| 产品描述: | TP-10 is a selective PDE10A inhibitor with an IC50 value of 0.8 nM. TP-10 shows an antioxidant activity with IC50s of 31.72 and 16.04 μg/ml for DPPH and CUPRAC, respectively. TP-10 can be used for the research of neuropathy |
| 靶点: |
IC50: 0.8 nM (PDE10A), 31.72 μg/mL (DPPH), 16.04 μg/mL (CUPRAC);PDE |
| 体内研究: |
TP-10 (0.1-10 mg/kg; i.h. once) shows an effect on cyclic nucleotides. Animal Model: Male CD rats Dosage: 0.1, 0.32, 1.0, 3.2 and 10 mg/kg Administration: Subcutaneous injection; 0.1-10 mg/kg once Result: Dose- and time-dependently increased the levels of both cGMP and cAMP in striatal of mice. Increased pCREB-LI level first and returned to basal levels after injected for 3 hours at a dose of 3.2 mg/kg. |
| 参考文献: |
1. Hamaguchi W, et al. Synthesis and in vivo evaluation of novel quinoline derivatives as phosphodiesterase 10A inhibitors. Chem Pharm Bull (Tokyo). 2014;62(12):1200-1213. 2. Schmidt CJ, et al. Preclinical characterization of selective phosphodiesterase 10A inhibitors: a new therapeutic approach to the treatment of schizophrenia. J Pharmacol Exp Ther. 2008 May;325(2):681-90. 3. Kaproń B, et al. 1,2,4-Triazole-based anticonvulsant agents with additional ROS scavenging activity are effective in a model of pharmacoresistant epilepsy. J Enzyme Inhib Med Chem. 2020 Dec;35(1):993-1002. |
| 溶解性: |
Soluble in DMSO |
| 保存条件: |
2-8℃ |
| 配置溶液浓度参考: |
|
1mg |
5mg |
10mg |
| 1 mM |
2.174 ml |
10.87 ml |
21.739 ml |
| 5 mM |
0.435 ml |
2.174 ml |
4.348 ml |
| 10 mM |
0.217 ml |
1.087 ml |
2.174 ml |
| 50 mM |
0.043 ml |
0.217 ml |
0.435 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。 |