生物活性
Quinidine 是一种抗心律失常剂,也是 K+ 通道 (K+ channel) 的有效阻断剂,其 IC50 值为 19.9 μM。Quinidine is a stereoisomer of quinine, originally derived from the bark of the cinchona tree. Quinidine is used to treat abnormal heart rhythms. Like all other class I antiarrhythmic agents, quinidine primarily works by blocking the fast inward sodium current. At micromolar concentrations, quinidine inhibits Na+/K+-ATPase by binding to the same receptor sites as the digitalis glycosides such as ouabain. Quinidine is also used to treat malaria. The half life of oral quinidine is 6 to 8 hours, and it is eliminated by the cytochrome P450 system in the liver. About 20% is excreted unchanged via the kidneys. Quinidine is also an inhibitor of the cytochrome P450 enzyme 2D6, and can lead to increased blood levels of lidocaine, Beta blockers, opioids, and some anti-depressants. Quinidine also inhibits the transport protein P-glycoprotein and so can cause some peripherally acting drugs such as loperamide to have CNS side effects such as respiratory depression if the two drugs are co-administered.
化学数据
分子量 | 324.42 |
分子式 | C20H24N2O2 |
CAS号 | 56-54-2 |
纯度 | >98% |
溶解性(25°C) | DMSO 50 mg/mL |
储存和运输条件 | 2-8°C, protect from light, sealed 常温运输及临时存放 |
不同实验动物依据体表面积的等效剂量转换表(数据来源于FDA指南)
| 小鼠 | 大鼠 | 兔 | 豚鼠 | 仓鼠 | 狗 |
重量 (kg) | 0.02 | 0.15 | 1.8 | 0.4 | 0.08 | 10 |
体表面积 (m2) | 0.007 | 0.025 | 0.15 | 0.05 | 0.02 | 0.5 |
Km系数 | 3 | 6 | 12 | 8 | 5 | 20 |
动物 A (mg/kg) = 动物 B (mg/kg) × | 动物 B的Km系数 |
动物 A的Km系数 |
例如,依据体表面积折算法,将化合物用于小鼠的剂量20 mg/kg 换算成大鼠的剂量,需要将20 mg/kg 乘以小鼠的Km系数(3),再除以大鼠的Km系数(6),得到化合物用于大鼠的等效剂量为10 mg/kg。
储备液配制
以下数据基于产品分子量,对于特殊产品,请参照COA中的储备液配制条件和说明进行操作。
Concentration / Solvent Volume / Mass | 1 mg | 5 mg | 10 mg |
---|
1 mM | 3.0824 mL | 15.4121 mL | 30.8242 mL |
5 mM | 0.6165 mL | 3.0824 mL | 6.1648 mL |
10 mM | 0.3082 mL | 1.5412 mL | 3.0824 mL |