TLR8 agonist2 hydrochloride is a potent and selectiveTLR8agonist with anEC₅₀of 3 nM for humanTLR8.TLR8 agonist2 hydrochloride shows less active against humanTLR7(EC₅₀of 33.33 μM)^[1].

TLR8 agonist 2 (Example 1) increases the levels of TNF-α, IL-12p40, IFN-γ, and IFN-α with EC₅₀values 105 nM, 26 nM, 29 nM, and 2800 nM, respectively, in human peripheral blood mononuclear cells (hPBMC)^[1].

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 T_1/2of TLR8 agonist 2 are 0.25 h (1 mg/kg i.v.) and 0.5 h (5 mg/kg p.o.), the AUC_lastare 450 ng/mL*hr (i.v.) and 624 ng/mL*hr (p.o.). And for oral administration, the bioavailability (%F) is 27.7%^[1]

C₁₆H₂₂N₈.xHCl

2412937-65-4

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