Cat. No.: HY-134581B

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Enpatoran dihydrochloride

Name: Enpatoran dihydrochloride
Brand: MedChemExpress
SKU: HY-134581B
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(Synonyms: M5049 dihydrochloride)

18 Cited Publications

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Based on 18 publication(s) in Google Scholar

Enpatoran dihydrochloride (M5049 dihydrochloride) is an orally active and selective TLR7/8 antagonist. Enpatoran dihydrochloride inhibits the activation of the downstream type I interferon pathway. Enpatoran dihydrochloride is used in studies of cutaneous lupus erythematosus, systemic lupus erythematosus with cutaneous manifestations, and psoriasis.

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

CAS No.: 2409589-21-3
Formula: C₁₆H₁₇Cl₂F₃N₄
Molecular Weight:393.23

Storage:

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

Enpatoran dihydrochloride Chemical Structure

CAS No.: 2409589-21-3

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Fluorescent Dye

Strong Fluorescence Signal / Multi-Disciplinary Applications / High Fluorescence Specificity

Biological Activity
- Description
- IC₅₀ & Target
- Cellular Effect
- In Vitro
- In Vivo
Chemical Information
Publications (18)
Purity & Documentation
References
Calculators
Help & FAQs
Classifications
Bioz

Biological Activity

Description

IC₅₀ & Target

^[2]

TLR8

TLR7

All Toll-like Receptor (TLR) Isoforms :

Cellular Effect

Cell Line	Type	Value	Description	References
HEK293	IC50	11.1 nM	Inhibition of R848-induced NF-κB luciferase activity in HEK293 cells stably transfected with TLR7 and NF-κB-luciferase reporter, incubated for 5 hours post-stimulation measured by luminescence using SteadyGlo substrate reagent. Inhibition of R848-induced NF-κB luciferase activity in HEK293 cells stably transfected with TLR7 and NF-κB-luciferase reporter, incubated for 5 hours post-stimulation measured by luminescence using SteadyGlo substrate reagent.	33328334
HEK293	IC50	24.1 nM	Inhibition of R848-induced NF-κB luciferase activity in HEK293 cells stably transfected with TLR8 and NF-κB-luciferase reporter, incubated for 5 hours post-stimulation measured by luminescence using SteadyGlo substrate reagent. Inhibition of R848-induced NF-κB luciferase activity in HEK293 cells stably transfected with TLR8 and NF-κB-luciferase reporter, incubated for 5 hours post-stimulation measured by luminescence using SteadyGlo substrate reagent.	33328334
PBMC	IC50	68.3 nM	Inhibition of IL-6 production stimulated by TLR7-specific agonist CL-087 in human PBMCs, with 30 minutes pre-incubation of M5049 and overnight incubation after ligand addition measured by AlphaLISA. Inhibition of IL-6 production stimulated by TLR7-specific agonist CL-087 in human PBMCs, with 30 minutes pre-incubation of M5049 and overnight incubation after ligand addition measured by AlphaLISA.	33328334
PBMC	IC50	620 nM	Inhibition of IL-6 production stimulated by TLR8-specific agonist in human PBMCs, with 30 minutes pre-incubation of M5049 and overnight incubation after ligand addition measured by AlphaLISA. Inhibition of IL-6 production stimulated by TLR8-specific agonist in human PBMCs, with 30 minutes pre-incubation of M5049 and overnight incubation after ligand addition measured by AlphaLISA.	33328334
PBMC	IC50	8.9 nM	Inhibition of R848-stimulated IFN-α production in human PBMCs, with 30 minutes pre-incubation of M5049 and overnight cell incubation measured by AlphaLISA. Inhibition of R848-stimulated IFN-α production in human PBMCs, with 30 minutes pre-incubation of M5049 and overnight cell incubation measured by AlphaLISA.	33328334
PBMC	IC50	68.5 nM	Inhibition of Alu RNA-stimulated IFN-α production in human PBMCs, with 30 minutes pre-incubation of M5049 and overnight cell incubation measured by AlphaLISA. Inhibition of Alu RNA-stimulated IFN-α production in human PBMCs, with 30 minutes pre-incubation of M5049 and overnight cell incubation measured by AlphaLISA.	33328334
PBMC	IC50	161 nM	Inhibition of Let7c-stimulated IFN-α production in human PBMCs, with 30 minutes pre-incubation of M5049 and overnight cell incubation measured by AlphaLISA. Inhibition of Let7c-stimulated IFN-α production in human PBMCs, with 30 minutes pre-incubation of M5049 and overnight cell incubation measured by AlphaLISA.	33328334
PBMC	IC50	210 nM	Inhibition of miR-122-stimulated IFN-α production in human PBMCs, with 30 minutes pre-incubation of M5049 and overnight cell incubation measured by AlphaLISA. Inhibition of miR-122-stimulated IFN-α production in human PBMCs, with 30 minutes pre-incubation of M5049 and overnight cell incubation measured by AlphaLISA.	33328334

