WAY 316606
(Synonyms: 5-(苯磺酰基)-N-(哌啶-4-基)-2-(三氟甲基)苯磺酰胺,WAY-316606;WAY316606) 目录号 : GC15661
WAY 316606是一种强效分泌型卷曲相关蛋白1（sFRP-1）抑制剂，IC50值为0.5μM。
Cas No.:915759-45-4
Sample solution is provided at 25 µL, 10mM.
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WAY 316606 is a potent inhibitor of Secreted Frizzled-Related Protein I (sFRP-1), with an IC50 value of 0.5μM[1]. WAY 316606 can regulate the activation of Wnt signaling pathway by inhibiting sFRP-1 activity, and is used as a key regulator to modulate osteoclastogenesis and bone resorption[2]. WAY 316606 can be used as a hair growth promoter in human hair follicle organ models to induce hair growth in humans[3].
In vitro, WAY 316606 treatment at 2μM for 72 hours stimulated the proliferation of human neural stem cells, and increased the activity of the Wnt pathway[4]. Treatment with 2μM WAY 316606 for 7 days significantly increased mineralization and the expression of mineralization-related genes in periodontal ligament fibroblasts, and improved mineral homeostasis[5]. Treatment with 2μM WAY 316606 for 12 hours can partially alleviate the growth inhibition of U251 cells induced by H2O2 (1 mM; 12 hours), reduce cell apoptosis, and increase cell viability[6].
In vivo, WAY 316606 treatment (0.5μM/5μL) via intraneural injection per 3 days for 2 weeks significantly promoted the axon regrowth of transected nerves in mice following nerve transection[7]. In female Sprague-Dawley rats, WAY 316606 exhibited high plasma clearance (77mL/min/kg) following a single intravenous bolus dose (2mg/kg)[8].
References:
[1] Moore W J, Kern J C, Bhat R, et al. Modulation of Wnt signaling through inhibition of secreted frizzled-related protein I (sFRP-1) with N-substituted piperidinyl diphenylsulfonyl sulfonamides[J]. Journal of medicinal chemistry, 2009, 52(1): 105-116.
[2] Ma Q, Wang S, Xie Z, et al. The SFRP1 Inhibitor WAY‐316606 Attenuates Osteoclastogenesis Through Dual Modulation of Canonical Wnt Signaling[J]. Journal of Bone and Mineral Research, 2020, 37(1): 152-166.
[3] Hawkshaw N J, Hardman J A, Haslam I S, et al. Identifying novel strategies for treating human hair loss disorders: cyclosporine A suppresses the Wnt inhibitor, SFRP1, in the dermal papilla of human scalp hair follicles[J]. PLoS biology, 2018, 16(5): e2003705.
[4] Donega V, van der Geest A T, Sluijs J A, et al. Single-cell profiling of human subventricular zone progenitors identifies SFRP1 as a target to re-activate progenitors[J]. Nature communications, 2022, 13(1): 1036.
[5] Gopinathan G, Foyle D, Luan X, et al. The Wnt antagonist SFRP1: a key regulator of periodontal mineral homeostasis[J]. Stem cells and development, 2019, 28(15): 1004-1014.
[6] Xing Z, Ni Y, Zhao J, et al. Hydrogen peroxide-induced secreted frizzled-related protein 1 gene demethylation contributes to hydrogen peroxide-induced apoptosis in human U251 glioma cells[J]. DNA and cell biology, 2017, 36(5): 347-353.
[7] Yao X, Kong L, Qiao Y, et al. Schwann cell-secreted frizzled-related protein 1 dictates neuroinflammation and peripheral nerve degeneration after neurotrauma[J]. Cell Reports Medicine, 2024, 5(11).
[8] Bodine P V N, Stauffer B, Ponce-de-Leon H, et al. A small molecule inhibitor of the Wnt antagonist secreted frizzled-related protein-1 stimulates bone formation[J]. Bone, 2009, 44(6): 1063-1068.
