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Enpatoran

Name: Enpatoran
Brand: TargetMol
SKU: T9570
Price: 122 USD
Availability: InStock
Rating: 5 (10 reviews)

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Catalog No. T9570Cas No. 2101938-42-3

Enpatoran is an inhibitor of TLR7(IC50 = 11.1 nM) and TLR8(IC50 = 24.1 nM). Enpatoran was found to be inactive against TLR3, TLR4, and TLR9 in vitro and in vivo.

Enpatoran

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Purity: 99.38%

Catalog No. T9570Cas No. 2101938-42-3

Enpatoran is an inhibitor of TLR7(IC50 = 11.1 nM) and TLR8(IC50 = 24.1 nM). Enpatoran was found to be inactive against TLR3, TLR4, and TLR9 in vitro and in vivo.

Pack Size	Price	USA Warehouse	Global Warehouse
1 mg	$122	In Stock	In Stock
5 mg	$247	In Stock	In Stock
10 mg	$372	In Stock	In Stock
25 mg	$613	In Stock	In Stock
50 mg	$869	In Stock	In Stock
100 mg	$1,170	In Stock	In Stock
200 mg	$1,570	In Stock	In Stock
1 mL x 10 mM (in DMSO)	$173	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:99.38%

Appearance:Solid

Color:Yellow

Resource Download

COA HPLC HNMR

Product Introduction

Bioactivity

Description	Enpatoran is an inhibitor of TLR7(IC50 = 11.1 nM) and TLR8(IC50 = 24.1 nM). Enpatoran was found to be inactive against TLR3, TLR4, and TLR9 in vitro and in vivo.
Targets&IC50	TLR8:620 nM (in peripheral blood mononuclear cells (PBMCs)), TLR7:2.2 nM (in whole blood (WB) cells), TLR7:68.3 nM (in peripheral blood mononuclear cells (PBMCs)), TLR8:24.1 nM, TLR8:120 nM (in whole blood (WB) cells), TLR7:11.1 nM
In vitro	Enpatoran inhibited activity against different TLRs in a variety of cellular systems. Enpatoran potently inhibited TLR7 and TLR8 in HEK NF-κB-luciferase reporter cells with IC50 values in the low nanomolar range. Additionally, Enpatoran was found to be potent against TLR7 and TLR8 in PBMCs as well as whole blood. There appears to be an increased selectivity for TLR7 inhibition relative to TLR8 for Enpatoran in whole blood compared with PBMCs and transfected HEK cells[1].
In vivo	In the BXSB-Yaa model, there is a robust increase in multiple autoantibodies, and Enpatoran significantly reduced both DNA-containing reactivities such as anti-dsDNA and anti-histones, as well as RNA-binding protein reactivities such as anti-RiboP and anti-SmRNP. At high dosages of Enpatoran, the effect on autoantibodies is so profound that titers are reduced below the baseline levels[1].

Chemical Properties

Molecular Weight	320.31
Formula	C₁₆H₁₅F₃N₄
Cas No.	2101938-42-3
Smiles	N[C@@H]1C[C@@H](CN(C1)c1ccc(C#N)c2ncccc12)C(F)(F)F
Relative Density.	1.37 g/cm3 (Predicted)

Storage & Solubility Information

Storage

store at low temperature | Powder: -20°C for 3 years | In solvent: -80°C for 1 year | Shipping with blue ice/Shipping at ambient temperature.

Solubility Information

DMSO: 83.33 mg/mL (260.15 mM), Sonication is recommended.

In Vivo Formulation

10% DMSO+40% PEG300+5% Tween 80+45% Saline: 2 mg/mL (6.24 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	3.1220 mL	15.6099 mL	31.2198 mL	156.0988 mL
5 mM	0.6244 mL	3.1220 mL	6.2440 mL	31.2198 mL
10 mM	0.3122 mL	1.5610 mL	3.1220 mL	15.6099 mL
20 mM	0.1561 mL	0.7805 mL	1.5610 mL	7.8049 mL
50 mM	0.0624 mL	0.3122 mL	0.6244 mL	3.1220 mL
100 mM	0.0312 mL	0.1561 mL	0.3122 mL	1.5610 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