| 产品描述: | TLR激动剂;TLR Agonists;;InformationMotolimod (VTX-2337) Motolimod (VTX-2337) is a selective and potent Toll-like receptor 8 (TLR8) agonist with EC50 of 100 nM, > 50-fold selectivity over TLR7. Phase 2.TargetsTLR8 100 nM(EC50)In vitroVTX-2337 stimulates the production of both TNFα with EC50 of 140 nM and IL-12 with EC50 of 120 nM in PBMCs. In monocytes and mDCs, VTX-2337 selectively induces the production of TNFα and IL-12 via NF-κB activation. VTX-2337 also stimulates IFNγ production from NK cells, augments the lytic function of NK cells and enhances ADCC.In vivoIn an ovarian cancer mouse model, TX-2337 enhances the effect of pegylated liposomal doxorubicin (PLD).Cell Research(from reference)Cell lines:PBMCs or purified NK cells Concentrations:~500 nM Incubation Time:48 h |
| 体内研究: |
猴子皮下注射 Motolimod (1 或 10 mg/kg),并在给药前、注射后 6、12、24 和 96 小时收集血浆。10 mg/kg Motolimod,IL-1β 的平均血浆水平从 0.5 pg/mL 的基线水平增加,在注射 6 小时后高达 9.12±2.7 ng/mL (p<0.05,t 检验) (10 mg/kg)。IL-18 的循环水平也从 ~1 pg/mL 的基线增加到 68.7±4.4 pg/mL (p<0.05,t 检验)。监测 IL-6 的水平,因为 IL-6 是响应 TLR8 激活而诱导的,但 IL-6 释放与 NLRP3 炎性体激活无关。此外,IFNγ 的血浆水平被评估为 NK 细胞活化对 Motolimod 处理的反应。 |
| 保存条件: |
-80℃(运输条件:冰袋低温运输) |
| 配置溶液浓度参考: |
|
1mg |
5mg |
10mg |
| 1 mM |
2.181 ml |
10.903 ml |
21.805 ml |
| 5 mM |
0.436 ml |
2.181 ml |
4.361 ml |
| 10 mM |
0.218 ml |
1.09 ml |
2.181 ml |
| 50 mM |
0.044 ml |
0.218 ml |
0.436 ml |
|
| 注意: |
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