FzM1
Based on 1 publication(s) in Google Scholar
FzM1 is a negative allosteric modulator (NAM) of Frizzled receptor FZD4. FzM1 reduces WNT5A-dependent WNT responsive element (WRE) activity (log EC50inh=?6.2). FzM1 binds to an allosteric binding site located in intracellular loop 3 (ICL3) of FZD4 and alters the conformation of the receptor, ultimately inhibiting the WNT/β-catenin cascade.
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- 純度: 98.72%
- CAS 番号: 1680196-54-6
- 分子式: C21H16N2O2S
- 分子量:360.43
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保管条件:Powder -20°C, 3 years ; In solvent -80°C, 6 months , -20°C, 1 month
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生物活性
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化学情報
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溶剤 & 溶解度
- 純度とドキュメンテーション
- 参考文献
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MedChemExpress（MCE）の使用を引用している文献 FzM1
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生物活性
In HEK293 cells (co-transfected with FZD4 and a WNT reporter construct), FzM1 acts as a negative allosteric regulator of FZD4, inhibiting the WNT/β-catenin pathway without increasing the activity of the WNT reporter construct[1]. In CaCo-2 cells, FzM1 (15 μM; 24 h, 48 h) resulted in decreased cell viability[1]. In HEK293 cells expressing FZD4, FzM1 acts as a negative allosteric regulator of FZD4 signaling initiated by WNT5A, reducing WNT5A-dependent WRE activity[1].
MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.
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Cell Line:HEK293 cells
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Concentration:15 μM
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Incubation Time:24 h, 48 h
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Result:Decreased the cell viability of HEK293 cells expressing FZD4.
Did not increase the activity of the WNT reporter construct, indicating its inhibitory effect on the WNT/β-catenin pathway.
MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.
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Animal Model:AGEs-RAGE-activated (intrahippocampal injection) rat model in Wistar rats (male, 6 weeks old)[1]
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Dosage:1 mg/kg/d
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Administration:Intraperitoneal injection, once daily, for 4 weeks
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Result:Reduced the levels of Aβ1-40 and Aβ1-42 in the hippocampus of rats.
Inhibited the increased expressions of Aβ metabolism-related proteins (RAGE, BACE1, and APP), pro-inflammatory cytokines (p-NF-κB, TNF-α, and IL-1β) induced by AGEs.
Upregulated the antioxidant defense system, with reduced levels of ROS and LPO, and increased content of GSH, and activities of SOD and GPx.
Also, alleviated the memory impairment of rats induced by AGEs, as shown by a significant decrease in the escape latency in the Morris water maze test.
化学情報
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CAS 番号 1680196-54-6
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性状 Solid
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分子量 360.43
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分子式 C21H16N2O2S
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Color White to light brown
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SMILES
O=C(NC1=CC2=CC=CC=C2C=C1)NC3=CC(O)=CC(C4=CC=CS4)=C3
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輸送条件
Room temperature in continental US; may vary elsewhere.
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保管条件
Powder -20°C 3 years In solvent -80°C 6 months -20°C 1 month
Publications (1)
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Journal Impact Factor
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Most Recent
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Res Sq
Spatial Transcriptomics and Dual Dye Mapping Identify Wnt-Driven BBB Protection in Endothelial EphA4-Deficiency. [Abstract]2026 Apr 9:rs.3.rs-9261231. PMID: 41994141
溶剤 & 溶解度
DMSO : 62.5 mg/mL (173.40 mM; Need ultrasonic; Hygroscopic DMSO has a significant impact on the solubility of product, please use newly opened DMSO)
Please refer to the solubility information to select the appropriate solvent. Once prepared, please aliquot and store the solution to prevent product inactivation from repeated freeze-thaw cycles.
Storage method and period of stock solution: -80°C, 6 months; -20°C, 1 month. When stored at -80°C, please use it within 6 months. When stored at -20°C, please use it within 1 month.
Please refer to the solubility information to select the appropriate solvent. Once prepared, please aliquot and store the solution to prevent product inactivation from repeated freeze-thaw cycles.
Storage method and period of stock solution: -80°C, 6 months; -20°C, 1 month. When stored at -80°C, please use it within 6 months. When stored at -20°C, please use it within 1 month.
濃度 (開始) × 体積 (開始) = 濃度 (終了) × 体積 (終了)
Select the appropriate dissolution method based on your experimental animal and administration route.
- For the following dissolution methods, please ensure to first prepare a clear stock solution using an In Vitro approach and then sequentially add co-solvents:
- To ensure reliable experimental results, the clarified stock solution can be appropriately stored based on storage conditions. As for the working solution for In Vivo experiments, it is recommended to prepare freshly and use it on the same day.
- The percentages shown for the solvents indicate their volumetric ratio in the final prepared solution. If precipitation or phase separation occurs during preparation, heat and/or sonication can be used to aid dissolution.
