Gardiquimod trifluoroacetate
Gardiquimod trifluoroacetate Basic information
- Product Name:
- Gardiquimod trifluoroacetate
- Synonyms:
-
- Gardiquimod trifluoroacetate
- 1H-Imidazo[4,5-c]quinoline-1-ethanol, 4-amino-2-[(ethylamino)methyl]-α,α-dimethyl-, 2,2,2-trifluoroacetate (1:2)
- gardiquimod TFA salt
- Gardiquimod TFA
- Gardiquimod diTFA
- 1-(4-Amino-2-((ethylamino)methyl)-1H-imidazo[4,5-c]quinolin-1-yl)-2-methylpropan-2-ol bis(2,2,2-trifluoroacetate)
- CAS:
- 1159840-61-5
- MF:
- C19H24F3N5O3
- MW:
- 427.43
- Mol File:
- 1159840-61-5.mol
Gardiquimod trifluoroacetate Chemical Properties
- 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
Gardiquimod trifluoroacetate Usage And Synthesis
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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