TLR7-agonist-1

Research use only, not for human use.

TLR7-agonist-1 is a specific and effective Toll-like Receptor 7 (TLR7) agonist (LEC=0.4 μM).

TLR7-agonist-1 is a specific and effective Toll-like Receptor 7 (TLR7) agonist (LEC=0.4 μM).

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 μMfor 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).

TLR7 agonist 2 is found to be rapidly cleared in conjunction with our target profile. Both Cmax 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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Others

Other Targets

TLR7

Infection|Inflammation/Immunology

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1642857-69-9

336.36

C17H16N6O2

>98% (HPLC)

DMSO : 160 mg/mL 475.69 mM;

CC1=CC(=NO1)COC2=NC(=NC3=C2N(C=C3)CC4=CC=CC=N4)N

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(-20℃)

With Ice Pack

≥ 2 years