1. Signaling Pathways
  2. Immunology/Inflammation
  3. Toll-like Receptor (TLR)
  4. TLR7 Isoform
  5. TLR7 Antagonist

TLR7 Antagonist

TLR7 Antagonists (6):

Cat. No. Product Name Effect Purity
  • HY-N0201
    Atractylenolide I
    Antagonist 99.94%
    Atractylenolide I is a sesquiterpene derived from the rhizome of Atractylodes macrocephala, possesses diverse bioactivities, such as neuroprotective, anti-allergic, anti-inflammatory and anticancer properties. Atractylenolide I reduces protein levels of phosphorylated JAK2 and STAT3 in A375 cells, and acts as a TLR4-antagonizing agent.
  • HY-12756A
    E6446 dihydrochloride
    Antagonist 99.29%
    E6446 dihydrochloride is a potent and orally acitve TLR7 and TLR9 antagonist, used in the research of deleterious inflammatory responses. E6446 dihydrochloride is also a potent SCD1 inhibitor (KD: 4.61 μM), significantly inhibiting adipogenic differentiation and hepatic lipogenesis through SCD1-ATF3 signaling. E6446 dihydrochloride also improves liver pathology in high-fat diet (HFD)-fed mice and may be useful in the study of non-alcoholic fatty liver disease (NAFLD).
  • HY-12756
    E6446
    Antagonist 98.78%
    E6446 is a potent and orally acitve TLR7 and TLR9 antagonist, used in the research of deleterious inflammatory responses. E6446 is also a potent SCD1 inhibitor (KD: 4.61 μM), significantly inhibiting adipogenic differentiation and hepatic lipogenesis through SCD1-ATF3 signaling. E6446 also improves liver pathology in high-fat diet (HFD)-fed mice and may be useful in the study of non-alcoholic fatty liver disease (NAFLD).
  • HY-131945
    CU-115
    Antagonist 99.63%
    CU-115 is a potent TLR8 antagonist (IC50=1.04 µM), and shows selective for TLR8 over TLR7 (IC50=>50 µM). CU-115 decreases TNF-α and IL-1β production activated by R-848 in THP-1 cells.
  • HY-178037
    TLR9 antagonist 1
    Antagonist
    TLR9 antagonist 1 (Compound 38) is a selective TLR9 antagonist with an IC50 of 0.1  nM for hTLR9 over hTLR2/4/5/7/8. TLR9 antagonist 1 exacerbates disease symptoms with increased anti-dsDNA and anti-Sm levels in systemic lupus erythematosus (SLE) mouse models. TLR9 antagonist 1 can be used for inflammatory and immune diseases like lupus and arthritis research.
  • HY-175782
    SMU-R39
    Antagonist
    SMU-R39 is a TLR7 and TLR8 antagonist with IC50 values of 3.22 μM and 0.24 μM, respectively. SMU-R39 binds to recombinant mTLR7 protein (KD = 2.36 μM) and to recombinant hTLR8 protein (KD = 105 nM). SMU-R39 suppresses downstream NF-κB and MAPK signaling, and reduces secretion/transcription of pro-inflammatory cytokines (TNF-α, IL-1β, IL-6) in PBMCs and THP-1 cells. SMU-R39 demonstrates anti-inflammatory efficacy in Imiquimod (IMQ) (HY-B0180)-induced psoriasis mouse model. SMU-R39 can be used for the study of autoimmune diseases such as psoriasis.