A TLR7 agonist
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TLR7 Agonist 2

Item No. 28450

Technical Information
Formal Name
4-[(5-methyl-3-isoxazolyl)methoxy]-5-(2-pyridinylmethyl)-5H-pyrrolo[3,2-d]pyrimidin-2-amine
CAS Number
1642857-69-9
Synonyms
  • Toll-Like Receptor 7 Agonist 2
Molecular Formula
C17H16N6O2
Formula Weight
Purity
≥98%
A crystalline solid
DMSO: 160 mg/ml
λmax
232, 269, 294 nm
SMILES
NC1=NC(OCC2=NOC(C)=C2)=C3C(C=CN3CC4=NC=CC=C4)=N1
InChi Code
InChI=1S/C17H16N6O2/c1-11-8-13(22-25-11)10-24-16-15-14(20-17(18)21-16)5-7-23(15)9-12-4-2-3-6-19-12/h2-8H,9-10H2,1H3,(H2,18,20,21)
InChi Key
FVKOYFLAKSGBBV-UHFFFAOYSA-N
Shipping & Storage Information
Storage
-20°C
Shipping
Room temperature in continental US; may vary elsewhere
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    Product Description

    TLR agonist 2 is a toll-like receptor 7 (TLR7) agonist with a lowest effective concentration (LEC) value of 0.4 μM in a cell-based reporter assay.1 It is selective for TLR7 over TLR8 (LEC = >100 μM). TLR7 agonist 2 (0.3-10 mg/kg) increases IFN-α levels and the IFN-stimulated gene (ISG) response, increasing the expression of Oas1b, Isg15, and Mx1, in mouse liver and plasma. It increases plasma levels of IFN-α, CCL2, IL-6, IL-1Ra, G-CSF, and IL-10 in cynomolgus monkeys when administered at a dose of 10 mg/kg. TLR agonist 2 (0.3-5 mg/kg) reduces serum and liver viral load in the hydrodynamic injection (HDI) hepatitis B virus (HBV) mouse model.

    WARNING This product is not for human or veterinary use.

    References & Product Citations
    Product Description References

    1. McGowan, D.C., Herschke, F., Pauwels, F., et alIdentification and optimization of pyrrolo[3,2-d]pyrimidine toll-like receptor 7 (TLR7) selective agonists for the treatment of Hepatitis B. J. Med. Chem. 60(14), 6137-6151 (2017).