TLR7 agonist 2 是选择性 Toll 样受体 7 激动剂，LEC值为 0.4 μM。

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

In HEK293 cell, Receptor 7 (TLR7) agonist with a lowest effective concentration (LEC) of 0.4 μM. For human TLR8,LEC of TLR7-agonist-1 is >100 μM. For the hERG potassium ion channel 3H-dofetilide,TLR7-agonist-1 has limited inhibition of binding (IC50 >50 μM).

The ability of TLR7-agonist-1 to activate human TLR7 and/or TLR8 is assessed by using HEK293 cells. Briefly, HEK293 cells are grown in culture medium (DMEM supplemented with 10% FCS and 2 mM Glutamine). Transfected cells are then detached with Trypsin-EDTA, washed in PBS and resuspended in medium to a density of 1.67×105 cells/mL. Thirty microliters of cells are then dispensed into each well in 384-well plates, where 10 μL of TLR7-agonist-1 in 4% DMSO is already present. Following 6 hours incubation at 37°C, 5% CO2, the luciferase activity is determined by adding 15 μL of Steady Lite Plus substrate to each well and readout performed on a microplate imager. Lowest effective concentrations (LEC) values are determined for TLR7-agonist-1.

In C57Bl/6 mice model,Single oral administration of 0.3, 1, 3, and 10 mg/kg doses of TLR7-agonist-1.

1642857-69-9

C17H16N6O2

336.355

TLR7-agonist-1;TLR7-IN-1

DMSO:160 mg/mL
Powder: -20°C for 3 years
In solvent: -80°C for 2 years