Cat. No.: HY-134581

Enpatoran

Name: Enpatoran
Brand: MedChemExpress
SKU: HY-134581
Price: 150.00 USD
Availability: InStock
Rating: 5 (18 reviews)

(Synonyms: M5049)

18 Cited Publications

Customer Review

Based on 18 publication(s) in Google Scholar

Enpatoran (M5049) is an orally active and selective TLR7/8 antagonist. Enpatoran inhibits the activation of the downstream type I interferon pathway. Enpatoran 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.

Purity: 99.87%
CAS No.: 2101938-42-3
Formula: C₁₆H₁₅F₃N₄
Molecular Weight:320.31

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)

Enpatoran Chemical Structure

CAS No.: 2101938-42-3

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Top Publications Citing

Use of MCE Products

Fluorescent Dye

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

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

Biological Activity

Description

IC₅₀ & Target

^[2]

TLR8

TLR7

All Toll-like Receptor (TLR) Isoforms :

In Vitro

Enpatoran (1 μM; 1 h pretreatment before pso-miR stimulation) 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) potently suppresses pso-miR-triggered NK cell degranulation (CD107a surface expression) in human PBMCs^[2].
Enpatoran (1 μM; 1 h) 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. 2101938-42-3
Appearance Solid
Molecular Weight 320.31
Formula C₁₆H₁₅F₃N₄
Color Light yellow to yellow
SMILES

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

M5049
Shipping

Room temperature in continental US; may vary elsewhere.
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)

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 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 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 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 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 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 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

Solvent & Solubility

In Vitro:

DMSO : 100 mg/mL (312.20 mM; Need ultrasonic; Hygroscopic DMSO has a significant impact on the solubility of product, please use newly opened DMSO)

Ethanol : 100 mg/mL (312.20 mM; Need ultrasonic)

View the Complete Stock Solution Preparation Table

Preparing Stock Solutions

View the Complete Stock Solution Preparation Table

Concentration Solvent Mass

1 mg

5 mg

10 mg

Concentration

Solvent

Mass

1 mM

3.1220 mL

15.6099 mL

31.2198 mL

5 mM

0.6244 mL

3.1220 mL

6.2440 mL

10 mM

0.3122 mL

1.5610 mL

3.1220 mL

Please refer to the solubility information to select the appropriate solvent. Once prepared, please aliquot and store the solution to prevent product inactivation from repeated freeze-thaw cycles.

Storage method and period of stock solution: -80°C, 2 years; -20°C, 1 year (sealed storage, away from moisture and light). When stored at -80°C, please use it within 2 years. When stored at -20°C, please use it within 1 year.

Molarity Calculator

Mass (g) = Concentration (mol/L) × Volume (L) × Molecular Weight (g/mol)

Mass Mass

Concentration Concentration

Volume Volume

Molecular Weight Molecular Weight

Dilution Calculator

Concentration _(start) × Volume _(start) = Concentration _(final) × Volume _(final)

Concentration _(start) Concentration _(start)

Volume _(start) Volume _(start)

Concentration _(final) Concentration _(final)

Volume _(final) Volume _(final)

In Vivo:

Select the appropriate dissolution method based on your experimental animal and administration route.

Stock Solution Working Solution

For the following dissolution methods, please ensure to first prepare a clear stock solution using an In Vitro approach and then sequentially add co-solvents:
To ensure reliable experimental results, the clarified stock solution can be appropriately stored based on storage conditions. As for the working solution for In Vivo experiments, it is recommended to prepare freshly and use it on the same day.
The percentages shown for the solvents indicate their volumetric ratio in the final prepared solution. If precipitation or phase separation occurs during preparation, heat and/or sonication can be used to aid dissolution.

Protocol 1

Add each solvent one by one: 10% DMSO 40% PEG300 5% Tween-80 45% Saline

Solubility: ≥ 2.44 mg/mL (7.62 mM); Clear solution

This protocol yields a clear solution of ≥ 2.44 mg/mL (saturation unknown).

