WAY 316606 is an inhibitor of the secreted proteinsFRP-1, an endogenous antagonist of the secretedglycoproteinWnt. The affinity of WAY-316606 forsFRP-1is determined using theFPbinding assay withIC₅₀of 0.5 μM^[1].

IC50: 0.5 μM (sFRP-1)^[1]

The EC₅₀of WAY-316606 for Wnt-Luciferase Activity from U2-OS Cells is 0.65 μM^[1]. WAY-316606 binds to secreted frizzled-related protein (sFRP)-1 inhibitor with a K_Dof 0.08 μM and inhibits sFRP-1 with an EC₅₀of 0.65 μM. WAY-316606 also binds to sFRP-2, albeit over 10 times weaker with a K_Dof 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 IC₅₀for WAY-316606 is 0.5 μM^[2].

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 EC₅₀of 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^[2].

448.48

Solid

C₁₈H₁₉F₃N₂O₄S₂

915759-45-4

Room temperature in continental US; may vary elsewhere.

DMSO : ≥ 100 mg/mL(222.98 mM)

*"≥" means soluble, but saturation unknown.

请根据产品在不同溶剂中的溶解度选择合适的溶剂配制储备液；一旦配成溶液，请分装保存，避免反复冻融造成的产品失效。
储备液的保存方式和期限：-80℃, 6 months; -20℃, 1 month。-80℃ 储存时，请在 6 个月内使用，-20℃ 储存时，请在 1 个月内使用。

请根据您的实验动物和给药方式选择适当的溶解方案。以下溶解方案都请先按照In Vitro方式配制澄清的储备液，再依次添加助溶剂：

——为保证实验结果的可靠性，澄清的储备液可以根据储存条件，适当保存；体内实验的工作液，建议您现用现配，当天使用； 以下溶剂前显示的百
分比是指该溶剂在您配制终溶液中的体积占比；如在配制过程中出现沉淀、析出现象，可以通过加热和/或超声的方式助溶

• 1.

  请依序添加每种溶剂： 10% DMSO    90% (20%SBE-β-CDin saline)

  Solubility: ≥ 2.5 mg/mL (5.57 mM); Clear solution

  此方案可获得 ≥ 2.5 mg/mL (5.57 mM，饱和度未知) 的澄清溶液。

  以 1 mL 工作液为例，取 100 μL 25.0 mg/mL 的澄清 DMSO 储备液加到 900 μL20% 的 SBE-β-CD 生理盐水水溶液中，混合均匀。

  将 2 g 磺丁基醚 β-环糊精加入 5 mL 生理盐水中，再用生理盐水定容至 10 mL，完全溶解，澄清透明
• 2.

  请依序添加每种溶剂： 10% DMSO    90%corn oil

  Solubility: ≥ 2.5 mg/mL (5.57 mM); Clear solution

  此方案可获得 ≥ 2.5 mg/mL (5.57 mM，饱和度未知) 的澄清溶液，此方案不适用于实验周期在半个月以上的实验。

  以 1 mL 工作液为例，取 100 μL 25.0 mg/mL 的澄清 DMSO 储备液加到 900 μL玉米油中，混合均匀。