TLR7/8 agonist 1

MCE 国际站：TLR7/8 agonist 1

CAS：1258457-59-8

品牌：MedChemExpress (MCE)

存储条件：4°C, protect from light *In solvent : -80°C, 6 months; -20°C, 1 month (protect from light)

生物活性：TLR7/8 agonist 1是一种 toll 样受体 (TLR7)/TLR8 的双重激动剂。

体外：TLR7/8 agonist 1 (Compound 5d) shows prominent immunostimulatory activities. TLR7/8 agonist 1 serves as a convenient precursor for the covalent attachment of fluorophores without significant loss of activity.TLR7/8 agonist 1 retains TLR7-agonistic activity with an EC50 of 20 nM. TLR7/8 agonist 1 is covalently coupled directly to commercially-available fluorescein isothiocyanate and rhodamine B isothiocyanate[1]. TLR7/8 agonist 1 (Compound 1) shows substantially different agonistic potencies in human TLR7 (50 nM) and TLR8 (55 nM) primary screens[2]. MCE has not independently confirmed the accuracy of these methods. They are for reference only.

激酶试验：使用人类 TLR-2、TLR3、TLR4、TLR5、TLR7、TLR8、TLR9 和 NOD-1/NOD-2 特异性、快速通量、液体处理机辅助报告基因检测对 NF-κB 的诱导进行定量。 HEK293 细胞与适当的 hTLR（或 NOD）和分泌的碱性磷酸酶（sAP）稳定共转染，维持在 HEK-Blue 选择培养基中。适当的 TLR/NOD 激动剂可诱导 NF-κB/AP-1 启动子控制下的分泌型碱性磷酸酶 (sAP) 的稳定表达，并且上清液中的细胞外 sAP 与 NF-κB 诱导成正比。报告细胞以约 105 个细胞/mL 的密度、80 μL/孔的体积在 384 孔平底细胞培养处理的微量滴定板中在分级浓度的刺激存在下孵育。使用碱性磷酸酶特异性色原（存在于 HEK 检测介质中）在 620 nm 处通过分光光度法测定 sAP[2]。

细胞试验：新鲜人外周血单核细胞 (hPBMC) 在知情同意的情况下从静脉穿刺获得的人血液中分离出来，并按照聚蔗糖-泛影葡胺梯度的机构指南进行。用分级浓度的测试化合物（例如，TLR7/8激动剂1；0.1、1、10和100μg/mL）刺激PBMC的等分试样（100μL/孔中105个细胞）12小时。通过离心分离上清液，并使用分析物特异性多重细胞因子/趋化因子珠阵列分析进行重复分析[2]。

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研究领域：Immunology/Inflammation

作用靶点：Toll-like Receptor (TLR)

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参考文献：[1]. Shukla NM, et al. Syntheses of fluorescent imidazoquinoline conjugates as probes of Toll-like receptor 7. Bioorg Med Chem Lett. 2010 Nov 15;20(22):6384-6.[2]. Beesu M, et al. Structure-Based Design of Human TLR8-Specific Agonists with Augmented Potency and Adjuvanticity. J Med Chem. 2015 Oct 8;58(19):7833-49.