产品信息
抗原名称
sFRP-1
商品描述
WAY-316606 is a small molecule inhibitors of the secreted protein sFRP-1, an endogenous antagonist of the secreted glycoprotein Wnt.
分子量
448.48
纯度
>98%
可溶性
DMSO : ≥ 100 mg/mL (222.98 mM)
In vitro(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.
In vivo(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.
背景
分子式
C18H19F3N2O4S2
CAS号
915759-45-4
制备和贮存
保存方式
Store at -20℃ for one year（Powder）；Store at 2-4℃ for two weeks；Store at -20℃ for six months after dissolution.
参考图片
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