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Enpatoran

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Purity:99.38%

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COA HNMR HPLC

Enpatoran

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.

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Pack Size	Price	Availability
1 mg	$122	In Stock
5 mg	$247	In Stock
10 mg	$372	In Stock
25 mg	$638	In Stock
50 mg	$955	In Stock
100 mg	$1,390	In Stock
200 mg	$1,980	In Stock
1 mL x 10 mM (in DMSO)	$289	In Stock

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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.
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

Storage & Solubility Information

Storage

Powder: -20°C for 3 years | In solvent: -80°C for 1 year

Solubility Information

DMSO: 24.44 mg/mL (76.30 mM)

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

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In Vivo Formulation Calculator (Clear solution)

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Mother liquor preparation method: 2 mg of drug dissolved in 50 μL DMSO TargetMol | reagent

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Preparation method for in vivo formula: Take 50 μL DMSO TargetMol | reagent

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mix well and clarify, then add 50 more μL Tween 80, mix well and clarify, then add 600 more μLddH2O TargetMol | reagent

mix well and clarify

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