Enpatoran
Based on 17 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 .
For research use only. We do not sell to patients.
- Purity: 99.80%
- CAS No.: 2101938-42-3
- Formula: C16H15F3N4
- Molecular Weight:320.31
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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)
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Biological Activity
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Chemical Information
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Solvent & Solubility
- Purity & Documentation
- References
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Help & FAQs
Publications Citing Use of MedChemExpress (MCE) Enpatoran
More- Science. 2026 Feb 26;391(6788):eads4405. [Abstract]
- Immunity. 2026 Mar 26:S1074-7613(26)00083-X. [Abstract]
- J Extracell Vesicles. 2025 Jul;14(7):e70134. [Abstract]
- Adv Sci (Weinh). 2026 Jun;13(31):e14588. [Abstract]
- Cell Commun Signal. 2024 Nov 8;22(1):536. [Abstract]
- Cell Commun Signal. 2023 Aug 18;21(1):215. [Abstract]
- Br J Pharmacol. 2024 Oct;181(19):3760-3778. [Abstract]
- Biomed Pharmacother. 2025 Sep 17:192:118569. [Abstract]
- J Autoimmun. 2024 May:145:103189. [Abstract]
- J Med Chem. 2025 Dec 15;68(24):26030–26048.
- Int Immunopharmacol. 2025 May 14:158:114804. [Abstract]
- J Periodontal Res. 2025 Feb 25. [Abstract]
- Mol Immunol. 2026 Feb:190:101-109. [Abstract]
- J Innate Immun. 2023;15(1):517-530. [Abstract]
- Patent. US20250312471A1.
- bioRxiv. 2024 July 25.
- bioRxiv. 2024 Jul 15:2024.07.15.603540. [Abstract]
Customer Validation & Images
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ELISA
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In Vivo Efficacy Study
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RT-PCR
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Histological Imaging/Staining
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WB
Biological Activity
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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) |
? 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.
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Animal Model:Female C57BL/6 mice[1]
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Dosage:0.1 mg/kg and 1 mg/kg
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Administration:Oral gavage; administered 1 hour prior to R848 challenge
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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.
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Animal Model:Female CD1 mice, Female Wistar rats, Female beagle dogs[1]
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Dosage:1 mg/kg (Pharmacokinetic Analysis)
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Administration:Intravenous (i.v.) or oral gavage
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Result:T1/2s of 1.4, 5.0 and 13 h for mice, rats and dogs, respectively.
Chemical Information
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CAS No. 2101938-42-3
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Appearance Solid
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Molecular Weight 320.31
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Formula C16H15F3N4
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Color Light yellow to yellow
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SMILES
N#CC(C=C1)=C(N=CC=C2)C2=C1N3C[C@@H](C(F)(F)F)C[C@@H](N)C3
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Synonyms
M5049
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Shipping
Room temperature in continental US; may vary elsewhere.
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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 (17)
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Journal Impact Factor
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Most Recent
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Science
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 -
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.
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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.
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Br J Pharmacol
2024 Oct;181(19):3760-3778. PMID: 38872396 -
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 -
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 -
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Int Immunopharmacol
Elevated transferrin receptor 1 promoting B-cell autoimmunity in systemic lupus erythematosus. [Abstract]2025 May 14:158:114804. 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 -
Mol Immunol
2026 Feb:190:101-109. PMID: 41564652 -
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 -
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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
Ethanol : 100 mg/mL (312.20 mM; Need ultrasonic)
DMSO : 24.44 mg/mL (76.30 mM; Need ultrasonic; Hygroscopic DMSO has a significant impact on the solubility of product, please use newly opened DMSO)
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.
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.
Concentration (start) × Volume (start) = Concentration (final) × Volume (final)
Select the appropriate dissolution method based on your experimental animal and administration route.
- 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.
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.
Preparation of Saline: Dissolve 0.9 g sodium chloride in ddH₂O and dilute to 100 mL to obtain a clear Saline solution.
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.
Preparation of 20% SBE-β-CD in Saline (4°C, storage for one week): 2 g SBE-β-CD powder is dissolved in 10 mL Saline, completely dissolve until clear.
Please enter the basic information of animal experiments:
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Recommended: Prepare an additional quantity of animals to account for potential losses during experiments.
Please enter your animal formula composition:
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%DMSO +
Recommended: Keep the proportion of DMSO in working solution below 2% if your animal is weak.
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%+
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+%Tween-80 + +
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%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
Method for preparing stock solution: mg drug dissolved in μL DMSO. Stock solution concentration: mg/mL. * In solvent : -80°C, 2 years; -20°C, 1 year (sealed storage, away from moisture and light)
1. Take μL DMSO stock solution;
2. Add μL .
μL , mix evenly;
3. Then add μL Tween 80, mix evenly;
4. Then add μL
Please ensure that the stock solution in the first step is dissolved to a clear state, and add co-solvents in sequence. You can use ultrasonic heating (ultrasonic cleaner, recommended frequency 20-40 kHz), vortexing, etc. to assist dissolution.
Purity & Documentation
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Data Sheet (278 KB)
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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)
- Portuguese - PT (252 KB)
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Handling Instructions (2659 KB)
References
Complete Stock Solution Preparation Table
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.
| Optional Solvent | Concentration Solvent Mass | 1 mg | 5 mg | 10 mg | 25 mg |
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| 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 | |
| Ethanol | 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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