/X C3: LOG(C3):
    C4=C3/X C4: LOG(C4):
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    C7=C6/X C7: LOG(C7):
    C8=C7/X C8: LOG(C8):