罗替戈汀
罗替戈汀 性质
| 熔点 | 78 °C |
|---|---|
| 沸点 | 470.1±45.0 °C(Predicted) |
| 密度 | 1.15±0.1 g/cm3(Predicted) |
| 储存条件 | room temp |
| 水溶解性 | Insoluble in water |
| 溶解度 | DMF：30mg/mL； DMF:PBS(pH7.2)(1:2)：0.33mg/ml； DMSO：20mg/mL；乙醇：1mg/mL |
| 酸度系数(pKa) | 10.49±0.40(Predicted) |
| 形态 | 粉末晶体 |
| 颜色 | 白色到近乎白色 |
罗替戈汀 用途与合成方法
| Target | Value |
| Dopamine receptor |
Rotigotine (N-0437; N-0923) has a 10-fold selectivity for D3 (pK
i
9.2) receptors compared with D2, D4 and D5 (pK
i
8.5-8.0) and a 100-fold selectivity compared with D1 receptors (pK
i
7.2). In functional studies, Rotigotine behaves as full agonist at all dopamine receptors but notably the potency for stimulation of D1 receptors is similar to that for D2 and D3 receptors (pEC
50
respectively: 9.0, 9.4-8.6, 9.7).
Rotigotine (10 µM) decreases the number of THir neurons by 40% in primary mesencephalic cell culture. Rotigotine (0.01 µM) slightly protects dopaminergic neurons against MPP
+
toxicity, significantly protects dopaminergic neurons against rotenone-induced cell death, and significantly inhibits ROS production by rotenone.
In primed rats, Rotigotine (N-0437; N-0923; 0.035, 0.1 and 0.35 mg/kg) induces contralateral turning behavior in a dose dependent manner. In drug naive rats, the turning behavior induced by Rotigotine, either alone or in combination with SCH 39166, is reduced compared to primed rats.
罗替戈汀 价格(试剂级)
| 更新日期 | 产品编号 | 产品名称 | CAS号 | 包装 | 价格 |
|---|---|---|---|---|---|
| 2024-01-25 | HY-75502 | 5 mg | 487 | ||
| 2024-01-25 | HY-75502 | 罗替戈汀 | 99755-59-6 | 10mg | 780 |
