TLR8 agonist 2
Names
[ CAS No. ]:
2412937-64-3
[ Name ]:
TLR8 agonist 2
Biological Activity
[Description]:
TLR8 agonist 2 is a potent and selective TLR8 agonist with an EC50 of 3 nM for human TLR8. TLR8 agonist 2 shows less active against human TLR7 (EC50 of 33.33 μM)[1].
[Related Catalog]:
[Target]
TLR8:3 nM (EC50)
TLR7:33.33 μM (EC50)
[In Vitro]
TLR8 agonist 2 (Example 1) increases the levels of TNF-α, IL-12p40, IFN-γ, and IFN-α with EC50 values 105 nM, 26 nM, 29 nM, and 2800 nM, respectively, in human peripheral blood mononuclear cells (hPBMC)[1].
[In Vivo]
The pharmacokinetic related parameters of TLR8 agonist 2 (Example 1) in mice administered with the intravenous administration of 1 mg/kg and the oral administration of 5 mg/kg are detected. The T1/2 of TLR8 agonist 2 are 0.25 h (1 mg/kg i.v.) and 0.5 h (5 mg/kg p.o.), the AUClast are 450 ng/mL*hr (i.v.) and 624 ng/mL*hr (p.o.). And for oral administration, the bioavailability (%F) is 27.7%[1]
[References]
Chemical & Physical Properties
[ Molecular Formula ]:
C16H22N8
[ Molecular Weight ]:
326.40