| 产品描述: | PDE4B-IN-2 is an orally active and selective PDE4B inhibitor with an IC50 of 15 nM. PDE4B-IN-2 inhibits PDE4D (IC50=1.7 µM). PDE4B-IN-2 exhibits potent anti-inflammatory effects |
| 靶点: |
PDE4B:15 nM (IC50);PDE4D:1.7 μM (IC50) |
| 体外研究: |
PDE4B-IN-2 (compound 33) does not inhibit CYP1A2, CYP3A4, CYP2C9, and CYP2D (IC50>10 µM). PDE4B-IN-2 inhibits LPS-induced TNF-aproduction in vitro from mouseperipheral blood mononuclear cell (PBMC; IC50=0.5 M). |
| 体内研究: |
PDE4B-IN-2 (compound 33; 2 mg/kg; po) has a Cmax of 8.7 μg/mL and an AUC of 52.3 μg•h/mL in mice. |
| 参考文献: |
1. Kenji Naganuma, et al. Discovery of selective PDE4B inhibitors. Bioorg Med Chem Lett. 2009 Jun 15;19(12):3174-6. |
| 溶解性: |
soluble in DMSO |
| 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 |
2.578 ml |
12.891 ml |
25.781 ml |
| 5 mM |
0.516 ml |
2.578 ml |
5.156 ml |
| 10 mM |
0.258 ml |
1.289 ml |
2.578 ml |
| 50 mM |
0.052 ml |
0.258 ml |
0.516 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。 |