| 产品描述: | RO8191 (CDM-3008) 是一种咪唑啉并吡啶化合物,是具有口服活性的,有效的干扰素 (IFN) 受体激动剂。RO8191 直接与 IFNα/β 受体 2 (IFNAR2) 结合,激活 IFN 刺激的基因 (ISGs) 表达和 JAK/STAT 磷酸化。RO8191 对 HCV 和 EMCV 均显示抗病毒活性,对 HCV 复制子的 IC50 为 200 nM。RO8191 通过具有干扰素样活性发挥 cccDNA 调节剂 (CDM) 作用,并具有抗 HBV 活性。
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| 靶点: |
JAK1 |
| 体外研究: |
RO8191 (CDM-3008) exerts antiviral activity dependent on IFNAR2/JAK1, but is independent of IFNAR1/Tyk2. RO8191, an IFNAR2 agonist, stimulates IFN signals in mice[1]. RO8191 (0.08, 0.4, 2, 10 μM; for 72 h) strongly suppresses HCV replicon activity at 72 h in a dose-dependent manner. RO8191 reduces levels of the proteins HCV NS3 and NS4A, which are localized mainly in the perinuclear region of the replicon cells[1]. RO8191 (0.08-10 μM; for 72 h) results in the disappearance of viral proteins such as NS3, NS4A/B, and NS5A/B[1]. |
| 体内研究: |
RO8191 (CDM-3008; 30 mg/kg; oral) significantly induces antiviral genes Oas1b, Mx1, and Pkr in the livers of six-week-old C57BL/6J mice[1]. |
| 参考文献: |
[1]. Hideyuki Konishi, et al. An Orally Available, Small-Molecule Interferon Inhibits Viral Replication. Sci Rep. 2012;2:259. [Content Brief]
[2]. Yutaka Furutani, et al. An interferon-like small chemical compound CDM-3008 suppresses hepatitis B virus through induction of interferon-stimulated genes. PLoS One. 2019 Jun 12;14(6):e0216139. [Content Brief] |
| 溶解性: |
DMSO : 5 mg/mL (13.40 mM; ultrasonic and warming and heat to 60°C) |
| 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 |
2.679 ml |
13.397 ml |
26.795 ml |
| 5 mM |
0.536 ml |
2.679 ml |
5.359 ml |
| 10 mM |
0.268 ml |
1.34 ml |
2.679 ml |
| 50 mM |
0.054 ml |
0.268 ml |
0.536 ml |
|
| 注意: |
部分产品我司仅能提供部分信息,我司不保证所提供信息的权威性,仅供客户参考交流研究之用。 |