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Enpatoran

CAT: 0804-HY-134581-01Size: 1 mgDry Ice: NoHazardous: No
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CAT#:0804-HY-134581-01Size:1 mg
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Description
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].
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.