Enpatoran hydrochloride

CAS No. 2101945-93-9

Enpatoran hydrochloride( —— )

Catalog No. M34931 CAS No. 2101945-93-9

Enpatoran (M5049) hydrochloride is a potent, orally active dual inhibitor of TLR7/8 with IC50 values of 11.1 nM and 24.1 nM in HEK293 cells, respectively.

Purity : >98% (HPLC)

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Biological Information

  • Product Name
    Enpatoran hydrochloride
  • Note
    Research use only, not for human use.
  • Brief Description
    Enpatoran (M5049) hydrochloride is a potent, orally active dual inhibitor of TLR7/8 with IC50 values of 11.1 nM and 24.1 nM in HEK293 cells, respectively.
  • 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.
  • 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.
  • 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. Enpatoran hydrochloride exhibits high oral bioavailability (mouse 100%, rat 87%, dog 84%) following oral administration (mouse, rat and dog 1.0 mg/kg). 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).Animal Model:Female C57BL/6 mice 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 hydrochloridedecreased IFN-α and IL-6 production stimulated by R848.
  • Synonyms
    ——
  • Pathway
    Others
  • Target
    Other Targets
  • Recptor
    Others
  • Research Area
    ——
  • Indication
    ——

Chemical Information

  • CAS Number
    2101945-93-9
  • Formula Weight
    356.78
  • Molecular Formula
    C16H16ClF3N4
  • Purity
    >98% (HPLC)
  • Solubility
    In Vitro:?DMSO : 16.67 mg/mL (46.72 mM; Ultrasonic (<60°C)
  • SMILES
    Cl.N[C@@H]1C[C@@H](CN(C1)c1ccc(C#N)c2ncccc12)C(F)(F)F
  • Chemical Name
    ——

Shipping & Storage Information

  • Storage
    (-20℃)
  • Shipping
    With Ice Pack
  • Stability
    ≥ 2 years

Reference

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.?
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