生物活性
Terbinafine hydrochloride (Lamisil) is a hydrochloride salt of terbinafine that is a synthetic allylamine antifungal and a squalene epoxidase inhibitor with an IC50 of 30 nM for Candida albicans.?Terbinafine hydrochloride (Lamisil) is highly lipophilic in nature and tends to accumulate in skin, nails, and fatty tissues. Like other allylamines, terbinafine hydrochloride (Lamisil) inhibits ergosterol synthesis by inhibiting squalene epoxidase, an enzyme that is part of the fungal cell membrane synthesis pathway. Because terbinafine hydrochloride (Lamisil) prevents conversion of squalene to lanosterol, ergosterol cannot be synthesized. This is thought to change cell membrane permeability, causing fungal cell lysis. At 90-120 uM, terbinafine exhibits antitumor and antiangiogenic activity by inducing cell cycle arrest at the G0/G1 stage in COLO 205 tumor cells and human vascular endothelia cells.
化学数据
分子量 | 327.89 |
分子式 | C21H25N.HCl |
CAS号 | 78628-80-5 |
纯度 | 100.0% |
溶解性(25°C) | DMSO 60 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 | 3.0498 mL | 15.249 mL | 30.498 mL |
5 mM | 0.61 mL | 3.0498 mL | 6.0996 mL |
10 mM | 0.305 mL | 1.5249 mL | 3.0498 mL |