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915759-45-4

时间：2023-07-15 来源：化工号作者：C₁₈H₁₉F₃N₂O₄S₂

中间体

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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