N-[4-(4-Amino-2-ethyl-1H-imidazo[4,5-c]quinolin-1-yl)butyl]-methylesulfonamide CAS#: 532959-63-0

N-[4-(4-Amino-2-ethyl-1H-imidazo[4,5-c]quinolin-1-yl)butyl]-methylesulfonamide Basic information

Product Name:

N-[4-(4-Amino-2-ethyl-1H-imidazo[4,5-c]quinolin-1-yl)butyl]-methylesulfonamide

Synonyms:

N-[4-(4-Amino-2-ethyl-1H-imidazo[4,5-c]quinolin-1-yl)butyl]-methylesulfonamide
PF-4878691
3M-852A
Methanesulfonamide, N-[4-(4-amino-2-ethyl-1H-imidazo[4,5-c]quinolin-1-yl)butyl]-
PF-4878691 (3M-852A)
N-[4-(4-Amino-2-ethyl-1H-imidazo[4,5-c]quinolin-1-yl)butyl]-methyl sulfonamide,immunomodulator, immune response modifier
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)methanesulfonamide

CAS:

532959-63-0

MF:

C17H23N5O2S

MW:

361.46

Mol File:

532959-63-0.mol

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N-[4-(4-Amino-2-ethyl-1H-imidazo[4,5-c]quinolin-1-yl)butyl]-methylesulfonamide Chemical Properties

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

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N-[4-(4-Amino-2-ethyl-1H-imidazo[4,5-c]quinolin-1-yl)butyl]-methylesulfonamide Usage And Synthesis

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

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

N-[4-(4-Amino-2-ethyl-1H-imidazo[4,5-c]quinolin-1-yl)butyl]-methylesulfonamideSupplier

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