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

TLR7 agonist 22 (Compound 11a) 是可选择性的 TLR7 激动剂，其 IC50 值为25.86 μM。TLR7 agonist 22 抑制细胞HBsAg 的分泌，有效激活 TLR7，从而诱导人类 PBMC 细胞中 TLR7 调控的细胞因子 IL-12，TNF-α 和 IFN-α 的分泌。TLR7 agonist 22 有希望用于开发新型免疫调节抗 HBV 药物的领域研究。

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TLR7 agonist 22 Chemical Structure

TLR7 agonist 22 Chemical Structure

CAS No. : 3036114-68-5

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TLR7 agonist 22 相关抗体

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  • 生物活性

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生物活性

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)

体外研究
(In Vitro)

TLR7 agonist 22 (4 μM, 72h) 在 HepG2 细胞中抑制 HBV DNA 复制，其 IC50 值为 0.36 μM[1]。
TLR7 agonist 22 (0.4, 2, 10 μM, 48 h) 具有 TLR7 激动效应，并有效增加 TLR7 诱导的 NF-κB 活性[1]。
TLR7 agonist 22 (0.4, 2, 10 μM, 24 h) 剂量依赖性增强人类PBMC细胞中 IL-12、TNF-α 和 IFN-α 的产生[1]。

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

TLR7 agonist 22 相关抗体:

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.
体内研究
(In Vivo)

TLR7 agonist 22 (10 MG/KG, i.g.) 在雄性 Sprague-Dawley 大鼠中具有相对适当的吸收时间和消除时间[1]。

TLR7激动剂22的主要药代动力学参数[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

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]
分子量

368.42

Formula

C20H17FN2O2S
CAS 号
运输条件

Room temperature in continental US; may vary elsewhere.
储存方式

Please store the product under the recommended conditions in the Certificate of Analysis.
纯度 & 产品资料
参考文献

TLR7 agonist 22 相关分类

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  • 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.

Keywords:

TLR7 agonist 223036114-68-5Toll-like Receptor (TLR)Human PBMC cellsHBV deseaseHBsAg secretion inhibitionHBV replicationInhibitorinhibitorinhibit

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