生物活性
Tetracaine hydrochloride (Pontocaine) is a hydrochloride salt form of tetracaine which is a potent local anaesthetic and a channel function allosteric inhibitor. Tetracaine hydrochloride (Pontocaine) is used to block temporarily the pain "message" that is sent along the nerves that connect the eyes to the brain. Tetracaine hydrochloride (Pontocaine) is mainly used topically in ophthalmology and as an antipruritic, and it has been used in spinal anesthesia. In biomedical research, tetracaine is used to alter the function of calcium release channels (ryanodine receptors) that control the release of calcium from intracellular stores. In addition, tetracaine serves as an allosteric blocker of channel function. At low concentrations, tetracaine gives rise to an initial prevention of spontaneous calcium release events, while at high concentrations, tetracaine blocks release completely.
化学数据
分子量 | 300.82 |
分子式 | C15H24N2O2.HCl |
CAS号 | 136-47-0 |
纯度 | >98% |
溶解性(25°C) | DMSO 50 mg/mL |
储存和运输条件 | 固体粉末: -20°C 冷藏长期储存 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 | 3.3242 mL | 16.6212 mL | 33.2425 mL |
5 mM | 0.6648 mL | 3.3242 mL | 6.6485 mL |
10 mM | 0.3324 mL | 1.6621 mL | 3.3242 mL |