RGNCY-0003 (TLR7-8 inhibitor)

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Substituted Imidazoquinoline with low micromolar activation of both TLR7 (Ec50=1.5uM) and TLR8 (Ec50=49.6uM), which are key targets in the design and development of immunomodulating agents for use as vaccine adjuvants. 








SMILES: CCCCC(N1CC(C)(O)C)=NC2=C1C3=CC=C(C(OC)=O)C=C3N=C2N

Systematic Name: methyl 4-amino-2-butyl-1-(2-hydroxy-2-methylpropyl)-1H-imidazo[4,5-c]quinoline-7-carboxylate 

Molecular Weight: 370.45

PMID: 24383475

Reference: Schiaffo, Charles E., et al. "Structure–Activity Relationship Analysis of Imidazoquinolines with Toll-like Receptors 7 and 8 Selectivity and Enhanced Cytokine Induction." Journal of Medicinal Chemistry 57.2 (2014): 339-347.

Formula: C20H26N4O3

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Tags: TLR7, TLR8, immunity, RGNCY-0003, vaccine