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Bexotegrast

Name: Bexotegrast
Brand: TargetMol
SKU: T39933
Price: 64 USD
Availability: InStock
Rating: 5 (10 reviews)

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Catalog No. T39933Cas No. 2376257-44-0

Alias PLN-74809

Bexotegrast (PLN-74809) is an orally active and potent inhibitor of αvβ6 and αvβ1 integrins with antifibrotic effects, inhibiting αvβ6 and αvβ1-induced activation of TGF-β. It is applicable for studies of idiopathic pulmonary fibrosis (IPF) and non-specific interstitial pneumonia (NSIP).

Bexotegrast

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Purity: 99.53%

Catalog No. T39933Alias PLN-74809Cas No. 2376257-44-0

Pack Size	Price	USA Warehouse	Global Warehouse
1 mg	$64	In Stock	In Stock
5 mg	$156	In Stock	In Stock
10 mg	$247	-	In Stock
25 mg	$397	-	In Stock
50 mg	$589	-	In Stock
1 mL x 10 mM (in DMSO)	$169	-	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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Batch Information

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Purity:99.53%

Appearance:Solid

Color:White

Resource Download

COA HPLC HNMR

Product Introduction

Bioactivity

Description	Bexotegrast (PLN-74809) is an orally active and potent inhibitor of αvβ6 and αvβ1 integrins with antifibrotic effects, inhibiting αvβ6 and αvβ1-induced activation of TGF-β. It is applicable for studies of idiopathic pulmonary fibrosis (IPF) and non-specific interstitial pneumonia (NSIP).
Targets&IC50	αvβ1 integrin:3.4 nM (Kd), αvβ6 integrin:5.7 nM (Kd)
In vitro	Bexotegrast (PLN-74809; 1.82 µM; incubation for 7 days) inhibits lung collagen deposition and Smad3 phosphorylation in a dose-dependent manner[2].
In vivo	Bexotegrast（PLN-74809；100–500 mg/kg), administered orally to mice 7 to 21 days after bleomycin-induced lung injury, dose-dependently reduces interstitial fibrotic collagen deposition caused by bleomycin and blocks Smad3 phosphorylation [2].
Synonyms	PLN-74809

Chemical Properties

Molecular Weight	492.61
Formula	C₂₇H₃₆N₆O₃
Cas No.	2376257-44-0
Smiles	N([C@@H](CCN(CCCCC=1NC=2C(=CC1)CCCN2)CCOC)C(O)=O)C=3C4=C(N=CN3)C=CC=C4

Storage & Solubility Information

Storage

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

Solubility Information

DMSO: 100 mg/mL (203 mM), Sonication is recommended.

In Vivo Formulation

10% DMSO+40% PEG300+5% Tween 80+45% Saline: 4 mg/mL (8.12 mM), Sonication is recommended.

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	2.0300 mL	10.1500 mL	20.3000 mL	101.5002 mL
5 mM	0.4060 mL	2.0300 mL	4.0600 mL	20.3000 mL
10 mM	0.2030 mL	1.0150 mL	2.0300 mL	10.1500 mL
20 mM	0.1015 mL	0.5075 mL	1.0150 mL	5.0750 mL
50 mM	0.0406 mL	0.2030 mL	0.4060 mL	2.0300 mL
100 mM	0.0203 mL	0.1015 mL	0.2030 mL	1.0150 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:

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