TLR7 agonist2 is a potent and selectiveToll-like Receptor7(TLR7) agonist with aLECof 0.4 μM.

LEC: 0.4 μM (TLR7)^[1]

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 channel³H-dofetilide bindingin vitro(IC₅₀>50 μM)^[1].

TLR7 agonist 2 is found to be rapidly cleared in conjunction with our target profile. Both C_maxand 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^[1].

336.35

Solid

C₁₇H₁₆N₆O₂

1642857-69-9

Room temperature in continental US; may vary elsewhere.

DMSO : 160 mg/mL(475.69 mM;Need ultrasonic and warming)

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