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CAS No.: 1159840-61-5

Gardiquimod diTFA Catalog No. CSN24481

Synonyms: Gardiquimod TFA salt;Gardiquimod

Gardiquimod trifluoroacetate is a specific TLR7 agonist.

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技术信息

生物活性

描述Immune response modifiers are being studied as therapeutic agents for viral infections and cancer. These molecules include agonists for the Toll-like receptors (TLR), a family of innate immune receptors. TLR7 and 8, located in cellular endosomes, bind single-stranded RNA characteristic of viral genomes, and trigger intracellular signaling pathways that induce inflammatory cytokines and antiviral innate immune factors^[1]. Gardiquimod trifluoroacetate is a specific TLR7 agonist when used at concentrations below 10 μM, which can also inhibit HIV-1 reverse transcriptase^[1]. Levels of HIV-1 DNA are significantly lower in Gardiquimod trifluoroacetate-treated cells compared 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 peripheral blood mononuclear cells (PBMCs). Gardiquimod trifluoroacetate significantly increased IFN-α mRNA levels 80-, 20-, and 35-fold above the level of detection at 2, 4, and 6 h post treatment, respectively^[1]. Gardiquimod, added prior to or within 2 days after infection with X4, R5, or dual-tropic (R5/X4) strains of HIV-1, significantly reduced infection in macrophages and activated PBMCs. Cocultures of activated PBMCs added to gardiquimod-treated and HIV-1-exposed macrophages demonstrated minimal HIV-1 replication for up to 10 days, suggesting that gardiquimod inhibited activated PBMCs viral amplification from HIV-1-exposed macrophages. Gardiquimod treatment of both activated PBMCs and macrophages induced interferon-alpha (IFN-α) transcription within hours of addition, and sustained IFN-α protein secretion for several days^[1]. On day 12, the tumor volume in mice injected with PBS increased to 1770 ± 370 mm³, whereas it was only 230 ± 70 mm³ in mice treated with Gardiquimod trifluoroacetate^[2].
参考文献

[1] Buitendijk M, Eszterhas SK, Howell 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. Epub 2013 Feb 5. PMID: 23316755; PMCID: PMC3653394.
[2] Ma F, Zhang J, Zhang J, Zhang C. 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. Epub 2010 Jun 14. PMID: 20543857; PMCID: PMC4002679.

实验方案

计算器摩尔计算器总药量计算器工作液计算器
储存液制备
- 1 mg
- 5 mg
- 10 mg
- 1 mM
- 1.8469 mL
- 9.2346 mL
- 18.4691 mL
- 5 mM
- 0.3694 mL
- 1.8469 mL
- 3.6938 mL
- 10 mM
- 0.1847 mL
- 0.9235 mL
- 1.8469 mL

技术信息

CAS号

1159840-61-5

储存条件

粉末: Inert atmosphere,Room Temperature

液体: -20°C:3-6 月 -80°C:12月

分子式

C21H25F6N5O5

运输

蓝冰

分子量

541.44

别名

Gardiquimod TFA salt;Gardiquimod

溶解度

DMSO	95.0 mg/mL (175.5 mM) warming
Water	24.0 mg/mL (44.3 mM) warming

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