TLR7 agonist 22
TLR7 agonist 22 (Compound 11a) emerges as a selective TLR7 agonist with an IC50 value of 25.86 μM. TLR7 agonist 22 inhibits the cellular HBsAg secretion and effectively activates TLR7, thereby inducing the secretion of TLR7-regulated cytokines IL-12, TNF-αand IFN-αin human PBMC cells. TLR7 agonist 22 is a promising for research in the field of developing novel immunomodulatory anti-HBV agents.
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- CAS. Nr.: 3036114-68-5
- Formel: C20H17FN2O2S
- Molecular Weight:368.42
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Speicherung:
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Biologische Aktivität
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HBV DNA 25.86 μM (IC50) |
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Cell Line
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Type | Value | Description | References |
|---|---|---|---|---|
| HepG2 2.2.15 | CC50 |
>50 μM
Compound: 11a
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Cytotoxicity against human HepG2.2.15 cells incubated for 72 hrs by CCK8 assay
Cytotoxicity against human HepG2.2.15 cells incubated for 72 hrs by CCK8 assay
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[PMID: 38865744] |
| HepG2 2.2.15 | IC50 |
25.86 μM
Compound: 11a
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Inhibition of HBsAg secretion in human HepG2.2.15 cells treated for 6 days with replacement of medium containing compound on every 2 days by RT-PCR analysis
Inhibition of HBsAg secretion in human HepG2.2.15 cells treated for 6 days with replacement of medium containing compound on every 2 days by RT-PCR analysis
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[PMID: 38865744] |
TLR7 agonist 22 (4 μM, 72 h) inhibits on HBV DNA replication with an IC50 value of 0.36 μM in HepG2 cells[1]. TLR7 agonist 22 (0.4, 2, 10 μM, 48 h) possesses an agonistic effect on TLR7 and increases TLR7-induced NF-κB activity effectively in HEK293T cells[1]. TLR7 agonist 22 (0.4, 2, 10 μM, 24 h) dose-dependently enhances IL-12, TNF-α and IFN-α production in human PBMC cells[1].
MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.
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Cell Line:HepG2 cells
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Concentration:4 μM
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Incubation Time:72 h
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Result:Exhibited significant inhibitory effect on HBV DNA replication in HepG2 cells.
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Cell Line:HEK293T cells
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Concentration:0.4, 2, 10 μM
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Incubation Time:48 h
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Result:Dose-dependently increased TLR7-induced NF-κB activity effectively in HEK293T cells.
Main pharmacokinetic parameters of TLR7 agonist 22[1]
| AUClast (h·ng/mL) | Cmax (ng/mL) | Tmax (h) | T1/2 (h) |
| 252.30 ± 15.54 | 66.00 ± 11.83 | 2 | 2.00 ± 0.10 |