In Vitro

Enpatoran (1 μM; 1 h pretreatment before pso-miR stimulation) dihydrochloride effectively inhibits pso-miR-induced NK cell cytotoxicity against K562 target cells in human PBMCs by blocking TLR7/8 signaling^[2].
Enpatoran (1 μM; 1 h pretreatment before pso-miR stimulation) dihydrochloride potently suppresses pso-miR-triggered NK cell degranulation (CD107a surface expression) in human PBMCs^[2].
Enpatoran (1 μM; 1 h) dihydrochloride markedly reduces the pso-miR-triggered secretion of the TLR7/8-dependent, NK-activating cytokines IFN-α, IFN-β, IL-12, and IL-18 in human PBMCs^[2].

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

In Vivo

Enpatoran (0.1-10 mg/kg; p.o.; once per day; 14 weeks) dihydrochloride effectively ameliorates spontaneous TLR7-driven lupus disease in BXSB-Yaa mice via reduction of proteinuria, autoantibody production, and inflammatory IFN and myeloid gene signatures^[3].

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

Animal Model:

BXSB-Yaa mice (Male, 7 to 8 weeks old, sourced from Jackson Laboratories)^[3]
Dosage:

0.1, 1, 10 mg/kg
Administration:

p.o.; once per day; 14 weeks
Result:

Improved survival of BXSB-Yaa mice.
Reduced kidney disease as evidenced by decreased proteinuria (lower urinary albumin-to-creatinine ratio).
Significantly reduced levels of both DNA-containing autoantibodies (anti-dsDNA, anti-histone) and RNA-binding protein autoantibodies (anti-RiboP, anti-SmRNP), with 10 mg/kg doses reducing autoantibody titers below pre-treatment baseline levels.
Significantly reduced IFN gene signature scores calculated from a panel of 10 IFN-regulated disease-related genes, and downregulated expression of myeloid and granulocyte marker genes (CLEC4E, TLR8, FCER1G, LILRA5) as well as TLR7.

Chemical Information

CAS No. 2409589-21-3
Molecular Weight 393.23
Formula C₁₆H₁₇Cl₂F₃N₄
SMILES

N#CC1=CC=C(N2C[C@H](C[C@H](C2)N)C(F)(F)F)C3=C1N=CC=C3.Cl.Cl
Synonyms

M5049 dihydrochloride
Shipping

Room temperature in continental US; may vary elsewhere.
Storage

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

Publications (18)

All ELISAIn Vivo Efficacy StudyRT-PCRHistological Imaging/StainingWBIHC

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Journal Impact Factor

Science

STING-NF-κB signaling builds an influenza spillover barrier. [Abstract]

2026 Feb 26;391(6788):eads4405. PMID: 41747053
Immunity

p16High-expressing immune cells control disease tolerance as a defense and health span-extending strategy. [Abstract]

2026 Mar 26:S1074-7613(26)00083-X. PMID: 41895292
J Extracell Vesicles

Extracellular Vesicles Derived From Streptococcus anginosus Aggravate Lupus Nephritis by Triggering TLR2-MyD88-NF-κB Signalling in NK Cells. [Abstract]

2025 Jul;14(7):e70134. PMID: 40673809
Adv Sci (Weinh)

Improved Systemic Immunochemotherapy Employing an Oxaliplatin-TLR7/8 Agonist Prodrug Strategy. [Abstract]

2026 Jun;13(31):e14588. PMID: 41969225
Biomaterials

Conjugated polymer intrachain donor-acceptor reconfiguration-tailored off-on NIR-II photoacoustic probes with ultralow background for high-fidelity imaging of immunotherapy-associated macrophage reprogramming. [Abstract]

2026 Aug:331:124126. PMID: 41830766
Cell Commun Signal

Cell damage shifts the microRNA content of small extracellular vesicles into a Toll-like receptor 7-activating cargo capable to propagate inflammation and immunity. [Abstract]

2024 Nov 8;22(1):536. PMID: 39516877

Enpatoran dihydrochloride purchased from MedChemExpress. Usage Cited in: Cell Commun Signal. 2024 Nov 8;22(1):536. [Abstract]

pDCs were pretreated or not with Enpatoran (Enp, 1 µM) for 1 h and then stimulated with miR203a for 24 h. IFN-α secretion was evaluated by ELISA.
Cell Commun Signal

TLR7 activation by miR-21 promotes renal fibrosis by activating the pro-inflammatory signaling pathway in tubule epithelial cells. [Abstract]

2023 Aug 18;21(1):215. PMID: 37596656

Enpatoran dihydrochloride purchased from MedChemExpress. Usage Cited in: Cell Commun Signal. 2023 Aug 18;21(1):215. [Abstract]

M5049 (0.3 mg/kg; oral administration). Serum BUN levels of folic acid-treated mice with or without M5049 administration.

