2. Immunology/Inflammation
  3. Toll-like Receptor (TLR)
  4. Enpatoran

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.

Enpatoran Chemical Structure

Enpatoran Chemical Structure

CAS No. : 2101938-42-3

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Based on 5 publication(s) in Google Scholar

Other Forms of Enpatoran:

Enpatoran Related Antibodies

Top Publications Citing Use of Products

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TLR3 TLR8 TLR9 TLR2 TLR4 TLR7 TLR1 TLR6

  • Biological Activity

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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 [1].

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)

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.

Enpatoran Related Antibodies
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: T1/2s of 1.4, 5.0 and 13 h for mice, rats and dogs, respectively.
Clinical Trial
Molecular Weight

320.31

Formula

C16H15F3N4
CAS No.
Appearance

Solid

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
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)

Solvent & Solubility
In Vitro: 

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)

Preparing
Stock Solutions
Concentration Solvent Mass 1 mg 5 mg 10 mg
1 mM 3.1220 mL 15.6099 mL 31.2198 mL
5 mM 0.6244 mL 3.1220 mL 6.2440 mL
View the 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.

  • Molarity Calculator

  • Dilution Calculator

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

Mass
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Concentration
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Volume
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Molecular Weight *

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

This equation is commonly abbreviated as: C1V1 = C2V2

Concentration (start)

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C2

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V2

In Vivo:

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.

  • 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.

    Preparation of Saline: Dissolve 0.9 g sodium chloride in ddH₂O and dilute to 100 mL to obtain a clear Saline solution.
  • 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.

    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.
In Vivo Dissolution Calculator
Please enter the basic information of animal experiments:

Dosage

mg/kg

Animal weight
(per animal)

g

Dosing volume
(per animal)

μL

Number of animals

Recommended: Prepare an additional quantity of animals to account for potential losses during experiments.
Please enter your animal formula composition:
%
DMSO +
% 
+
%
Tween-80 +
%
Saline
Recommended: Keep the proportion of DMSO in working solution below 2% if your animal is weak.
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).
Calculation results:
Working solution concentration: 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)

The concentration of the stock solution you require exceeds the measured solubility. The following solution is for reference only. If necessary, please contact MedChemExpress (MCE).
Method for preparing in vivo working solution for animal experiments: Take μL DMSO stock solution, add μL . μL , mix evenly, next add μL Tween 80, mix evenly, then add μL Saline.
 If the continuous dosing period exceeds half a month, please choose this protocol carefully.
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

Purity: 99.77%

COA (248 KB) HNMR (382 KB) LCMS (107 KB)

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
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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Enpatoran Related Classifications

Help & FAQs
  • Do most proteins show cross-species activity?

    Species cross-reactivity must be investigated individually for each product. Many human cytokines will produce a nice response in mouse cell lines, and many mouse proteins will show activity on human cells. Other proteins may have a lower specific activity when used in the opposite species.

Keywords:

Enpatoran2101938-42-3M5049M 5049M-5049Toll-like Receptor (TLR)selectiveTLR7/8autoimmunityInhibitorinhibitorinhibit

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