Diprovocim 是一种有效的TLR1/TLR2激动剂。Diprovocim 在人 THP-1 细胞中引发完全激动剂活性 (EC50=110 pM)。Diprovocim 刺激小鼠巨噬细胞释放TNF-α(EC50=1.3 nM)。Diprovocim 激活下游MAPK和NF-κB信号通路。Diprovocim 在小鼠中显示出很强的佐剂活性，尤其是促进细胞免疫反应。
| 生物活性 | Diprovocim is a potentTLR1/TLR2agonist. Diprovocim elicits full agonist activity in human THP-1 cells (EC50=110 pM). Diprovocim stimulates the release ofTNF-αfrom mouse macrophages (EC50=1.3 nM). Diprovocim activates downstreamMAPKandNF-κBsignaling pathway. Diprovocim displays strong adjuvant activity in mice, particularly abetting cellular immune responses[1][2]. |
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体外研究
(In Vitro) | Diprovocim (在 THP-1 细胞中为 5 nM, 在小鼠腹膜巨噬细胞中为 500 nM; 15-120 分钟) 诱导 IKKα、IKKβ、p38、JNK 和 ERK 的磷酸化，以及 IκBα 的降解[2]。
Diprovocim (0.01-10000 nM; 4 小时) 诱导 THP-1 细胞 (EC50=110 pM)、人外周血单核细胞 (PBMC) (EC50=875 pM) 和小鼠腹腔巨噬细胞 (EC50=1.3 nM) 和骨髓来源的树突状细胞 (BMDC) (EC50=6.7 nM) 产生剂量依赖性 TNF。 除 TNF 外，Diprovocim 还诱导小鼠 BMDC 产生 IL-6[2]。
Western Blot Analysis[2] | Cell Line: | THP-1 cells and mouse peritoneal macrophages | | Concentration: | 5 nM in THP-1 and 500 nM in mouse peritoneal macrophages | | Incubation Time: | 15, 30, 60, 120 mins | | Result: | Induced phosphorylation of IKKα, IKKβ, p38, JNK, and ERK, as well as degradation of IκBα. |
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体内研究
(In Vivo) | Diprovocim (10 mg/kg) 用作佐剂，在与卵清蛋白 (OVA; 100 μg) 混合并肌肉注射，14 天后检测发现可以诱导相似水平的血清 OVA 特异性 IgG[2]。
Diprovocim (10 mg/kg) 与卵清蛋白 (OVA; 100 μg) 混合后，在接种 B16-OVA 细胞免疫前进行肌肉注射，可以显着减缓肿瘤生长速度[2]。
| Animal Model: | WT or Tlr2–/–C57BL/6J mice[2] | | Dosage: | 10 mg/kg | | Administration: | IM | | Result: | Induced similar levels of serum OVA-specific IgG, which were highly elevated compared with levels induced by immunization with OVA plus vehicle by i.m. with 100 μg OVA mixed with this drug. |
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| 运输条件 | Room temperature in continental US; may vary elsewhere. |
| 储存方式 | | Powder | -20°C | 3 years | | 4°C | 2 years | | In solvent | -80°C | 6 months | | -20°C | 1 month |
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