2. Immunology/Inflammation Apoptosis
  3. Toll-like Receptor (TLR) Interleukin Related IFNAR TNF Receptor
  4. TLR7/8 agonist 14

TLR7/8 agonist 14 是一种 TLR7 和 TLR8 双靶点激动剂。TLR7/8 agonist 14 对 TLR7 和 TLR8 的 EC50 值分别为 75 μM和 96 μM。TLR7/8 agonist 14 能够促进促炎细胞因子 TNF-α、 IL-1β、 IL-8 及 IFN-γ 的分泌，同时增强细胞因子分泌和 CD86 表达水平。 TLR7/8 agonist 14 可用于结直肠癌相关研究。

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TLR7/8 agonist 14

TLR7/8 agonist 14 Chemical Structure

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TLR7/8 agonist 14 相关抗体

Top Publications Citing Use of Products

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TLR3 TLR8 TLR9 TLR2 TLR4 TLR7 TLR1 TLR6

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TNFRSF1A/CD120a TNFRSF3/CD18 TNFRSF4 TNFRSF5/CD40 TNFRSF6/Fas/CD95 TNFRSF7/CD27 TNFRSF8/CD30 TNFRSF9/4-1BB/CD137 TNFRSF12A/TWEAK TNFRSF16/NGF Receptor/CD271 TNFRSF18/GITR/CD357

  • 生物活性

  • 纯度 & 产品资料

  • 参考文献

生物活性

TLR7/8 agonist 14 is a TLR7 and TLR8 agonist with EC50 values of 0.53 μM and 4.3 μM, respectively. TLR7/8 agonist 14 increases the secretion of the proinflammatory cytokines TNF-α, IL-1β, IL-8 and IFN-γ. TLR7/8 agonist 14 increases cytokine secretion and expression of CD86. LR7/8 agonist 14 can be used for research colorectal carcinoma[1].

IC50 & Target[1]

TLR7

0.53 μM (EC50)

TLR8

4.3 μM (EC50)

IL-1β

 

IL-8

 

TNF-α

 

体外研究
(In Vitro)

TLR7/8 agonist 14 (compound 69) (1-5 μM, 24 h) 在体外细胞中具有免疫调节特性[1]。
TLR7/8 agonist 14 (5 μM, 24 h) 在未成熟树突状细胞中可作为促进适应性抗肿瘤免疫发展的佐剂候选分子[1]。
TLR7/8 agonist 14 (20 μM) 可激活下游 MyD88 依赖性信号通路，导致 THP-1 细胞中 AP-1 的活化，并诱导 MEK-1、p38、IκB 和 ERK1/2 的磷酸化，进而激活下游信号通路[1]。
TLR7/8 agonist 14 (10 mM, 1 h) 在人肝微粒体中的半衰期 t₁/₂ 为 5.6 min，微粒体内在清除率 CLint (mic) 为 246.9 μL/min/mg，肝内在清除率CLint (liver) 为 222.2 ml/min/kg[1]。

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

TLR7/8 agonist 14 相关抗体:

ELISA Assay[1]

Cell Line: Human peripheral blood mononuclear cells (PBMCs)
Concentration: 1 μM; 5 μM
Incubation Time: 24 h
Result: Increased the secretion of the inflammatory cytokines TNF-α, IL-1β, and IL-8.
Increase IL-6 slightly.

Immunofluorescence[1]

Cell Line: Immature dendritic cells
Concentration: 5 μM
Incubation Time: 24 h
Result: Increased CD86 expression.
体内研究
(In Vivo)

TLR7/8 agonist 14 (compound 69) (2.5-10 mg/kg，皮下注射，单次或于第 1、2、4 天三次瘤内给药) 在结直肠癌同系小鼠模型 (CT26) 中展现出潜在的抗肿瘤活性且未出现全身毒性[1]。

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

Animal Model: CT26 murine colorectal carcinoma cells (0.3 × 106 in 100 μL of sterile 0.9 % NaCl, s.c.) induced female BALB/c mice (8-10 weeks, 19-21 g)[1]
Dosage: 2.5, 5, or 10 mg/kg
Administration: s.c., 2.5 mg/kg single injection, 5 mg/kg single injection, 10 mg/kg single injection, 2.5 mg/kg triple injections, 5 mg/kg triple injections, 10 mg/kg triple injections.
Result: Had a dose-and frequency-dependent inhibition of tumor growth.
Suppressed tumor growth and increased survival time (10 mg/kg triple injections).
Resulted in a modest delay in tumor growth (approximately 3 days).
Resulted in a robust and statistically significant suppression of tumor growth.
Resulted in 8 days of tumor growth delay.
Resulted a 2.7-fold increase at the highest dose tested.
Resulted also in significantly increased survival of mice.
分子量

322.83

Formula

C17H23ClN2O2
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

TLR7/8 agonist 14 相关分类

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The dilution calculator equation

Concentration (start) × Volume (start) = Concentration (final) × Volume (final)

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× = ×
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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.

Keywords:

TLR7/8 agonist 14Toll-like Receptor (TLR)Interleukin RelatedIFNARTNF ReceptorILInterferon-α/β receptorInterferon-alpha/beta receptor Tumor Necrosis Factor ReceptorTNFRviral infectionsautoimmune diseasescolorectal carcinomaTLR7TLR8Inhibitorinhibitorinhibit

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