WAY 316606是一种强效分泌型卷曲相关蛋白1（sFRP-1）抑制剂，IC50值为0.5μM[1]。WAY 316606通过抑制sFRP-1活性调控Wnt信号通路激活，可作为关键调节剂影响破骨细胞生成和骨吸收过程[2]。WAY 316606在人毛囊器官模型中作为毛发促进剂诱导毛发生长[3]。
在体外，2μM的WAY 316606处理72小时可刺激人神经干细胞增殖并增强Wnt通路活性[4]。2μM的WAY 316606处理7天能显著促进牙周膜成纤维细胞矿化，上调矿化相关基因表达并改善矿物质稳态[5]。2μM的WAY 316606处理12小时可部分缓解H2O2（1mM，12小时）诱导的U251细胞生长抑制，减少细胞凋亡并提高细胞活力[6]。
在体内，小鼠神经横断后通过神经内注射WAY 316606（0.5μM/5μL；每3天一次；持续2周）可显著促进轴突再生[7]。雌性Sprague-Dawley大鼠单次静脉推注2mg/kg的WAY 316606后，WAY 316606表现出高血浆清除率（77mL/min/kg）[8]。
| Cell experiment [1]: | |
Cell lines | Mouse bone marrow-derived macrophage |
Preparation Method | Mouse bone marrow-derived macrophages were seeded (8 × 103 cells/well) and treated with Macrophage-colony stimulating factor (M-CSF) (30ng/mL) and receptor activator of nuclear factor-κB ligand (RANKL) (50ng/mL) for 5 days until osteoclasts matured. Indicated concentrations of WAY 316606 (0, 6.25, 12.5 and 25μM) were used to treat cells for another 5 days. After that, cells were removed from the surface of bovine slices. The resorption pits were captured using a scanning electron microscope, then ImageJ software was used to quantify the area of bone resorption. |
Reaction Conditions | 0, 6.25, 12.5 and 25μM; 5 days |
Applications | WAY 316606 significantly inhibited osteoclastogenesis induced by RANKL in a dose-dependent manner within mouse bone marrow-derived macrophage. |
| Animal experiment [2]: | |
Animal models | C57BL/6J mice |
Preparation Method | A complete transection injury was made at a distance of 5mm proximal to the trapezium of the sciatic nerve in C57BL/6J mice mice. After the injury, the nerve ends at the proximal and distal ends were reconnected using 6-0 sutures. After suturing the wound, the mice were returned to the cages. For sFRP1 inhibition treatment, WAY 316606 (0.5μM, 5μL) and LPS (15mg/kg) were injected into different mice via intraneural injection, and the control group mice received PBS injections. The nerve injections of WAY 316606 and PBS were repeated every 3 days for 2 weeks. After collecting the mice, they were killed with carbon dioxide, then their cervical dislocation was performed, and the sciatic nerve was cut with scissors for analysis. |
Dosage form | 0.5μM/5μL; every 3 days for 2 weeks; intraneural injection |
Applications | WAY 316606 treatment significantly promoted the axon regrowth of transected nerves in mice. |
References: | |
| Cas No. | 915759-45-4 | SDF | |
| 别名 | 5-(苯磺酰基)-N-(哌啶-4-基)-2-(三氟甲基)苯磺酰胺,WAY-316606;WAY316606 | ||
| 化学名 | 5-(benzenesulfonyl)-N-piperidin-4-yl-2-(trifluoromethyl)benzenesulfonamide | ||
| Canonical SMILES | C1CNCCC1NS(=O)(=O)C2=C(C=CC(=C2)S(=O)(=O)C3=CC=CC=C3)C(F)(F)F | ||
| 分子式 | C18H19F3N2O4S2 | 分子量 | 448.48 |
| 溶解度 | ≥ 44.8 mg/mL in DMSO with ultrasonic, ≥ 6.26 mg/mL in EtOH with ultrasonic and warming | 储存条件 | Store at -20°C |
| General tips | 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°C 储存时，请在 6 个月内使用，-20°C 储存时，请在 1 个月内使用。 为了提高溶解度，请将管子加热至37℃，然后在超声波浴中震荡一段时间。 |
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| Shipping Condition | 评估样品解决方案：配备蓝冰进行发货。所有其他可用尺寸：配备RT，或根据请求配备蓝冰。 | ||
| 制备储备液 | |||
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1 mg | 5 mg | 10 mg |
| 1 mM | 2.2298 mL | 11.1488 mL | 22.2975 mL |
| 5 mM | 446 μL | 2.2298 mL | 4.4595 mL |
| 10 mM | 223 μL | 1.1149 mL | 2.2298 mL |
| 第一步：请输入基本实验信息（考虑到实验过程中的损耗，建议多配一只动物的药量） | ||||||||||
| 给药剂量 | mg/kg |  |
动物平均体重 | g | |
每只动物给药体积 | ul | |
动物数量 | 只 |
| 第二步：请输入动物体内配方组成（配方适用于不溶于水的药物；不同批次药物配方比例不同，请联系GLPBIO为您提供正确的澄清溶液配方） | ||||||||||
| % DMSO % % Tween 80 % saline | ||||||||||
| 计算重置 | ||||||||||
计算结果:
工作液浓度： mg/ml；
DMSO母液配制方法： mg 药物溶于 μL DMSO溶液（母液浓度 mg/mL，
体内配方配制方法：取 μL DMSO母液，加入 μL PEG300，混匀澄清后加入μL Tween 80，混匀澄清后加入 μL saline，混匀澄清。
1. 首先保证母液是澄清的；
2.
一定要按照顺序依次将溶剂加入，进行下一步操作之前必须保证上一步操作得到的是澄清的溶液，可采用涡旋、超声或水浴加热等物理方法助溶。
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