1. Immunology/Inflammation
  2. Toll-like Receptor (TLR)
  3. Enpatoran

Enpatoran (Synonyms: M5049)

Cat. No.: HY-134581
Handling Instructions

Enpatoran (M5049) is an orally active and dual TLR7/8 inhibitor with IC50s of 11.1 nM and 24.1 nM in HEK293 cells, respectively. Enpatoran can block both innate and adaptive autoimmunity. Enpatoran is inactive against TLR3, TLR4 and TLR9. Enpatoran (M5049) can block molecule synthetic ligands and natural endogenous RNA ligands. Enpatoran (M5049) inhibits cytokine release, causing great potency in pharmacokinetic/pharmacodynamic properties.

For research use only. We do not sell to patients.

Enpatoran Chemical Structure

Enpatoran Chemical Structure

CAS No. : 2101938-42-3

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Description

Enpatoran (M5049) is an orally active and dual TLR7/8 inhibitor with IC50s of 11.1 nM and 24.1 nM in HEK293 cells, respectively. Enpatoran can block both innate and adaptive autoimmunity. Enpatoran is inactive against TLR3, TLR4 and TLR9. Enpatoran (M5049) can block molecule synthetic ligands and natural endogenous RNA ligands. Enpatoran (M5049) inhibits cytokine release, causing great potency in pharmacokinetic/pharmacodynamic properties[1].

IC50 & Target[1]

TLR7

11.1 nM (IC50, in HEK293 cells)

TLR8

24.1 nM (IC50, in HEK293 cells)

TLR7

68.3 nM (IC50, in peripheral blood mononuclear cells (PBMCs))

TLR8

620 nM (IC50, in peripheral blood mononuclear cells (PBMCs))

TLR7

2.2 nM (IC50, in whole blood (WB) cells)

TLR8

120 nM (IC50, in whole blood (WB) cells)

In Vitro

Enpatoran (0.01 nM-10 μM) inhibits production of IL-6 stimulated by all the ligands (miR-122, Let7c RNA, Alu RNA, and R848) with IC50 values ranging from 35 to 45 nM[1].

MCE has not independently confirmed the accuracy of these methods. They are for reference only.

In Vivo

Pre-treatment with Enpatoran (M5049; oral gavage; 1 mg/kg) before R848 (intraperitoneal injection of 25 µg) dose-dependently inhibits the production of IL-6 and IFN-α in mice[1].
Enpatoran (M5049) exhibits high oral bioavailability (mouse 100%, rat 87%, dog 84%) following oral administration (mouse, rat and dog 1.0 mg/kg)[1].
Enpatoran exhibits moderate half-lives (mouse 1.4, rat 5.0 and dog 13 h) due to high plasma clearance (1.4, 1.2 and 0.59 L/h/kg, respectively) combined with large volumes of distribution (2.7, 8.7 and 5.7 L/kg, respectively) following intravenous administration (mouse, rat and dog 1.0 mg/kg)[1].

MCE has not independently confirmed the accuracy of these methods. They are for reference only.

Animal Model: Female C57BL/6 mice[1]
Dosage: 0.1 mg/kg and 1 mg/kg
Administration: Oral gavage; administered 1 hour prior to R848 challenge
Result: The TLR7/8 agonist R848 stimulated both IFN-α and IL-6 production in mice.
Enpatoran decreased IFN-α and IL-6 production stimulated by R848.
Animal Model: Female CD1 mice, Female Wistar rats, Female beagle dogs[1]
Dosage: 1 mg/kg (Pharmacokinetic Analysis)
Administration: Intravenous (i.v.) or oral gavage
Result: T1/2s of 1.4, 5.0 and 13 h for mice, rats and dogs, respectively.
Molecular Weight

320.31

Formula

C₁₆H₁₅F₃N₄

CAS No.

2101938-42-3

SMILES

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

Shipping

Room temperature in continental US; may vary elsewhere.

Storage

Please store the product under the recommended conditions in the Certificate of Analysis.

References
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Keywords:

EnpatoranM5049M 5049M-5049Toll-like Receptor (TLR)selectiveTLR7/8autoimmunityInhibitorinhibitorinhibit

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