生物活性
BGP-15 protects against nephrotoxicity of cisplatin without compromising its antitumor activity. BGP-15 inhibits caspase-independent programmed cell death in acetaminophen-induced liver injury. Moreover, BGP-15 was found to prevent imatinib-induced cardiotoxicity by activating Akt and suppressing JNK and p38 MAP kinases.
In vivo, BGP-15 (10 and 30 mg/kg) increases insulin sensitivity by 50% and 70%, respectively, in cholesterol-fed but not in normal rabbits. After 5 days of treatment with BGP-15, the glucose infusion rate is increased in a dose-dependent manner in genetically insulin-resistant GK rats. The most effective dose is 20 mg/kg, which shows a 71% increase in insulin sensitivity compared to control group. BGP-15 treatment is associated with a reduced PR interval in the HF+AF model.
化学数据
分子量 | 351.27 |
分子式 | C14H24Cl2N4O2 |
CAS号 | 66611-37-8 |
纯度 | >98% |
溶解性(25°C) | DMSO 10 mg/mL (Need warming) |
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 | 2.8468 mL | 14.2341 mL | 28.4681 mL |
5 mM | 0.5694 mL | 2.8468 mL | 5.6936 mL |
10 mM | 0.2847 mL | 1.4234 mL | 2.8468 mL |