Enpatoran dihydrochloride purchased from MedChemExpress. Usage Cited in: Cell Commun Signal. 2023 Aug 18;21(1):215. [Abstract]

M5049 (0.3 mg/kg; oral administration). Relative mRNA levels of kidney damage-related genes (Havcr1 and Lcn2) in the kidney of folic acid-treated mice with or without M5049 administration.

Enpatoran dihydrochloride purchased from MedChemExpress. Usage Cited in: Cell Commun Signal. 2023 Aug 18;21(1):215. [Abstract]

M5049 (0.3 mg/kg; oral administration). Relative mRNA levels of kidney damage-related genes (Havcr1 and Lcn2) in the kidney of folic acid-treated mice with or without M5049 administration.

Enpatoran dihydrochloride purchased from MedChemExpress. Usage Cited in: Cell Commun Signal. 2023 Aug 18;21(1):215. [Abstract]

M5049 (0.3 mg/kg; oral administration). Protein levels of p65, p-p65, CD3, and CD68 in the kidneys were determined via western blotting. α-tubulin was used as a loading control.

Enpatoran dihydrochloride purchased from MedChemExpress. Usage Cited in: Cell Commun Signal. 2023 Aug 18;21(1):215. [Abstract]

M5049 (0.3 mg/kg; oral administration). Representative IHC images of p-p65 in the kidneys.
Br J Pharmacol

Factor XII and prekallikrein promote microvascular inflammation and psoriasis in mice. [Abstract]

2024 Oct;181(19):3760-3778. PMID: 38872396
J Med Chem

2025 Dec 15;68(24):26030–26048.
J Autoimmun

Extracellular microRNAs induce dendritic cell-dependent joint inflammation and potentiate osteoclast differentiation via TLR7/8 engagement. [Abstract]

2024 May:145:103189. PMID: 38442677
Int Immunopharmacol

Elevated transferrin receptor 1 promoting B-cell autoimmunity in systemic lupus erythematosus. [Abstract]

2025 Jun 17:158:114804. PMID: 40373595
J Periodontal Res

Toll-Like Receptor 7 Promotes Periodontal Inflammation and Alveolar Bone Resorption Through the NF-κB Signaling Pathway. [Abstract]

2025 Feb 25. PMID: 40007244
J Innate Immun

TLR7 activation in M-CSF-dependent monocyte-derived human macrophages potentiates inflammatory responses and prompts neutrophil recruitment. [Abstract]

2023;15(1):517-530. PMID: 37040733
Mol Immunol

Inhibition of RNase L enhances the expression efficiency of mRNA-LNPs. [Abstract]

2026 Feb:190:101-109. PMID: 41564652
Patent

US20250312471A1.
Biomed Pharmacother

Baicalin attenuates acetaminophen-induced acute liver injury through inhibiting TLR2-dependent neutrophil extracellular trap formation. [Abstract]

2025 Sep 17:192:118569. PMID: 40967078
bioRxiv

2024 July 25.
bioRxiv

p16High immune cell - controlled disease tolerance as a broad defense and healthspan extending strategy. [Abstract]

2024 Jul 15:2024.07.15.603540. PMID: 39026790

Purity & Documentation

Handling Instructions (2659 KB)

References

[1]. Morand EF, et al. Efficacy and safety of enpatoran, a Toll-like receptor 7/8 inhibitor, in patients with skin manifestations of cutaneous lupus erythematosus or systemic lupus erythematosus: findings from Cohort A of a multicentre, international, double-blind, placebo-controlled, dose-finding phase 2 trial. The Lancet. Rheumatology. 2026 Jul;8(7):e513-e527.

[2]. Gaudenzi C, et al. Psoriatic microRNAs induce NK cell activation via an innate immune crosstalk abrogated by the Toll-like receptor 7/8 antagonist Enpatoran. Journal of translational medicine. 2026 Mar 02;24(1):478.

[3]. Vlach J, et al. Discovery of M5049: A Novel Selective Toll-Like Receptor 7/8 Inhibitor for Treatment of Autoimmunity. The Journal of pharmacology and experimental therapeutics. 2021 Mar;376(3):397-409. [Content Brief]

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Help & FAQs

How should lyophilized recombinant proteins be reconstituted and stored?

1. Before opening the cap, centrifuge the vial at 13000 rpm for 20-30 seconds. This step will ensure that any lyophilized powder that may have adhered to the cap or walls is collected at the bottom of the vial, minimizing the risk of product loss.

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Enpatoran dihydrochloride

18 Cited Publications

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Enpatoran dihydrochloride

Publications Citing Use of MedChemExpress (MCE) Enpatoran dihydrochloride

All Toll-like Receptor (TLR) Isoforms