TLR8 agonist 2 hydrochloride

Names

[ Name ]:
TLR8 agonist 2 hydrochloride

Biological Activity

[Description]:

TLR8 agonist 2 hydrochloride is a potent and selective TLR8 agonist with an EC50 of 3 nM for human TLR8. TLR8 agonist 2 hydrochloride shows less active against human TLR7 (EC50 of 33.33 μM)[1].

[Related Catalog]:

Signaling Pathways >> Immunology/Inflammation >> Toll-like Receptor (TLR)

Research Areas >> Inflammation/Immunology

[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]

[1]. Zhe Cai, et al. Tlr8 agonist. WO2020057604A1.

Chemical & Physical Properties

[ Molecular Formula ]:
C₁₆H₂₂N_8.xHCl

Related Compounds

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