| 产品描述: | Tavapadon (PF-06649751) is an orally active and highly selective dopamine D1/D5 receptor partial agonist. Tavapadon is effective in enabling movement and reducing disability and has the potential for Parkinson's disease |
| 靶点: |
dopamine D1/D5 receptor;DopamineReceptor |
| 体内研究: |
Tavapadon (PF-06649751; 0.02 and 0.04 mg/kg; s.c.) at the 0.04 mg/kg test dose increases locomotor activity, whereas the 0.02 mg/kg dose has little or no effect. Tavapadon (0.04 mg/kg, s.c.) also improves parkinsonian disability scores with the maximal improvement observed at 110 min after drug administration. Higher doses of Tavapadon (0.1 and 0.15 mg/kg; s.c.) leads to statistically significant improvement relative to vehicle in locomotor activity. Tavapadon (0.1 mg/kg; s.c.) has the mean maximal unbound plasma concentration of 8 nM and achieves 3 hours after compound administration in captive-bred macaques |
| 参考文献: |
1. Young D, et al. D1 Agonist Improved Movement of Parkinsonian Nonhuman Primates with Limited DyskinesiaSide Effects. ACS Chem Neurosci. 2020 Feb 19;11(4):560-566. |
| 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 |
2.555 ml |
12.777 ml |
25.553 ml |
| 5 mM |
0.511 ml |
2.555 ml |
5.111 ml |
| 10 mM |
0.256 ml |
1.278 ml |
2.555 ml |
| 50 mM |
0.051 ml |
0.256 ml |
0.511 ml |
|
| 注意: |
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