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TLR7 agonist 2

CAS No. : 1642857-69-9

MCE 站：TLR7 agonist 2

产品活性：TLR7 agonist 2 是一种有效且有选择性的 Toll 样受体 7 (TLR7) 激动剂，LEC 值为 0.4 μM。

研究领域：Immunology/Inflammation

作用靶点：Toll-like Receptor (TLR)

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 (IC₅₀ >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 ³H-dofetilide binding in vitro (IC₅₀ >50 μM).

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.

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