MedChemExpress -Model Enpatoran -2101938-42-3

FromMedChemExpress LLC (MCE)

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].

Enpatoran

MCE China：Enpatoran

Brand：MedChemExpress (MCE)

Cat. No.HY-134581

CAS：2101938-42-3

Synonyms：M5049

Purity：99.80%

Storage：-20°C, sealed storage, away from moisture and light *In solvent : -80°C, 2 years; -20°C, 1 year (sealed storage, away from moisture and light)

Shipping：Room temperature in continental US; may vary elsewhere.

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 .

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].

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].

IC50 & Target：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)

References：

[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. [Content Brief]

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