| Description | TLR7 agonist 2 (TLR7-IN-1) is a specific and effective Toll-like Receptor 7 (TLR7) agonist (LEC=0.4 μM). |
| Cell experiments | 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. |
| Animal experiments | In C57Bl/6 mice model,Single oral administration of 0.3, 1, 3, and 10 mg/kg doses of TLR7-agonist-1. |
| Target activity | TLR7:LEC: 0.4 μM |
| Synonyms | TLR7-agonist-1, TLR7-IN-1 |
| molecular weight | 336.35 |
| Molecular formula | C17H16N6O2 |
| CAS | 1642857-69-9 |
| Storage | Powder: -20°C for 3 years | In solvent: -80°C for 1 year |
| Solubility | DMSO: 45 mg/mL (133.79 mM) |
| References | 1. McGowan DC, et al. Identification and Optimization of Pyrrolo[3,2-d]pyrimidine Toll-like Receptor 7 (TLR7) Selective Agonists for the Treatment of Hepatitis B. J Med Chem. 2017 Jul 27;60(14):6137-6151. |
| Citations | 1. Lu J, Zhong X, Guo C, et al.TLR7-MyD88-DC-CXCL16 axis results neutrophil activation to elicit inflammatory response in pustular psoriasis.Cell Death & Disease.2023, 14(5): 1-13. |