1. Immunology/Inflammation
  2. Toll-like Receptor (TLR)
  3. TLR8 antagonist-2

TLR8 antagonist-2 (Compound 35) 是一种选择性的 TLR8 拮抗剂,对 hTLR8 的 IC50 为 0.032 μM。TLR8 antagonist-2 强效抑制 TL8-506 (HY-20457) 刺激细胞中 TLR8 依赖性 NF-κB 活性。TLR8 antagonist-2 可用于炎症和免疫性疾病的相关研究。

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TLR8 antagonist-2

TLR8 antagonist-2 Chemical Structure

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查看 Toll-like Receptor (TLR) 亚型特异性产品:

  • 生物活性

  • 纯度 & 产品资料

  • 参考文献

生物活性

TLR8 antagonist-2 (Compound 35) is a selective TLR8 antagonist with an IC50 of 0.032 μM against hTLR8. TLR8 antagonist-2 potently inhibits TLR8-dependent NF-κB activity in cells stimulated with TL8-506 (HY-20457). TLR8 antagonist-2 can be used in research related to inflammatory and immune diseases[1].

IC50 & Target[1]

hTLR8

0.032 μM (IC50)

体外研究
(In Vitro)

TLR8 antagonist-2 (10 μM) 可强效抑制 TL8-506 刺激的 hTLR8-HEK293 报告细胞中 TLR8 依赖性 NF-κB 活性,其 IC50 为 0.032 μM[1]
TLR8 antagonist-2 (1 h) 可强效抑制 TL8-506 诱导的 TNF 分泌,在 THP-1 巨噬细胞中的 IC50 值为 0.014 μM,在 PBMC 中的 IC50 值为 0.107 μM[1]
TLR8 antagonist-2 强效抑制 TL8-506 刺激 THP-1 巨噬细胞产生的细胞应答,其 IC50 为 0.0022 μM[1]
TLR8 antagonist-2 在小鼠肝微粒体中的半衰期为 73.6 min[1]

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

ELISA Assay[1]

Cell Line: THP-1 macrophages, human peripheral blood mononuclear cells (PBMCs)
Concentration: 0.014 μM (THP-1 TNF IC50); 0.107 μM (PBMC TNF IC50); 1 μM (IL-8 inhibition); up to 50 μM (cytotoxicity test)
Incubation Time: 1 h (preincubation); 4 h (agonist stimulation)
Result: Demonstrated concentration-dependent inhibition of TNF secretion, with an IC50 of 0.014 μM in THP-1 macrophages and 0.107 μM in PBMCs.
Completely inhibited TL8-506-induced IL-8 secretion at 1 μM in both cell types.
Showed no cytotoxicity detected up to 50 μM via LDH assay.
分子量

418.53

Formula

C25H30N4O2

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
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  • 稀释计算器

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The dilution calculator equation

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

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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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产品名称:
TLR8 antagonist-2
目录号:
HY-183276
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