Cat. No.: HY-134581

Enpatoran

(Synonyms: M5049)

18 Cited Publications

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Based on 18 publication(s) in Google Scholar

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 .

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Pureté: 99.87%
CAS No.: 2101938-42-3
Formule: C₁₆H₁₅F₃N₄
Masse moléculaire:320.31

Stockage:

-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

Activité biologique
- Description
- IC₅₀ & Target
- In Vitro
- In Vivo
Chemical Information
Publications (18)
Solvant et solubilité
- In Vitro
- In Vivo
Pureté et documentation
Références
Help & FAQs
Classifications
Bioz

Activité biologique

Description

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)

Voir tous les produits spécifiques à Isoform Toll-like Receptor (TLR) :

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].

MedChemExpress (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].

MedChemExpress (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:

T_1/2s of 1.4, 5.0 and 13 h for mice, rats and dogs, respectively.

Chemical Information

CAS No. 2101938-42-3
Appearance Solid
Masse moléculaire 320.31
Formule 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
Livraison

Room temperature in continental US; may vary elsewhere.
Stockage

-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

Solvant et solubilité

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.

Calculateur de molarité

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

Mass Mass

Concentration Concentration

Volume Volume

Molecular Weight Molecular Weight

Calculateur de dilution

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

Pureté et documentation

Select Batch:

Pureté: 99.98%

Assay: 99.98%

ee.: 99.98%

Fiche technique (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)
Instruction de manipulation (2659 KB)

Références

[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]

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

Keywords

Enpatoran

18 Cited Publications

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Enpatoran

MCE Bioactive Compound Library

Publications Citing Use of MedChemExpress (MCE) Enpatoran

Voir tous les produits spécifiques à Isoform Toll-like Receptor (TLR)

Activité biologique

Chemical Information

Publications (18)

Solvant et solubilité

Pureté et documentation

Références

Help & FAQs

Complete Stock Solution Preparation Table

Enpatoran

MCE Bioactive Compound Library

Publications Citing Use of MedChemExpress (MCE) Enpatoran

Voir tous les produits spécifiques à Isoform Toll-like Receptor (TLR)

Activité biologique

Chemical Information

Publications (18)

Solvant et solubilité

Pureté et documentation

Références

Help & FAQs

Complete Stock Solution Preparation Table

Enpatoran Related Classifications

HY-134581 Related Classifications