| 产品描述: | CD38 inhibitor 1 (compound 78c, CD38-IN-78c, MDK-7553)是一种有效的 CD38 抑制剂,对人CD38和小鼠CD38的IC50分别为7.3 nM和1.9 nM |
| 靶点: |
mCD38(Cell-free assay):1.9 nM; hCD38(Cell-free assay):7.3 nM;CD38 |
| 体外研究: |
CD38 inhibitor 1 (compound 78c) increases NAD+ levels, resulting in activation of pro-longevity and health span-related factors including sirtuins, AMPK, and PARPs |
| 体内研究: |
CD38 inhibitor 1 (compound 78c) is found to not only be a very potent inhibitor, but also had suitable physiochemical properties to serve as a robust tool for in vivo studies. In addition, CD38 inhibitor 1 (compound 78c) is able to elevate NAD in both liver and gastrocnemius tissue when dosed orally in a DIO mouse |
| 细胞实验: |
Cell lines: HEK293T, MEFs, A549, Jurkat T and AML12 cells Concentrations: 0.5 μM, 0.2 - 0.5 μM Incubation Time: 16 h, 24 h Method: To test the reversibility of the CD38i, A549 cells were treated with vehicle or 0.5 μM 78c for 16 hours. Then, cells were washed and incubated with (78c) or without (78c+release) 78c for another 8 hours. |
| 动物实验: |
Animal Models: DIO C57Bl6 mice Dosages: 30 mg/kg, 2 mg/kg Administration: Oral gavage, IV |
| 参考文献: |
1. Curt D Haffner, et al. Discovery, Synthesis, and Biological Evaluation of Thiazoloquin(az)olin(on)es as Potent CD38 Inhibitors. J Med Chem. 2015 Apr 23;58(8):3548-71. 2. Mariana G Tarragó, et al. A Potent and Specific CD38 Inhibitor Ameliorates Age-Related Metabolic Dysfunction by Reversing Tissue NAD+ Decline. Cell Metab. 2018 May 1;27(5):1081-1095.e10. |
| 溶解性: |
Soluble in DMSO |
| 保存条件: |
-20℃ |
| 配置溶液浓度参考: |
|
1mg |
5mg |
10mg |
| 1 mM |
2.418 ml |
12.091 ml |
24.182 ml |
| 5 mM |
0.484 ml |
2.418 ml |
4.836 ml |
| 10 mM |
0.242 ml |
1.209 ml |
2.418 ml |
| 50 mM |
0.048 ml |
0.242 ml |
0.484 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。 |