| 产品描述: | ITI-214 is a potent, CNS-active, orally bioavailable PDE1 inhibitor (Ki of 58 pM) with excellent selectivity against other PDE family members and against a panel of enzymes, receptors, transporters and ion channels. ITI-214 inhibits recombinant full-length human PDE1A, PDE1B and PDE1C with Kis of 33 pM, 380 pM and 35 pM, respectively. ITI-214 shows efficacy in various animal models of motor and cognitive functions |
| 靶点: |
PDE1:58 pM (Ki);PDE1A:33 pM (Ki);PDE1B:380 pM (Ki);PDE1C:35 pM (Ki);PDE |
| 体外研究: |
ITI-214 expresses >1000-fold greater activity toward PDE1 isoforms compared with the next nearest PDE family enzyme, PDE4D (Ki= 33 nM) and 10,000-300,000-fold selectivity toward all other PDE enzyme families |
| 体内研究: |
ITI-214 significantly enhances memory performance in the test with a minimum effective dose of 3 mg/kg. Animal Model: Male Sprague-Dawley rats Dosage: 0.1-10 mg/kg Administration: p.o. Result: Significantly enhanced memory performance in the test with a minimum effective dose of 3 mg/kg. |
| 参考文献: |
1. Li P, et al. Discovery of Potent and Selective Inhibitors of Phosphodiesterase 1 for the Treatment of Cognitive Impairment Associated with Neurodegenerative and Neuropsychiatric Diseases. J Med Chem. 2016;59(3):1149-1164. 2. Snyder GL, et al. Preclinical profile of ITI-214, an inhibitor of phosphodiesterase 1, for enhancement of memory performance in rats. Psychopharmacology (Berl). 2016;233(17):3113-3124. |
| 溶解性: |
soluble in DMSO |
| 保存条件: |
-20℃ |
| 配置溶液浓度参考: |
|
1mg |
5mg |
10mg |
| 1 mM |
1.651 ml |
8.257 ml |
16.514 ml |
| 5 mM |
0.33 ml |
1.651 ml |
3.303 ml |
| 10 mM |
0.165 ml |
0.826 ml |
1.651 ml |
| 50 mM |
0.033 ml |
0.165 ml |
0.33 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。 |