S89293 |
MDK-7553 |
源叶(MedMol) | 98% |
- 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
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质量 (mg) = 浓度 (mM) x 体积 (mL) x 分子摩尔量 (g/mol)