TLR7-agonist-1( —— )

Catalog No. M18104 CAS No. 1642857-69-9

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Product Name

TLR7-agonist-1
Note

Research use only, not for human use.
Brief Description

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

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

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.
Synonyms

——
Pathway

Others
Target

Other Targets
Recptor

TLR7
Research Area

Infection|Inflammation/Immunology
Indication

——

1.McGowan DC, et al.. J Med Chem. 2017 Jul 27;60(14):6137-6151.

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