[CAS NO. 1642857-69-9] TLR7 agonist 2
PRODUCTS SPECIFICATIONS [1642857-69-9]
DESCRIPTION [1642857-69-9]
Overview
| MDL | - |
|---|---|
| Molecular Weight | 336.35 |
| Molecular Formula | C17H16N6O2 |
| SMILES | CC1=CC(COC2=C(N(CC3=NC=CC=C3)C=C4)C4=NC(N)=N2)=NO1 |
Summary
TLR7 agonist 2 is a potent and selective Toll-like Receptor 7 ( TLR7 ) agonist with a LEC of 0.4 μM.
IC50 & Target
LEC: 0.4 μM (TLR7) [1]
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 μM for human TLR8. TLR7 agonist 2 demonstrates low inhibition across five CYP450 isozymes (IC 50 >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 3 H-dofetilide binding in vitro (IC 50 >50 μM) [1] .
MCE has not independently confirmed the accuracy of these methods. They are for reference only.
In Vivo
TLR7 agonist 2 is found to be rapidly cleared in conjunction with our target profile. Both C max 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 [1] .
MCE has not independently confirmed the accuracy of these methods. They are for reference only.
Appearance
Solid
Shipping
Room temperature in continental US; may vary elsewhere.
Storage
| Powder | -20°C | 3 years |
|---|---|---|
| 4°C | 2 years | |
| In solvent | -80°C | 6 months |
| -20°C | 1 month |
Solvent & Solubility
DMSO : 160 mg/mL ( 475.69 mM ; Need ultrasonic and warming)
Stock Solutions
| Concentration Solvent Mass | 1 mg | 5 mg | 10 mg |
|---|
| 1 mM | 2.9731 mL | 14.8655 mL | 29.7309 mL |
| 5 mM | 0.5946 mL | 2.9731 mL | 5.9462 mL |
| 10 mM | 0.2973 mL | 1.4865 mL | 2.9731 mL |
