| 产品描述: | InformationKY19382 (A3051) is a potent and orally active dual inhibitor of CXXC5-DVL and GSK3β with IC50 of 19 nM and 10 nM, respectively. KY19382 activates Wnt/β-catenin signaling through inhibitory effects on both CXXC5-DVL interaction and GSK3β activity. |
| 体内研究: |
KY19382 (0.1 mg/kg;每天腹腔注射一次,持续 2 周) 可延缓老年小鼠的生长板衰老并促进快速生长的年轻小鼠的生长板成熟。 KY19382 (0.1 mg /kg;腹腔注射;每天一次,持续 10 周) 显著增加小鼠胫骨的长度。 KY19382 (5 mg/kg;ip) 显示出相对有利的生物利用度 (F= 16.74%),半衰期为 16.20 小时,暴露水平为 6,555.79 ng h/mL。 KY19382 (A3051) (25 mg/kg;每日口服一次,持续 16 周) 显示脂肪细胞大小减少和抗炎作用。 A3051 (25 mg/kg;每天口服一次,连续 5 天) 降低小鼠的空腹血糖。 A3051 (25 mg/kg;每天口服一次,持续 3 周) 减少小鼠的肝脂肪变性。 |
| 参考文献: |
1. Choi S, et, al. CXXC5 mediates growth plate senescence and is a target for enhancement of longitudinal bone growth. Life Sci Alliance. 2019 Apr 10; 2(2): e201800254. 2. Choi KY, et, al. Compositions and methods for suppressing and/or treating metabolic diseases and/or a clinical condition thereof. WO2020079569. |
| 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 |
2.776 ml |
13.882 ml |
27.763 ml |
| 5 mM |
0.555 ml |
2.776 ml |
5.553 ml |
| 10 mM |
0.278 ml |
1.388 ml |
2.776 ml |
| 50 mM |
0.056 ml |
0.278 ml |
0.555 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。 |