生物活性
RSV604 (RSV-604) is a cell-permeable, non-cytotoxic (CC50 >50 μM) benzodiazepine derivative that is reported to target respiratory syncytial virus (RSV) nucleoprotein (N) via affinity interaction (Kd = 134 μM) and display similar antiviral potency against 40 clinical human RSV isolates (Ave. EC50= 800 nM), including both subtypes A and B. Although RSV604 displays host-dependent potency against RSV cellular replication (EC50= 2 μM/HeLa, 1.8 μM/HEp-2, >50 μM/BHK-21 based on cellular viral F protein level 72 hrs post RSV A2 infection) and release (by >1,000,000-fold/HeLa vs. no effect/BHK-21 72 hrs post infection; [RSV604] = EC90), complete loss of infectivity of released RSV from RSV604-treated cells is observed in both HeLa and BHK-21 cultures. RSV604 is also active against bovine RSV, but inactive toward mouse pneumonia virus, human metapneumovirus or parainfluenza virus types 1 &3 (PIV1 &PIV3).
化学数据
| 分子量 | 388.39 |
| 分子式 | C22H17FN4O2 |
| CAS号 | 676128-63-5 |
| 纯度 | >98% |
| 溶解性(25°C) | DMSO: 20 mg/mL clear |
| 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 | 2.5747 mL | 12.8737 mL | 25.7473 mL |
| 5 mM | 0.5149 mL | 2.5747 mL | 5.1495 mL |
| 10 mM | 0.2575 mL | 1.2874 mL | 2.5747 mL |