生物活性
Equisetin is a tetramic acid analog derived fromFusarium equisti.Equisetin is mainly known for its antibiotic and cytotoxic activity and for its inhibitory effect on HIV-1 integrase. Inhibition of HIV integrase by Equisetin was reported with IC50values of 5-20 μM. Moreover, it was shown that Equisetin specifically inhibits the substrate anion carriers of the inner membrane of mitochondria and acts nonspecifically on protein membranes and protein hydrophobic domains. In addition, it was demonstrated that Equisetin causes phytotoxicity by causing root Necrosis and was also identified in a mycotoxin cocktail associated with cattle feeding problems.
化学数据
分子量 | 373.49 |
分子式 | C22H31NO4 |
CAS号 | 57749-43-6 |
纯度 | >98% |
溶解性(25°C) | DMSO: soluble 1 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 | 2.6774 mL | 13.3872 mL | 26.7745 mL |
5 mM | 0.5355 mL | 2.6774 mL | 5.3549 mL |
10 mM | 0.2677 mL | 1.3387 mL | 2.6774 mL |