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Enpatoran

Catalog No. T9570 CAS 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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Enpatoran, CAS 2101938-42-3

Pack Size	Availability	Price/USD
1 mg	In stock	$ 122.00
5 mg	In stock	$ 247.00
10 mg	In stock	$ 372.00
25 mg	In stock	$ 638.00
50 mg	In stock	$ 955.00
100 mg	In stock	$ 1,390.00
200 mg	In stock	$ 1,980.00
1 mL * 10 mM (in DMSO)	In stock	$ 289.00

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Purity: 99.38%

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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	TLR8:24.1 nM, 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].

Molecular Weight	320.31
Formula	C16H15F3N4
CAS No.	2101938-42-3

Storage

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

Solubility Information

DMSO: 24.44 mg/mL (76.30 mM)

References and Literature

1. Jaromir Vlach, et al. Discovery of M5049: A Novel Selective TLR7/8 Inhibitor for Treatment of Autoimmunity. J Pharmacol Exp Ther. 2020 Dec 16;JPET-AR-2020-000275.

Related compound libraries

This product is contained In the following compound libraries：

Membrane Protein-targeted Compound Library Inhibitor Library Drug Repurposing Compound Library Orally Active Compound Library Immunology/Inflammation Compound Library Bioactive Compounds Library Max Bioactive Compound Library Clinical Compound Library Pyroptosis Compound Library

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RS 09 Toll-like receptor modulator 3M-011 Schaftoside CU-CPT9b MD2-IN-1 MD2-TLR4-IN-1 VB 201

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Keywords

Enpatoran 2101938-42-3 Immunology/Inflammation TLR inhibit M5049 Inhibitor Toll-like Receptor (TLR) M-5049 autoimmunity M 5049 TLR7/8 selective inhibitor

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