Taking 1 mL working solution as an example, add 100 μL DMSO stock solution (24.4 mg/mL) to 400 μL PEG300, and mix evenly; then add 50 μL Tween-80 and mix evenly; then add 450 μL Saline to adjust the volume to 1 mL.

Protocol 2

Add each solvent one by one: 10% DMSO 90% (20% SBE-β-CD in Saline)

Solubility: ≥ 2.44 mg/mL (7.62 mM); Clear solution

This protocol yields a clear solution of ≥ 2.44 mg/mL (saturation unknown).

Taking 1 mL working solution as an example, add 100 μL DMSO stock solution (24.4 mg/mL) to 900 μL 20% SBE-β-CD in Saline, and mix evenly.

In Vivo Dissolution Calculator

Please enter the basic information of animal experiments:

Dosage Dosage
mg/kg
Animal Weight (Per Animal) Animal Weight (Per Animal)
g
Dosing Volume (Per Animal) Dosing Volume (Per Animal)
μL
Number of Animals Number of Animals

Recommended: Prepare an additional quantity of animals to account for potential losses during experiments.

Recommended: Prepare an additional quantity of animals to account for potential losses during experiments.

Please enter your animal formula composition:

%
DMSO +

Recommended: Keep the proportion of DMSO in working solution below 2% if your animal is weak.
%
+
+
%
Tween-80 + +
%
Saline +

The co-solvents required include: DMSO, . All of co-solvents are available by MedChemExpress (MCE). , Tween 80. All of co-solvents are available by MedChemExpress (MCE).

Working solution concentration: 0.22 mg/mL

Purity & Documentation

Select Batch:

Purity: 99.98%

Assay: 99.98%

ee.: 99.98%

Data Sheet (278 KB)
SDS (252 KB)
- English - EN (252 KB)
- Français - FR (252 KB)
- Deutsch - DE (252 KB)
- Norwegian - NO (252 KB)
- Español - ES (252 KB)
- Swedish - SV (252 KB)
- Italian - IT (252 KB)
- Korean - KR (252 KB)
- Portuguese - PT (252 KB)
COA (2659 KB)
Elemental Analysis Report (2659 KB)
HNMR (2659 KB)
CNMR (2659 KB)
RP-HPLC (2659 KB)
NP-HPLC (2659 KB)
MS (2659 KB)
LCMS (2659 KB)
IR (2659 KB)
GC (2659 KB)
OR (2659 KB)
SDS-PAGE (2659 KB)
SEC-HPLC (2659 KB)
Other Report (2659 KB)
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]

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.

Complete Stock Solution Preparation Table

Optional Solvent	Concentration Solvent Mass	1 mg	5 mg	10 mg	25 mg
DMSO / Ethanol	1 mM	3.1220 mL	15.6099 mL	31.2198 mL	78.0494 mL
	5 mM	0.6244 mL	3.1220 mL	6.2440 mL	15.6099 mL
	10 mM	0.3122 mL	1.5610 mL	3.1220 mL	7.8049 mL
	15 mM	0.2081 mL	1.0407 mL	2.0813 mL	5.2033 mL
	20 mM	0.1561 mL	0.7805 mL	1.5610 mL	3.9025 mL
	25 mM	0.1249 mL	0.6244 mL	1.2488 mL	3.1220 mL
	30 mM	0.1041 mL	0.5203 mL	1.0407 mL	2.6016 mL
	40 mM	0.0780 mL	0.3902 mL	0.7805 mL	1.9512 mL
	50 mM	0.0624 mL	0.3122 mL	0.6244 mL	1.5610 mL
	60 mM	0.0520 mL	0.2602 mL	0.5203 mL	1.3008 mL
	80 mM	0.0390 mL	0.1951 mL	0.3902 mL	0.9756 mL
	100 mM	0.0312 mL	0.1561 mL	0.3122 mL	0.7805 mL

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Enpatoran

Publications Citing Use of MedChemExpress (MCE) Enpatoran

All Toll-like Receptor (TLR) Isoforms