| 产品描述： | AZD7986 is a Dipeptidyl peptidase 1 (DPP1) inhibitor (pIC50s: 6.85, 7.7, 7.6, 7.8, and 7.8 in human, rat, mouse, rabbit, and dog, respectively). |
| 靶点： |
Proteasome |
| 体内研究： |
AZD7986 shows good stability in plasma, with a half-life of >10 h. AZD7986 inhibits activation of Pr3 and NE, but not CatG, in bone marrow cell lysates in a dose-dependent manner in vivo. |
| 细胞实验： |
Cellular potency is studied using the DPP1-expressing monocytic U937 cell line. Briefly, cells grown in RPMI are plated on 384-well polypropylene v-bottom plates at a density of 5×10^5 cells/mL per well. Added to this is 10 μL of AZD7986 at 37°C for 60 min, followed by 350 μM Gly-Phe-AFC. The well fluorescence is read using a multilabel plate reader. Data are analyzed to calculate pIC50 values. |
| 动物实验： |
Rats are used for the in vivo study. Naive rats are dosed orally twice daily with AZD7986 at 0.2, 2, and 20 mg/kg/day for 8 days. At termination, bone marrow is taken by femural aspiration for neutrophil serine proteases activity analysis using commercial synthetic peptide substrates. |
| 参考文献： |
1. Doyle K, et al. Discovery of Second Generation Reversible Covalent DPP1 Inhibitors Leading to an Oxazepane Amidoacetonitrile Based Clinical Candidate (AZD7986). J Med Chem. 2016 Oct 27;59(20):9457-9472. |
| 溶解性： |
Soluble in DMSO |
| 保存条件： |
-20℃ |
| 配置溶液浓度参考： |
|
1mg |
5mg |
10mg |
| 1 mM |
2.378 ml |
11.892 ml |
23.783 ml |
| 5 mM |
0.476 ml |
2.378 ml |
4.757 ml |
| 10 mM |
0.238 ml |
1.189 ml |
2.378 ml |
| 50 mM |
0.048 ml |
0.238 ml |
0.476 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。 |
上海工商
危险品化学品经营许可证（不带存储）
营业执照(三证合一)
北京