915759-45-4 |
| 时间：2023-07-15 来源：化工号 作者：C18H19F3N2O4S2 |
方式 316606化合物WAY 316606SFRP-1抑制剂(WAY 316606)5-(苯磺酰基)-N-(哌啶-4-基)-2-(三氟甲基)苯磺酰胺
| 中文名 | WAY 316606
| | 英文名 | WAY 316606
| | 别名 | 方式 316606
化合物WAY 316606
SFRP-1抑制剂(WAY 316606)
5-(苯磺酰基)-N-(哌啶-4-基)-2-(三氟甲基)苯磺酰胺
| | 英文别名 | CS-2786
WAY316606
WAY-316606
WAY 316606
5-(benzenesulfonyl)-N-piperidin-4-yl-2-(trifluoromethyl)benzenesulfonamide
BenzenesulfonaMide, 5-(phenylsulfonyl)-N-4-piperidinyl-2-(trifluoroMethyl)-
5-(Phenylsulfonyl)-N-(piperidin-4-yl)-2-(trifluoromethyl)benzenesulfonamide
| | CAS | 915759-45-4
| | EINECS | 1592732-453-0 | | 化学式 | C18H19F3N2O4S2
| | 分子量 | 448.4796696 | | 密度 | 1.50±0.1 g/cm3(Predicted) | | 沸点 | 601.1±65.0 °C(Predicted) | | 酸度系数 | 8.76±0.20(Predicted) | | 存储条件 | 2-8℃ | | 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. | | 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. |
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