产品说明书
Gardiquimod diTFA
 |
同义名 : | GArdiquimod trifluoroacetate |
| CAS号 : | 1159840-61-5 | |
| 货号 : | A724317 | |
| 分子式 : | C21H25F6N5O5 | |
| 纯度 : | 99%+ | |
| 分子量 : | 541.444 | |
| MDL号 : | MFCD31619251 | |
| 存储条件： |
粉末 Inert atmosphere,Room Temperature 液体 -20°C:3-6个月-80°C:12个月 |
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| 溶解度 : |
DMSO: 50 mg/mL(92.35 mM)，配合低频超声助溶，注意：DMSO长时间开封后，会吸水并导致溶解能力下降，请避免使用长期开封的DMSO H2O: 25 mg/mL(46.17 mM)，配合低频超声助溶 |
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| 动物实验配方： |
| 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]. | ||
| 实验方案 | |||
|---|---|---|---|
| 1mg | 5mg | 10mg | |
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1 mM 5 mM 10 mM |
1.85mL 0.37mL 0.18mL |
9.23mL 1.85mL 0.92mL |
18.47mL 3.69mL 1.85mL |
| 参考文献 |
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