| Identification | Back Directory | [Name]
Gardiquimod trifluoroacetate | [CAS]
1159840-61-5 | [Synonyms]
Gardiquimod TFA
Gardiquimod diTFA
gardiquimod TFA salt
Gardiquimod trifluoroacetate
1H-Imidazo[4,5-c]quinoline-1-ethanol, 4-amino-2-[(ethylamino)methyl]-α,α-dimethyl-, 2,2,2-trifluoroacetate (1:2)
1-(4-Amino-2-((ethylamino)methyl)-1H-imidazo[4,5-c]quinolin-1-yl)-2-methylpropan-2-ol bis(2,2,2-trifluoroacetate) | [Molecular Formula]
C19H24F3N5O3 | [MOL File]
1159840-61-5.mol | [Molecular Weight]
427.43 |
| Chemical Properties | Back Directory | [storage temp. ]
Inert atmosphere,Store in freezer, under -20°C | [solubility ]
DMSO:50.0(Max Conc. mg/mL);116.98(Max Conc. mM)
Water:25.0(Max Conc. mg/mL);58.49(Max Conc. mM) | [form ]
Solid | [color ]
White to off-white |
| Hazard Information | Back Directory | [Uses]
Gardiquimod diTFA is an imidazoline TLR7/8 agonist. Gardiquimod diTFA inhibits HIV-1 infection of macrophages and activated peripheral blood mononuclear cells (PBMCs). Gardiquimod diTFA specifically activates TLR7 at concentrations below 10 μM. | [in vivo]
Dendritic cells (DCs) in combination with Gardiquimod (1 mg/kg per mouse; i.p.; daily for 7 days) improves the anti-tumor effects of NK cells[2]. | Animal Model: | Male athymic nude mice (Balb-nu/nu, 5 weeks old) (bearing human HepG2 liver carcinoma xenografts)[2] | | Dosage: | 1 mg/kg per mouse | | Administration: | i.p.; daily for 7 days | | Result: | Significantly suppressed the growth of human HepG2 liver carcinoma xenografts. |
| [IC 50]
TLR7; TLR8; HIV-1 | [References]
[1] Buitendijk M, et al. Gardiquimod: a Toll-like receptor-7 agonist that inhibits HIV type 1 infection of human macrophages and activated T cells. AIDS Res Hum Retroviruses. 2013 Jun;29(6):907-18. DOI:10.1089/aid.2012.0313
[2] Ma F, et al. The TLR7 agonists imiquimod and gardiquimod improve DC-based immunotherapy for melanoma in mice. Cell Mol Immunol. 2010 Sep;7(5):381-8. DOI:10.1038/cmi.2010.30
[3] Zhou Z, et al. TLR7/8 agonists promote NK-DC cross-talk to enhance NK cell anti-tumor effects in hepatocellular carcinoma. Cancer Lett. 2015 Dec 28;369(2):298-306. DOI:10.1016/j.canlet.2015.09.017 |
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