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L524-0366

Name: L524-0366
Brand: TargetMol
SKU: T8570
Price: 113 USD
Availability: InStock
Rating: 5 (10 reviews)

(Synonyms: [1-(3-chlorophenyl)triazol-4-yl]-thiomorpholino-methanone) Copy Product Info

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Synonyms: [1-(3-chlorophenyl)triazol-4-yl]-thiomorpholino-methanone

Catalog No. T8570 Copy Product Info

Purity: 99.13%

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L524-0366 is a selective Fn14 receptor antagonist that exerts its effects through competitive binding to the Fn14 receptor. L524-0366 specifically binds to the Fn14 receptor surface, with a KD of 7.12 μM. At a concentration of 10 μM, L524-0366 completely inhibits TWEAK-induced glial cell migration and exhibits no cytotoxicity at concentrations below 50 μM. L524-0366 possesses antitumor and anti-inflammatory activity and is widely used in research on diseases such as cancer.

Cas No. 951612-19-4

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Pack Size	Price	USA Stock	Global Stock
1 mg	$113	In Stock	-
5 mg	$247	In Stock	-
10 mg	$378	In Stock	-
25 mg	$653	In Stock	-
50 mg	$892	In Stock	-
100 mg	$1,180	In Stock	-

For In stock only · Estimated delivery: USA Stock (1-2 days) Global Stock (5-7 days)

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For research use only—not for human use. No sales to individuals. Use as intended only.

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Purity:99.13%

Appearance:Solid

Color:White

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COA HNMR LCMS

Product Introduction

Bioactivity

Description	L524-0366 is a selective Fn14 receptor antagonist that exerts its effects through competitive binding to the Fn14 receptor. L524-0366 specifically binds to the Fn14 receptor surface, with a KD of 7.12 μM. At a concentration of 10 μM, L524-0366 completely inhibits TWEAK-induced glial cell migration and exhibits no cytotoxicity at concentrations below 50 μM. L524-0366 possesses antitumor and anti-inflammatory activity and is widely used in research on diseases such as cancer.
Targets & IC50	sTWEAK:7.8 µM
In vitro	L524-0366 mitigated maladaptive remodeling with TAC. TWEAK induced secretion of the pro-inflammatory chemokine, monocyte chemoattractant protein 1 from WT but not Fn14-/-?fibroblasts in vitro, in part through activation of non-canonical NF-κB signaling. Finally, Fn14 expression was increased in mouse following TAC and in human failing hearts.
In vivo	Methods: Aortic stenosis surgery was performed on 8- to 12-week-old wild-type (WT) and Fn14 knockout mice to induce chronic pressure overload. Starting 3 days post-surgery, daily intraperitoneal injections of the Fn14 antagonist L524-0366 (9 mg/kg/day, dissolved in corn oil) were administered until 6 weeks post-surgery. Results: L524-0366 treatment significantly improved TAC-induced cardiac dysfunction, reduced cardiac fibrosis, and decreased macrophage infiltration. [1]
Synonyms	[1-(3-chlorophenyl)triazol-4-yl]-thiomorpholino-methanone
Cell Research	Wild type (WT) and Fn14 knock out (Fn14-/-) mice were subjected to pressure overload [transaortic constriction (TAC)] for 1 or 6 weeks. A subset of WT TAC animals were treated with the Fn14 antagonist L524-0366. Cardiac function was measured by echocardiography. Cardiac fibrosis and macrophage infiltration were quantified using immunohistochemistry and flow cytometry, respectively. Cardiac fibroblasts were isolated for quantifying TWEAK-induced chemokine release.

Chemical Properties

Molecular Weight	308.79
Formula	C₁₃H₁₃ClN₄OS
Cas No.	951612-19-4
Smiles	C(=O)(C1=CN(N=N1)C2=CC(Cl)=CC=C2)N3CCSCC3
Relative Density.	no data available

Storage & Solubility Information

Storage

Keep away from direct sunlight Powder: -20°C for 3 years | In solvent: -80°C for 1 year Shipping with blue ice/Shipping at ambient temperature.

Solubility Information

DMSO: 25 mg/mL (80.96 mM), Sonication is recommended.

In Vivo Formulation

5% DMSO+95% Corn oil: 1 mg/mL (3.24 mM), Suspension.

Please add the solvents sequentially, clarifying the solution as much as possible before adding the next one. Dissolve by heating and/or sonication if necessary. Working solution is recommended to be prepared and used immediately. The formulation provided above is for reference purposes only. In vivo formulations may vary and should be modified based on specific experimental conditions.

Solution Preparation Table

DMSO

	1mg	5mg	10mg	50mg
1 mM	3.2384 mL	16.1922 mL	32.3845 mL	161.9223 mL
5 mM	0.6477 mL	3.2384 mL	6.4769 mL	32.3845 mL
10 mM	0.3238 mL	1.6192 mL	3.2384 mL	16.1922 mL
20 mM	0.1619 mL	0.8096 mL	1.6192 mL	8.0961 mL
50 mM	0.0648 mL	0.3238 mL	0.6477 mL	3.2384 mL

Note : The dilution table applies only to solid products. For liquid products, please calculate the stock solution based on the stated concentration and/or density.

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In Vivo Formulation Calculator (Clear solution)

Please enter your animal experiment information in the following box and click Calculate to obtain the stock solution preparation method and in vivo formula preparation method:

For example, if the intended dosage is 10 mg/kg for animals weighing 20 g , with a dosing volume of 100 μL per animal, TargetMol | Animal experiments

and a total of 10 animals are to be administered, using a formulation of TargetMol | reagent

10% DMSO+ 40% PEG300+ 5% Tween 80+ 45% Saline/PBS/ddH₂O , the resulting working solution concentration would be 2 mg/mL.

Stock Solution Preparation:

Dissolve 2 mg of the compound in 100 μL DMSO TargetMol | reagent to obtain a stock solution at a concentration of 20 mg/mL . If the required concentration exceeds the compound's known solubility, please contact us for technical support before proceeding.

Preparation of the In Vivo Formulation:

1) Add 100 μL of the DMSO TargetMol | reagent stock solution to 400 µL PEG300 and mix thoroughly until the solution becomes clear.

2) Add 50 µL Tween 80 and mix well until fully clarified.

3) Add 450 µL Saline,PBS or ddH₂O TargetMol | reagent and mix thoroughly until a homogeneous solution is obtained.

This example is provided solely to demonstrate the use of the In Vivo Formulation Calculator and does not constitute a recommended formulation for any specific compound. Please select an appropriate dissolution and formulation strategy based on your experimental model and route of administration.

All co-solvents required for this protocol, includingDMSO, PEG300/PEG400, Tween 80, SBE-β-CD, and Corn oil, are available for purchase on the TargetMol website.

Dose Conversion

You can also refer to dose conversion for different animals. More Dose Conversion

Tech Support

Please see Inhibitor Handling Instructions for more frequently ask questions. Topics include: how to prepare stock solutions, how to store products, and cautions on cell-based assays & animal experiments, etc