生物活性
Cycloleucine is antagonist of NMDA receptor associated glycine receptor, with a Ki of 600 μM. Cycloleucine is a specific inhibitor of S-adenosyl-methionine mediated methylation. Cycloleucine is also a competitive inhibitor of ATP: L-methionine-S-adenosyl transferase in vitro. Cycloleucine (4-40 mM) 3 hours blocks internal methylation of viral RNA in B77 transformed chick embryo fibroblasts.
In vivo,
Cycloleucine (0.5-4 μg; intracerebroventrical injection) increases time spent in open arms, open arm entries, and extreme arrivals in rats. Cycloleucine reduces thymus and spleen weights in Semliki Forest virus (SFV) strain A7(74) infected and control mice.
化学数据
分子量 | 129.16 |
分子式 | C6H11NO2 |
CAS号 | 52-52-8 |
纯度 | >98% |
溶解性(25°C) | Water 50 mg/mL |
储存和运输条件 | -20°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 | 7.7423 mL | 38.7117 mL | 77.4234 mL |
5 mM | 1.5485 mL | 7.7423 mL | 15.4847 mL |
10 mM | 0.7742 mL | 3.8712 mL | 7.7423 mL |