1. Immunology/Inflammation
  2. Toll-like Receptor (TLR)
  3. 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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TLR7 agonist 22 Chemical Structure

TLR7 agonist 22 Chemical Structure

CAS No. : 3036114-68-5

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Description

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[1].

IC50 & Target

HBV DNA

25.86 μM (IC50)

In Vitro

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.

Real Time qPCR[1]

Cell Line: HepG2 cells
Concentration: 4 μM
Incubation Time: 72 h
Result: Exhibited significant inhibitory effect on HBV DNA replication in HepG2 cells.

Cell Viability Assay[1]

Cell Line: HEK293T cells
Concentration: 0.4, 2, 10 μM
Incubation Time: 48 h
Result: Dose-dependently increased TLR7-induced NF-κB activity effectively in HEK293T cells.
In Vivo

TLR7 agonist 22 (10 MG/KG, i.g.) has a relatively appropriate absorption time and elimination time in male Sprague-Dawley rats[1].

Main pharmacokinetic parameters of TLR7 agonist 22[1]

药代动力学分析[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

MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.

Animal Model: Male Sprague-Dawley rats
Dosage: 10 MG/KG
Administration: i.g., a single dose, measure at 5 min, 15 min, 30 min, 45 min, 1 h, 2 h, 4 h, 6 h, 8 h and 12 h using UPLC-MS/MS
Result: Had a relatively appropriate absorption time and elimination time in mice[1]
Molecular Weight

368.42

Formula

C20H17FN2O2S

CAS No.
SMILES

FC1=C(OCC2=NC(CC(N3CCC4=C3C=CC=C4)=O)=CS2)C=CC=C1

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Storage

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Purity & Documentation
References
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TLR7 agonist 22 Related Classifications

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Help & FAQs
  • Do most proteins show cross-species activity?

    Species cross-reactivity must be investigated individually for each product. Many human cytokines will produce a nice response in mouse cell lines, and many mouse proteins will show activity on human cells. Other proteins may have a lower specific activity when used in the opposite species.

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TLR7 agonist 22
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HY-162579
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