| 体内研究: |
Remodelin (2 或 20 mg/kg,腹腔注射,每两天一次,持续 4 周) 显著降低肿瘤异种移植裸鼠模型中 AR 阴性前列腺癌的生长。 Remodelin (100 mg/kg,口服) 在 LmnaG609G/G609G 小鼠早年衰老综合症 (HGPS) 模型中抑制 NAT10 并显著延长健康寿命。 Remodelin (5 mg/kg,口服) 显示在小鼠中 T1/2 为 1.81 小时,口服生物利用度 (F%) 为 43.5%。 Pharmacokinetic parameters for Remodelin in Mice |
| 参考文献: |
1. Larrieu D, et al. Chemical inhibition of NAT10 corrects defects of laminopathic cells. Science. 2014 May 2;344(6183):527-32. 2. Ma N, et.al. Inhibition of N-Acetyltransferase 10 Suppresses the Progression of Prostate Cancer through Regulation of DNA Replication. Int J Mol Sci. 2022 Jun 12;23(12):6573. 3. Balmus G, et.al. Targeting of NAT10 enhances healthspan in a mouse model of human accelerated aging syndrome. Nat Commun. 2018 Apr 27;9(1):1700. 4. Zhang X, et.al. N-Acetyltransferase 10 Enhances Doxorubicin Resistance in Human Hepatocellular Carcinoma Cell Lines by Promoting the Epithelial-to-Mesenchymal Transition. Oxid Med Cell Longev. 2019 Jul 1;2019:7561879. |
| 溶解性: |
10 mM 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 |
3.542 ml |
17.708 ml |
35.415 ml |
| 5 mM |
0.708 ml |
3.542 ml |
7.083 ml |
| 10 mM |
0.354 ml |
1.771 ml |
3.542 ml |
| 50 mM |
0.071 ml |
0.354 ml |
0.708 ml |
|
| 注意: |
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