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

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
Estimated Time of Arrival: December 31
5 mg USD 50 In-stock
Estimated Time of Arrival: December 31
10 mg USD 80 In-stock
Estimated Time of Arrival: December 31
25 mg USD 180 In-stock
Estimated Time of Arrival: December 31
50 mg USD 280 In-stock
Estimated Time of Arrival: December 31
100 mg USD 480 In-stock
Estimated Time of Arrival: December 31
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  • Biological Activity

  • Protocol

  • Technical Information

  • Purity & Documentation

  • References

Description

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].

Solvent & Solubility
In Vitro: 

10 mM in DMSO

Preparing
Stock Solutions
Concentration Solvent 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.
References
Cell Assay
[1]

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
[2]

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.

References
Molecular Weight

541.44

Formula

C₂₁H₂₅F₆N₅O₅

CAS No.

1159840-61-5

SMILES

OC(C)(C)CN1C(CNCC)=NC2=C1C3=CC=CC=C3N=C2N.FC(C(O)=O)(F)F.FC(C(O)=O)(F)F

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

Room temperature in continental US; may vary elsewhere

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Product Name:
Gardiquimod trifluoroacetate
Cat. No.:
HY-103697A
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Gardiquimod trifluoroacetate

Cat. No.: HY-103697A