1. Immunology/Inflammation
  2. Toll-like Receptor (TLR)

Gardiquimod trifluoroacetate 

Cat. No.: HY-103697A Purity: 99.28%
Handling Instructions

Gardiquimod trifluoroacetate is a specific TLR7 agonist which can also inhibit HIV-1 reverse transcriptase.

For research use only. We do not sell to patients.
Gardiquimod trifluoroacetate Chemical Structure

Gardiquimod trifluoroacetate Chemical Structure

CAS No. : 1159840-61-5

Size Price Stock Quantity
10 mM * 1 mL in DMSO USD 60 In-stock
5 mg USD 50 In-stock
10 mg USD 80 In-stock
25 mg USD 180 In-stock
50 mg USD 280 In-stock
100 mg USD 480 In-stock
200 mg   Get quote  
500 mg   Get quote  

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  • Biological Activity

  • Protocol

  • Technical Information

  • Purity & Documentation

  • References


Gardiquimod trifluoroacetate is a specific TLR7 agonist which can also inhibit HIV-1 reverse transcriptase.

IC50 & Target

TLR7, HIV-1 reverse transcriptase[1]

In Vitro

Levels of HIV-1 DNA measured by real-time PCR are significantly lower in Gardiquimod trifluoroacetate-treated cells compare to untreated controls on day 9 postinfection. Significantly lower levels of HIV-1 DNA and HIV-1 p24 are observed in Gardiquimod trifluoroacetate-treated and HIV-1-exposed macrophages cocultured with activated PBMCs. Gardiquimod trifluoroacetate significantly increases IFN-α mRNA levels 80-, 20-, and 35-fold above the level of detection at 2, 4, and 6 h posttreatment, respectively[1]. The results show that treatment with Gardiquimod trifluoroacetate results in significant increases in expression of CD69 on T, NK and natural killer T (NKT) cells. It is also found that Gardiquimod trifluoroacetate stimulation increases mRNA expression of IL-12 p40 in RAW264.7 cells. Furthermore, Gardiquimod trifluoroacetate induces augmented secretion of IL-12 p70 into culture supernatant 48 and 72 h after treatment[2].

In Vivo

On day 12, the tumor volume in mice injected with PBS increases to 1770±370 mm3, whereas it is only 230±70 mm3 in mice treated with Gardiquimod trifluoroacetate[2].

Preparing Stock Solutions
Concentration Volume Mass 1 mg 5 mg 10 mg
1 mM 1.8469 mL 9.2346 mL 18.4693 mL
5 mM 0.3694 mL 1.8469 mL 3.6939 mL
10 mM 0.1847 mL 0.9235 mL 1.8469 mL
Please refer to the solubility information to select the appropriate solvent.
Cell Assay

Peripheral blood cells (PBMCs) are resuspended at a concentration of 5×106 cells/mL in serum-free RPMI and added to large (150-cm2) tissue culture flasks to permit monocyte attachment. The cells are maintained in a humidified incubator at 37°C with 5% CO2 for a total of 8 days. On the fifth day of culture, the medium is refreshed and one-half of the cells are treated with 0.6 to 3.0 μM Gardiquimod trifluoroacetate for 3 days prior to infection with HIV-1 on day 8 of culture. Control macrophages are left untreated[1]. MCE has not independently confirmed the accuracy of these methods. They are for reference only.

Animal Administration

Six- to eight-week-old C57BL/6 mice weighing 20 to 24 g are used in this study. For subcutaneous (s.c.) tumors, 5×104 B16 cells in 100 µL of PBS are injected s.c. into the right flank of C57BL/6 mice on day 0. Mice are vaccinated intravenously with 4×104 DCs on day 7 and peritumorally injected with 1 mg/kg Gardiquimod trifluoroacetate on days 8 and 10. Control mice are injected with an equivalent volume of PBS. Beginning on day 8, the tumor length and width are measured with a vernier caliper, and tumor volume is calculated as length×width2/2. The mice are killed on day 13, and tumors are excised and weighed[2]. MCE has not independently confirmed the accuracy of these methods. They are for reference only.

Molecular Weight








Powder -20°C 3 years
  4°C 2 years
In solvent -80°C 6 months
  -20°C 1 month

Room temperature in continental US; may vary elsewhere

Solvent & Solubility

10 mM in DMSO

* "<1 mg/mL" means slightly soluble or insoluble. "≥" means soluble, but saturation unknown.

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