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Ertiprotafib

Name: Ertiprotafib
Brand: TargetMol
SKU: T15243
Price: 84 USD
Availability: InStock
Rating: 5 (10 reviews)

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Catalog No. T15243Cas No. 251303-04-5

Alias PTP-112, PTP112, PTP 112

Ertiprotafib (PTP 112), a selective and potent inhibitor of protein tyrosine phosphate 1B (PTP1B) and IkappaB kinase β (IKK-β), is a novel insulin sensitizer with potential anticancer activity for the study of type 2 diabetes and breast cancer.

Ertiprotafib

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Purity: 98.70%

Catalog No. T15243Alias PTP-112, PTP112, PTP 112Cas No. 251303-04-5

Pack Size	Price	USA Warehouse	Global Warehouse
1 mg	$84	In Stock	In Stock
5 mg	$198	In Stock	In Stock
10 mg	$347	In Stock	In Stock
25 mg	$668	In Stock	In Stock
50 mg	$987	In Stock	In Stock
100 mg	$1,330	In Stock	In Stock

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In Stock Estimated shipping dateUSA Warehouse[1-2 days] Global Warehouse[5-7 days]

This molecule is a custom-made product. TargetMol has an excellent synthesis team with the experience and capability to provide you with cost-effective products.If you have any questions, please feel free to contact us. We are committed to serving you wholeheartedly.

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:98.70%

ee:100%

Appearance:Solid

Color:Yellow

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COA CSFC HNMR LCMS ORP

Product Introduction

Bioactivity

Description	Ertiprotafib (PTP 112), a selective and potent inhibitor of protein tyrosine phosphate 1B (PTP1B) and IkappaB kinase β (IKK-β), is a novel insulin sensitizer with potential anticancer activity for the study of type 2 diabetes and breast cancer.
Targets&IC50	PPARβ:~1 μM (EC50), PPARα:~1 μM (EC50), PTP1B:1.6 μM, IKKβ:400 nM
In vitro	METHODS: To measure the kinase activity of IKK-b, ertiprotafib was used in doses (0.001-1 μM) and a peptide substrate containing the IjB phosphorylation motif was used, and the phosphorylated peptide product was determined using an ELISA-type assay with time-resolved fluorescence (TRF) measurements. RESULTS: Ertiprotafib is a potent IKK-b inhibitor with an IC50 value of 400 ± 40 nM, which is well below the value required for half-maximal inhibition of PTP1B p-nitrophenyl phosphatase activity. The reported IC50 values of ertiprotafib for PTP1B range from 1.6 to 29 μM, depending on the assay conditions. [1]
In vivo	METHODS: Here, 11-week-old leptin-deficient male ob/ob mice were administered Ertiprotafib (25 mg/kg, daily, for 4 days), and changes in blood glucose indicators were observed. RESULTS: Mice treated with ertiprotafib had fasting blood glucose levels returned to the normal range, along with a significant decrease in insulin levels and a significant decrease in serum triglyceride levels. [2]
Synonyms	PTP-112, PTP112, PTP 112

Chemical Properties

Molecular Weight	559.51
Formula	C₃₁H₂₇BrO₃S
Cas No.	251303-04-5
Smiles	CC=1C2=C(C=3C(C(Br)=C2SC1C)=CC=CC3)C4=CC(C)=C(O[C@H](CC5=CC=CC=C5)C(O)=O)C(C)=C4
Relative Density.	1.376 g/cm3 (Predicted)

Storage & Solubility Information

Storage

keep away from moisture,store under nitrogen,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: 80 mg/mL (142.98 mM), Sonication is recommended.

In Vivo Formulation

10% DMSO+90% Corn Oil: 3.3 mg/mL (5.9 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	1.7873 mL	8.9364 mL	17.8728 mL	89.3639 mL
5 mM	0.3575 mL	1.7873 mL	3.5746 mL	17.8728 mL
10 mM	0.1787 mL	0.8936 mL	1.7873 mL	8.9364 mL
20 mM	0.0894 mL	0.4468 mL	0.8936 mL	4.4682 mL
50 mM	0.0357 mL	0.1787 mL	0.3575 mL	1.7873 mL
100 mM	0.0179 mL	0.0894 mL	0.1787 mL	0.8936 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