產(chǎn)品描述： CD38 inhibitor 1 (compound 78c, CD38-IN-78c, MDK-7553)是一種有效的 CD38 抑制劑，對(duì)人CD38和小鼠CD38的IC50分別為7.3 nM和1.9 nM

靶點(diǎn)： mCD38(Cell-free assay):1.9 nM; hCD38(Cell-free assay):7.3 nM

體外研究：
CD38 inhibitor 1 (compound 78c) increases NAD+ levels, resulting in activation of pro-longevity and health span-related factors including sirtuins, AMPK, and PARPs

體內(nèi)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

細(xì)胞實(shí)驗(yàn)： 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.

動(dòng)物實(shí)驗(yàn)： Animal Models: DIO C57Bl6 mice Dosages: 30 mg/kg, 2 mg/kg Administration: Oral gavage, IV

參考文獻(xiàn)：
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

保存條件： -20℃