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5-(苯磺酰基)-N-(哌啶-4-基)-2-(三氟甲基)苯磺酰胺

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编辑结构

5-(苯磺酰基)-N-(哌啶-4-基)-2-(三氟甲基)苯磺酰胺

查看77 家供应商

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CAS No. 915759-45-4

分子式 C18H19F3N2O4S2

分子量 448.48

英文名称 BenzenesulfonaMide, 5-(phenylsulfonyl)-N-4-piperidinyl-2-(trifluoroMethyl)-

中文同义词 5-(苯磺酰基)-N-(哌啶-4-基)-2-(三氟甲基)苯磺酰胺;SFRP-1抑制剂(WAY 316606);化合物WAY 316606;方式 316606

基本信息

产品名称

5-(苯磺酰基)-N-(哌啶-4-基)-2-(三氟甲基)苯磺酰胺

中文同义词

5-(苯磺酰基)-N-(哌啶-4-基)-2-(三氟甲基)苯磺酰胺,SFRP-1抑制剂(WAY 316606),化合物WAY 316606,方式 316606

英文名称

BenzenesulfonaMide, 5-(phenylsulfonyl)-N-4-piperidinyl-2-(trifluoroMethyl)-

英文同义词

BenzenesulfonaMide, 5-(phenylsulfonyl)-N-4-piperidinyl-2-(trifluoroMethyl)-;WAY 316606;WAY-316606;5-(Phenylsulfonyl)-N-(piperidin-4-yl)-2-(trifluoromethyl)benzenesulfonamide;WAY-316606;WAY 316606;WAY316606;5-(benzenesulfonyl)-N-piperidin-4-yl-2-(trifluoromethyl)benzenesulfonamide;CS-2786;way-316606 /way 316606

CAS No.

915759-45-4

分子式

C18H19F3N2O4S2

分子量

448.48

EINECS号

1592732-453-0

MDL NO.

MFCD18206894

MOL

915759-45-4.mol

性质

密度

1.50±0.1 g/cm3(Predicted)

形态

粉末

沸点

601.1±65.0 °C(Predicted)

颜色

白色至米白色

酸度系数(pKa)

8.76±0.20(Predicted)

溶解度

DMF：3mg/mL； DMSO：3mg/mL； DMSO:PBS (pH 7.2) (1:10)：0.1 mg/mL

用途

靶点

TargetValue sFRP1 ()

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 EC 50 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 (t 1/2 >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.

体外研究

The EC 50 of WAY-316606 for Wnt-Luciferase Activity from U2-OS Cells is 0.65 μM. WAY-316606 binds to secreted frizzled-related protein (sFRP)-1 inhibitor with a K D of 0.08 μM and inhibits sFRP-1 with an EC 50 of 0.65 μM. WAY-316606 also binds to sFRP-2, albeit over 10 times weaker with a K D 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 IC 50 for WAY-316606 is 0.5 μM.

生物活性

WAY-316606是特异性SFRP1拮抗剂，在人类毛球中激活经典Wnt/β-catenin信号。

编辑结构

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