| Identification | Back Directory | [Name]
N-[4-(4-Amino-2-ethyl-1H-imidazo[4,5-c]quinolin-1-yl)butyl]-methylesulfonamide | [CAS]
532959-63-0 | [Synonyms]
3M-852A
PF-4878691
PF-4878691 (3M-852A)
Toll-like Receptor (TLR),inhibit,PF4878691,PF 4878691,PF-4878691,Inhibitor
N-(4-(4-Amino-2-ethyl-1H-imidazo[4,5-c]quinolin-1-yl)butyl)methanesulfonamide
N-[4-(4-Amino-2-ethyl-1H-imidazo[4,5-c]quinolin-1-yl)butyl]-methyl sulfonamide
N-[4-(4-Amino-2-ethyl-1H-imidazo[4,5-c]quinolin-1-yl)butyl]-methylesulfonamide
Methanesulfonamide, N-[4-(4-amino-2-ethyl-1H-imidazo[4,5-c]quinolin-1-yl)butyl]-
N-[4-(4-Amino-2-ethyl-1H-imidazo[4,5-c]quinolin-1-yl)butyl]-methyl sulfonamide,immunomodulator, immune response modifier | [Molecular Formula]
C17H23N5O2S | [MDL Number]
MFCD30533308 | [MOL File]
532959-63-0.mol | [Molecular Weight]
361.46 |
| Chemical Properties | Back Directory | [Boiling point ]
632.3±65.0 °C(Predicted) | [density ]
1.38±0.1 g/cm3(Predicted) | [storage temp. ]
Store at -20°C | [solubility ]
Soluble in DMSO | [form ]
Solid | [pka]
11.32±0.40(Predicted) | [color ]
White to off-white |
| Hazard Information | Back Directory | [Uses]
PF-4878691 (3M-852A) is an orally active TLR7 agonist. PF-4878691 has the innate immune response activity, antiviral efficacy against HCV, and can be used for the research of cancer[1][2]. | [in vivo]
PF-4878691 (10-150 mg, Oral gavage, single dose) induces pharmacology in BALB/c mice and C57bl/6 J mice[1]. | Animal Model: | BALB/c mice , C57bl/6 J mice[3] | | Dosage: | 30 mg/kg, 60 mg/kg, 90 mg/kg, 150 mg/kg | | Administration: | Oral gavage (p.o.) | | Result: | Induced dose and time dependant lymphopenia and 2,5,oligoadenylate synthetase (2,5,OAS).
Caused cardiovascular changes.
Significantly increased TLR7 receptor RNA. |
| [IC 50]
TLR7; IL-6; IL-8; IL-1β; IL-2 | [storage]
Store at -20°C | [References]
[1] Fidock MD, et al. The innate immune response, clinical outcomes, and ex vivo HCV antiviral efficacy of a TLR7 agonist (PF-4878691). Clin Pharmacol Ther. 2011 Jun;89(6):821-9. DOI:10.1038/clpt.2011.60
[2] Birmachu W, et al. Transcriptional networks in plasmacytoid dendritic cells stimulated with synthetic TLR 7 agonists [J]. BMC immunology, 2007, 8: 1-19.
[3] Horscroft NJ, et al. Antiviral applications of Toll-like receptor agonists. J Antimicrob Chemother. 2012 Apr;67(4):789-801. DOI:10.1093/jac/dkr588 |
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