| 产品描述: | CZC-25146是代谢稳定性的LRRK2抑制剂,对野生型LRRK2和G2019S LRRK2的IC50分别为4.76 nM和6.87 nM。 |
| 靶点: |
IC50: 4.76 nM (wild-type LRRK2), 6.87 nM (G2019S LRRK2) |
| 体内研究: |
CZC-25146 (250 mg/kg;口服;14 天) 降低过度表达人类聚合物 ATZ 小鼠的 ATZ 聚合物水平。 CZC-25146 (1 mg/kg 用于静脉注射;5 mg/kg for 口服,单词给药) 表现出相对良好的药代动力学特性,并在小鼠静脉注射后广泛分布于整个动物体内。 |
| 参考文献: |
1. Ramsden N, et al. Chemoproteomics-based design of potent LRRK2-selective lead compounds that attenuate Parkinson's disease-related toxicity in human neurons. ACS Chem Biol. 2011 Oct 21;6(10):1021-8. 2. Atashrazm F, et al. LRRK2 inhibitors and their potential in the treatment of Parkinson's disease: current perspectives. Clin Pharmacol. 2016 Oct 20;8:177-189. 3. Deniz Kent, et al. Small molecule screen employing patient-derived iPS hepatocytes identifies LRRK2 as a novel therapeutic target for Alpha1 Antitrypsin Deficiency. |
| 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 |
2.047 ml |
10.235 ml |
20.469 ml |
| 5 mM |
0.409 ml |
2.047 ml |
4.094 ml |
| 10 mM |
0.205 ml |
1.023 ml |
2.047 ml |
| 50 mM |
0.041 ml |
0.205 ml |
0.409 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。 |