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TGF-β1/Smad3-IN-1

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Catalog No. T209680Cas No. 3043687-96-0

TGF-β1/Smad3-IN-1 (Compound 5aa) is an orally administrable dual inhibitor of TGF-β1/Smad3 with anti-fibrotic activity and can be used for the study of idiopathic pulmonary fibrosis (IPF).

TGF-β1/Smad3-IN-1

TGF-β1/Smad3-IN-1

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Purity: 99.83%
Catalog No. T209680Cas No. 3043687-96-0
TGF-β1/Smad3-IN-1 (Compound 5aa) is an orally administrable dual inhibitor of TGF-β1/Smad3 with anti-fibrotic activity and can be used for the study of idiopathic pulmonary fibrosis (IPF).
Pack SizePriceUSA WarehouseGlobal WarehouseQuantity
1 mg$98-In Stock
5 mg$255-In Stock
10 mg$413-In Stock
25 mg$853-In Stock
50 mg$1,360-In Stock
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In Stock Estimated shipping dateUSA Warehouse[1-2 days] Global Warehouse[5-7 days]
All TargetMol products are for research purposes only and cannot be used for human consumption. We do not provide products or services to individuals. Please comply with the intended use and do not use TargetMol products for any other purpose.
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Purity:99.83%
Appearance:Solid
Color:Yellow
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Product Introduction

Bioactivity
Description
TGF-β1/Smad3-IN-1 (Compound 5aa) is an orally administrable dual inhibitor of TGF-β1/Smad3 with anti-fibrotic activity and can be used for the study of idiopathic pulmonary fibrosis (IPF).
In vitro
TGF-β1/Smad3-IN-1 (100-500 nM; 48 h) induced a decrease in TGF-β1 levels in H2228 cells [1].
TGF-β1/Smad3-IN-1 (2-6 μM; 24 h) dose-dependently inhibited p-Smad3 and α-SMA expression, significantly suppressing NIH3T3 cell migration[1].
TGF-β1/Smad3-IN-1 (3-10 μM; 72 h) increased Cleave-caspase3 expression in NIH3T3 cells and induced apoptosis in a dose-dependent manner [1].
In vivo
TGF-β1/Smad3-IN-1 (p.o.; 100 mg/kg/day; days 2–20) treated a bleomycin-induced mouse model of pulmonary fibrosis, suppressing bleomycin-induced expression of pulmonary TGFβ1 and HYP, reducing extracellular matrix deposition, and alleviating pulmonary fibrosis [1].
Chemical Properties
Molecular Weight578.68
FormulaC30H34N4O6S
Cas No.3043687-96-0
SmilesCCS(O)(=O)=O.COC(C1=CC=C2C(NC(/C2=C(C3=CC=CC=C3)\NC4=CC=C(N5CCN(CC5)C)C=C4)=O)=C1)=O
Storage & Solubility Information
StoragePowder: -20°C for 3 years | In solvent: -80°C for 1 year | Shipping with blue ice/Shipping at ambient temperature.
Solubility Information
DMSO: 80.00 mg/mL (138.25 mM), Sonication is recommended.
Solution Preparation Table
DMSO
1mg5mg10mg50mg
1 mM1.7281 mL8.6404 mL17.2807 mL86.4035 mL
5 mM0.3456 mL1.7281 mL3.4561 mL17.2807 mL
10 mM0.1728 mL0.8640 mL1.7281 mL8.6404 mL
20 mM0.0864 mL0.4320 mL0.8640 mL4.3202 mL
50 mM0.0346 mL0.1728 mL0.3456 mL1.7281 mL
100 mM0.0173 mL0.0864 mL0.1728 mL0.8640 mL

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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:
TargetMol | Animal experiments 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 DMSOTargetMol | 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 DMSOTargetMol | reagent stock solution to 400 μL PEG300TargetMol | reagent 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 ddH2OTargetMol | 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.
1 Enter information below:
mg/kg
g
μL
2 Enter the in vivo formulation:
% DMSO
%
% Tween 80
% Saline/PBS/ddH2O

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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
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