tcsc0032944 Gardiquimod trifluoroacetate

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].