WAY 316606 is an inhibitor of the secreted protein sFRP-1, an endogenous antagonist of the secreted glycoprotein Wnt. The affinity of WAY-316606 for sFRP-1 is determined using the FP binding assay with IC50 of 0.5 μM.
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 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.
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.
分子式
C18H19N2O4F3S2
分子量
448.48
CAS号
915759-45-4
运输条件
Room temperature in continental US; may vary elsewhere.