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

Enpatoran hydrochloride (Synonyms: M5049 hydrochloride)

Cat. No.: HY-134581A Purity: 98.82% ee.: 98.06%
Handling Instructions

Enpatoran (M5049) hydrochloride 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 hydrochloride is inactive against TLR3, TLR4 and TLR9. Enpatoran hydrochloride can block molecule synthetic ligands and natural endogenous RNA ligands. Enpatoran hydrochloride exhibits excellent pharmacokinetic properties in vivo. Enpatoran hydrochloride can be used for both innate and adaptive autoimmunity blocking research.

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

Enpatoran hydrochloride Chemical Structure

Enpatoran hydrochloride Chemical Structure

CAS No. : 2101945-93-9

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Solution
10 mM * 1 mL in DMSO USD 440 In-stock
Estimated Time of Arrival: December 31
Solid + Solvent
10 mM * 1 mL
ready for reconstitution
USD 440 In-stock
Estimated Time of Arrival: December 31
Solid
5 mg USD 400 In-stock
Estimated Time of Arrival: December 31
10 mg USD 680 In-stock
Estimated Time of Arrival: December 31
25 mg USD 1350 In-stock
Estimated Time of Arrival: December 31
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Based on 1 publication(s) in Google Scholar

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Description

Enpatoran (M5049) hydrochloride 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 hydrochloride is inactive against TLR3, TLR4 and TLR9. Enpatoran hydrochloride can block molecule synthetic ligands and natural endogenous RNA ligands. Enpatoran hydrochloride exhibits excellent pharmacokinetic properties in vivo. Enpatoran hydrochloride can be used for both innate and adaptive autoimmunity blocking research[1].

IC50 & Target[1]

TLR7

11.1 nM (IC50)

TLR8

24.1 nM (IC50)

In Vitro

Enpatoran hydrochloride (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].

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

In Vivo

Pre-treatment with Enpatoran hydrochloride (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 hydrochloride exhibits high oral bioavailability (mouse 100%, rat 87%, dog 84%) following oral administration (mouse, rat and dog 1.0 mg/kg)[1].
Enpatoran hydrochloride 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].

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 hydrochloride decreased IFN-α and IL-6 production stimulated by R848.
Molecular Weight

356.77

Formula

C₁₆H₁₆ClF₃N₄

CAS No.
SMILES

[H]Cl.N#CC(C=C1)=C(N=CC=C2)C2=C1N3C[[email protected]@H](C(F)(F)F)C[[email protected]@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, 6 months; -20°C, 1 month (sealed storage, away from moisture and light)

Solvent & Solubility
In Vitro: 

DMSO : 16.67 mg/mL (46.72 mM; ultrasonic and warming and heat to 60°C)

Preparing
Stock Solutions
Concentration Solvent Mass 1 mg 5 mg 10 mg
1 mM 2.8029 mL 14.0146 mL 28.0293 mL
5 mM 0.5606 mL 2.8029 mL 5.6059 mL
10 mM 0.2803 mL 1.4015 mL 2.8029 mL
*Please refer to the solubility information to select the appropriate solvent.
In Vivo:
  • 1.

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

    Solubility: 2 mg/mL (5.61 mM); Clear solution; Need ultrasonic

  • 2.

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

    Solubility: 2 mg/mL (5.61 mM); Clear solution; Need ultrasonic

  • 3.

    Add each solvent one by one:  10% DMSO    90% corn oil

    Solubility: 2 mg/mL (5.61 mM); Clear solution; Need ultrasonic

*All of the co-solvents are provided by MCE.
References

Purity: 98.82% ee.: 98.06%

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Keywords:

EnpatoranM5049M 5049M-5049Toll-like Receptor (TLR)endogenous RNA ligandsynthetic ligandautoimmunityinnate autoimmunityadaptive autoimmunityInhibitorinhibitorinhibit

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Enpatoran hydrochloride
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