Add each solvent one by one: 10% DMSO 40% PEG300 5% Tween-80 45% Saline
Solubility: 2.08 mg/mL (5.77 mM); Suspended solution; Need ultrasonic
This protocol yields a suspended solution of 2.08 mg/mL. Suspended solution can be used for oral and intraperitoneal injection.
Taking 1 mL working solution as an example, add 100 μL DMSO stock solution (20.8 mg/mL) to 400 μL PEG300, and mix evenly; then add 50 μL Tween-80 and mix evenly; then add 450 μL Saline to adjust the volume to 1 mL.
Preparation of Saline: Dissolve 0.9 g sodium chloride in ddH₂O and dilute to 100 mL to obtain a clear Saline solution.
Add each solvent one by one: 10% DMSO 90% (20% SBE-β-CD in Saline)
Solubility: 2.08 mg/mL (5.77 mM); Suspended solution; Need ultrasonic
This protocol yields a suspended solution of 2.08 mg/mL. Suspended solution can be used for oral and intraperitoneal injection.
Taking 1 mL working solution as an example, add 100 μL DMSO stock solution (20.8 mg/mL) to 900 μL 20% SBE-β-CD in Saline, and mix evenly.
Preparation of 20% SBE-β-CD in Saline (4°C, storage for one week): 2 g SBE-β-CD powder is dissolved in 10 mL Saline, completely dissolve until clear.
Please enter the basic information of animal experiments:
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Recommended: Prepare an additional quantity of animals to account for potential losses during experiments.
Please enter your animal formula composition:
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%DMSO +
Recommended: Keep the proportion of DMSO in working solution below 2% if your animal is weak.
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%+
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+%Tween-80 + +
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%Saline +
The co-solvents required include: DMSO, . All of co-solvents are available by MedChemExpress (MCE). , Tween 80. All of co-solvents are available by MedChemExpress (MCE).
Working solution concentration: 0.22 mg/mL
Method for preparing stock solution: mg drug dissolved in μL DMSO. Stock solution concentration: mg/mL.
1. Take μL DMSO stock solution;
2. Add μL .
μL , mix evenly;
3. Then add μL Tween 80, mix evenly;
4. Then add μL
Please ensure that the stock solution in the first step is dissolved to a clear state, and add co-solvents in sequence. You can use ultrasonic heating (ultrasonic cleaner, recommended frequency 20-40 kHz), vortexing, etc. to assist dissolution.
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データシート (276 KB)
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取扱説明書 (2659 KB)
参考文献
[1]. Gennaro Riccio, et al. A Negative Allosteric Modulator of WNT Receptor Frizzled 4 Switches into an Allosteric Agonist. Biochemistry. 2018 Feb 6;57(5):839-851. [Content Brief]
[2]. Hong Y, et al. Effects of RAGE-Specific Inhibitor FPS-ZM1 on Amyloid-β Metabolism and AGEs-Induced Inflammation and Oxidative Stress in Rat Hippocampus. Neurochem Res. 2016 May;41(5):1192-9. [Content Brief]
Complete Stock Solution Preparation Table
Please refer to the solubility information to select the appropriate solvent. Once prepared, please aliquot and store the solution to prevent product inactivation from repeated freeze-thaw cycles.
Storage method and period of stock solution: -80°C, 6 months; -20°C, 1 month. When stored at -80°C, please use it within 6 months. When stored at -20°C, please use it within 1 month.
| Optional Solvent | Concentration Solvent Mass | 1 mg | 5 mg | 10 mg | 25 mg |
|---|---|---|---|---|---|
| DMSO | 1 mM | 2.7745 mL | 13.8723 mL | 27.7446 mL | 69.3616 mL |
| 5 mM | 0.5549 mL | 2.7745 mL | 5.5489 mL | 13.8723 mL | |
| 10 mM | 0.2774 mL | 1.3872 mL | 2.7745 mL | 6.9362 mL | |
| 15 mM | 0.1850 mL | 0.9248 mL | 1.8496 mL | 4.6241 mL | |
| 20 mM | 0.1387 mL | 0.6936 mL | 1.3872 mL | 3.4681 mL | |
| 25 mM | 0.1110 mL | 0.5549 mL | 1.1098 mL | 2.7745 mL | |
| 30 mM | 0.0925 mL | 0.4624 mL | 0.9248 mL | 2.3121 mL | |
| 40 mM | 0.0694 mL | 0.3468 mL | 0.6936 mL | 1.7340 mL | |
| 50 mM | 0.0555 mL | 0.2774 mL | 0.5549 mL | 1.3872 mL | |
| 60 mM | 0.0462 mL | 0.2312 mL | 0.4624 mL | 1.1560 mL | |
| 80 mM | 0.0347 mL | 0.1734 mL | 0.3468 mL | 0.8670 mL | |
| 100 mM | 0.0277 mL | 0.1387 mL | 0.2774 mL | 0.6936 mL |
FzM1 関連分類
HY-116553 関連分類
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