FzM1 - CAS:1680196-54-6

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FzM1

目录号 : KCM11915 CAS No. : 1680196-54-6 纯度 : ≥95%

Data Sheet 产品使用指南

Wnt signaling proteins are small secreted proteins that are active in embryonic development, tissue homeostasis, and tumorigenesis. Wnt proteins initiate cell signaling by binding Frizzled (Fz) receptors, a family of G protein-coupled receptors. FzM1 is an allosteric ligand of Fz4. At 10 µM, it inhibits nuclear translocation of β-catenin in U87MG glioma cells treated with lithium chloride, a GSK3 inhibitor that enhances the Wnt canonical signaling pathway. FzM1 impairs the ability of U87MG cells to form neurospheres in culture and stimulates the differentiation of Caco-2 epithelial colorectal adenocarcinoma cells.

规格	价格	是否有货	数量
1mg		In-stock
5mg		In-stock
10mg		In-stock
10 mM * 1 mL in DMSO		In-stock

加入购物车大包装询价

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1H-Pyrazole-4-carboxamide, 5-methyl-1-phenyl-N-2-quinolinyl- In-stock
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PRI-724 In-stock
SRI 37892 In-stock

KKL Med 的所有产品和服务仅用于科学研究，不能被用于人体，兽医，我们也不向个人提供产品和服务。

生物活性

FzM1 is a negative allosteric modulator (NAM) of Frizzled receptor FZD4. FzM1 reduces WNT5A-dependent WNT responsive element (WRE) activity (log EC_50inh= 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.

体外研究

In HEK293 cells (transfected with both FZD4 and WNT reporter gene constructs), FzM1 acts as a negative sex conformation regulator of FZD4, inhibiting the WNT/β - catenin pathway without increasing the activity of WNT reporter gene constructs.
FzM1 (15 μM; 24 h, 48 h) resulted in a decrease in cell survival rate in CaCo-2 cell experiments.
In HEK293 cell experiments expressing FZD4, FzM1 acts as a negative sex structure modulator of FZD4 signaling triggered by WNT5A, reducing WNT5A dependent WRE activity.

Cell Viability Assay

Cell Line:	HEK293 cells
Concentration:	15 μM
Incubation Time:	24 hours, 48 hours
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.

体内研究

FPS-ZM1 (1 mg/kg/d; intraperitoneal injection; Once a day; In the AGEs RAGE activation model of Wistar rats at 4 weeks, the production of A β 1-40 and A β 1-42 in the hippocampus was reduced, the increase of A β metabolism related proteins (RAGE, BACE1, and APP) was inhibited, the expression of pro-inflammatory cytokines (p-NF - κ B, TNF - α, and IL-1 β) was downregulated, the antioxidant defense system was upregulated (reducing ROS and LPO levels, increasing GSH content, SOD and GPx activity), and AGEs induced memory damage in rats was alleviated.

Animal Model:	AGEs-RAGE-activated (intrahippocampal injection) rat model in Wistar rats (male, 6 weeks old)
Dosage:	1 mg/kg/d
Administration:	Intraperitoneal injection, once daily, for 4 weeks
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.

分子式

C₂₁H₁₆N₂O₂S

分子量

360.43

CAS号

1680196-54-6

运输条件

Room temperature in continental US; may vary elsewhere.

储存方式

Powder	-20°C	3 years
In solvent	-80°C	6 months
	-20°C	1 month

溶解性数据

In Vitro:

DMSO : 62.5 mg/mL (173.40 mM; Need ultrasonic)

配制储备液

浓度溶剂体积质量	1 mg	5 mg	10 mg

1 mM	2.7745 mL	13.8723 mL	27.7446 mL
5 mM	0.5549 mL	2.7745 mL	5.5489 mL
10 mM	0.2774 mL	1.3872 mL	2.7745 mL

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, 6 months; -20°C, 1 month。-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。

In Vivo:

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 → 40% PEG300 → 5% Tween-80 → 45% saline

Solubility: 2.08 mg/mL (5.77 mM); Suspended solution; Need ultrasonic

此方案可获得 2.08 mg/mL (5.77 mM) 的均匀悬浊液，悬浊液可⽤于⼝服和腹腔注射。

以 1 mL 工作液为例，取 100 μL 20.8 mg/mL 的澄清 DMSO 储备液加到 400 μL PEG300 中，混合均匀；向上述体系中加入50 μL Tween-80，混合均匀；然后继续加入 450 μL生理盐水定容至 1 mL。
2.

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

Solubility: 2.08 mg/mL (5.77 mM); Suspended solution; Need ultrasonic

此方案可获得 2.08 mg/mL (5.77 mM) 的均匀悬浊液，悬浊液可⽤于⼝服和腹腔注射。

以 1 mL 工作液为例，取 100 μL 20.8 mg/mL 的澄清 DMSO 储备液加到 900 μL 20% 的 SBE-β-CD ⽣理盐⽔⽔溶液中，混合均匀。