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Enpatoran

Enpatoran (M5049) is a potent, orally active and dual TLR7/8 inhibitor with IC50s of 11.1 nM and 24.1 nM in HEK293 cells, respectively. Enpatoran is inactive against TLR3, TLR4 and TLR9. Enpatoran can block molecule synthetic ligands and natural endogenous RNA ligands. Enpatoran exhibits excellent pharmacokinetic properties in vivo. Enpatoran can be used for both innate and adaptive autoimmunity blocking research [1].

Product Specifications

CAS Number

2101938-42-3

Product Name Alternative

M5049

UNSPSC

12352005

Target

Toll-like Receptor (TLR)

Type

Reference compound

Related Pathways

Immunology/Inflammation

Applications

COVID-19-immunoregulation

Field of Research

Inflammation/Immunology

Assay Protocol

https://www.medchemexpress.com/enpatoran.html

Purity

99.80

Solubility

DMSO : 24.44 mg/mL (ultrasonic) |Ethanol : 100 mg/mL (ultrasonic)

Smiles

N#CC(C=C1)=C(N=CC=C2)C2=C1N3C[C@@H](C(F)(F)F)C[C@@H](N)C3

Molecular Formula

C16H15F3N4

Molecular Weight

320.31

References & Citations

[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.

Shipping Conditions

Blue Ice

Storage Conditions

-20°C (Powder, sealed storage, away from moisture and light)

Scientific Category

Reference compound1

Clinical Information

Phase 2

Isoform

TLR7; TLR8

Citation 01

Biomed Pharmacother. 2025 Sep 17:192:118569.|bioRxiv. 2024 Jul 15:2024.07.15.603540.|bioRxiv. 2024 July 25.|Br J Pharmacol. 2024 Oct;181 (19) :3760-3778.|Cell Commun Signal. 2023 Aug 18;21 (1) :215.|Cell Commun Signal. 2024 Nov 8;22 (1) :536.|Int Immunopharmacol. 2025 May 14:158:114804.|J Autoimmun. 2024 May:145:103189.|J Innate Immun. 2023;15 (1) :517-530.|J Periodontal Res. 2025 Feb 25.|Patent. US20250312471A1.|J Extracell Vesicles. 2025 Jul;14 (7) :e70134.

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