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。

TLR7 agonist 2 is a potent and selective Toll-like Receptor 7 (TLR7) agonist with a LEC of 0.4 μM.

Solid

LEC: 0.4 μM (TLR7)

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 H-dofetilide binding in vitro (IC50 >50 μM). has not independently confirmed the accuracy of these methods. They are for reference only.

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. has not independently confirmed the accuracy of these methods. They are for reference only.

Room temperature in continental US; may vary elsewhere.

Powder -20°C 3 years；4°C 2 years

[1]. McGowan DC, et al. Identification and Optimization of Pyrrolo[3,2-d]pyrimidine Toll-like Receptor 7 (TLR7) Selective Agonists for the Treatment of Hepatitis B. J Med Chem. 2017 Jul 27;60(14):6137-6151.

In Vitro: DMSO : 160 mg/mL (475.69 mM; Need ultrasonic and warming)配制储备液