TLR7-agonist-1

CAS No. 1642857-69-9

TLR7-agonist-1( —— )

Catalog No. M18104 CAS No. 1642857-69-9

TLR7-agonist-1 is a specific and effective Toll-like Receptor 7 (TLR7) agonist (LEC=0.4 μM).

Purity : >98% (HPLC)

COA Datasheet HNMR HPLC MSDS Handing Instructions
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Biological Information

  • Product Name
    TLR7-agonist-1
  • Note
    Research use only, not for human use.
  • Brief Description
    TLR7-agonist-1 is a specific and effective Toll-like Receptor 7 (TLR7) agonist (LEC=0.4 μM).
  • Description
    TLR7-agonist-1 is a specific and effective Toll-like Receptor 7 (TLR7) agonist (LEC=0.4 μM).
  • In Vitro
    TLR7 agonist 2 is a potent and selective Toll-like Receptor 7 (TLR7) agonist with a lowest effective concentration (LEC) of 0.4 μM in HEK293 cell. TLR7 agonist 2 is found to be selective for TLR7 over TLR8 with LEC of >100 μMfor human TLR8. TLR7 agonist 2 demonstrates low inhibition across five CYP450 isozymes (IC50 >10 μM) and is also not a time dependent inhibitor of CYP450 3A4. TLR7 agonist 2 has limited inhibition of the hERG potassium ion channel 3H-dofetilide binding in vitro (IC50 >50 μM).
  • In Vivo
    TLR7 agonist 2 is found to be rapidly cleared in conjunction with our target profile. Both Cmax and AUC increase less than dose proportionally between 0.3 and 3 mg/kg and more than dose-proportionally between 3 and 10 mg/kg. TLR7 agonist 2 can induce an antiviral interferon stimulated gene (ISG) response without inducing an IFNα response at a low dose. TLR7 agonist 2 also induces a 2.7 log decrease in serum HBV viral load from 0.3 mg/kg, and a maximum 3.1 log decrease is observed for doses between 1 and 5 mg/kg.
  • Synonyms
    ——
  • Pathway
    Others
  • Target
    Other Targets
  • Recptor
    TLR7
  • Research Area
    Infection|Inflammation/Immunology
  • Indication
    ——

Chemical Information

  • CAS Number
    1642857-69-9
  • Formula Weight
    336.36
  • Molecular Formula
    C17H16N6O2
  • Purity
    >98% (HPLC)
  • Solubility
    DMSO : 160 mg/mL 475.69 mM;
  • SMILES
    CC1=CC(=NO1)COC2=NC(=NC3=C2N(C=C3)CC4=CC=CC=N4)N
  • Chemical Name
    ——

Shipping & Storage Information

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

Reference

1.McGowan DC, et al.. J Med Chem. 2017 Jul 27;60(14):6137-6151.
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