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CAS No.: 915759-45-4

WAY 316606 Catalog No. CSN18570

Synonyms: WAY-316606

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.

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实验方案

技术信息

生物活性

描述The Wnt signaling pathway is activated by secreted Wnt glycoproteins and regulates various biological processes, including skeletal development. Secreted frizzled-related protein-1 (sFRP-1) is a negative regulator or an antagonist of the Wnt signaling pathway. WAY-316606 is identified as an inhibitor of sFRP-1 with IC₅₀ value of 0.5 μM^[3]. WAY-316606 enhanced total bone area up to 60% in a dose-dependent manner when tested in a neonatal murine ex vivo calvarial assay^[3]. WAY-316606 treated rat mandibles (1 mM, 10 uL, on alternate days for 7 days) showed a substantial gain of interradicular bone mass near the inhibitor application site compared to rat mandibles treated with a vehicle control, in MicroCT analysis^[4]. Differentiating periodontal ligament cells cultured with 1 and 2 uM of WAY-316606 showed increased alkaline phosphatase activity and enhanced mineral deposits in a dose dependent manner compared to cells cultured with induction media alone^[4].
作用机制WAY-316606 inhibits sFRP-1 perhaps via the netrin domain.
动物研究
剂量
Rat: 2 mg/kg^[2] (i.v.)

给药途径
i.v.
参考文献

动物研究
剂量	Rat: 2 mg/kg^[2] (i.v.)
给药途径	i.v.

[1] Moore WJ, Kern JC, et al. Modulation of Wnt signaling through inhibition of secreted frizzled-related protein I (sFRP-1) with N-substituted piperidinyl diphenylsulfonyl sulfonamides. J Med Chem. 2009 Jan 8;52(1):105-16.
[2] Bodine PV, Stauffer B, et al. A small molecule inhibitor of the Wnt antagonist secreted frizzled-related protein-1 stimulates bone formation. Bone. 2009 Jun;44(6):1063-8.
[3] Moore WJ, Kern JC, Bhat R, Commons TJ, Fukayama S, Goljer I, Krishnamurthy G, Magolda RL, Nogle L, Pitts K, Stauffer B, Trybulski EJ, Welmaker GS, Wilson M, Bodine PV. Modulation of Wnt signaling through inhibition of secreted frizzled-related protein I (sFRP-1) with N-substituted piperidinyl diphenylsulfonyl sulfonamides. J Med Chem. 2009 Jan 8;52(1):105-16. doi: 10.1021/jm801144h. PMID: 19072540.
[4] Gopinathan G, Foyle D, Luan X, Diekwisch TGH. The Wnt Antagonist SFRP1: A Key Regulator of Periodontal Mineral Homeostasis. Stem Cells Dev. 2019 Aug 1;28(15):1004-1014. doi: 10.1089/scd.2019.0124. Epub 2019 Jul 22. PMID: 31215318; PMCID: PMC6661921.

实验方案

计算器摩尔计算器总药量计算器工作液计算器
储存液制备
- 1 mg
- 5 mg
- 10 mg
- 1 mM
- 2.2298 mL
- 11.1488 mL
- 22.2976 mL
- 5 mM
- 0.4460 mL
- 2.2298 mL
- 4.4595 mL
- 10 mM
- 0.2230 mL
- 1.1149 mL
- 2.2298 mL

技术信息

CAS号

915759-45-4

储存条件

粉末: Keep in dark place,Inert atmosphere,Room temperature

液体: -20°C:3-6 月 -80°C:12月

分子式

C18H19F3N2O4S2

运输

蓝冰

分子量

448.48

别名

WAY-316606

溶解度

DMSO	90.0 mg/mL (200.7 mM)
Water	Insoluble
Ethanol	7.0 mg/mL (15.6 mM)

动物实验配方

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