生物活性
TVB-3166 is a cell-permeable pyrrazole derivative that inhibits cellular palmitate synthesis (IC50<100 nM) by fatty acid synthase (FASN) keto-reductase activity in a potent and reversible manner (IC50= 42 nM), effectively inhibiting palmitate-dependent survival of various cancer cells in cultures and xenografted tumor growth in micevivo(60-100 mg/kg/d p.o.), while exhibiting little or no anti-proliferation activity toward non-palmitate-dependent growth of cancer and non-cancer cultures. FASN inhibition by TVB-3166 treatment is also effective against the replications respiratory viruses both in cultures (Effc. conc. 200 nM against RSV and PIV3 in A549, HEp2, and HeLa cultures) and in mice (50 mg/kg/12 h, p.o.; RSV)in vivowithout significant adverse effects to the host cells or mice.
化学数据
| 分子量 |
384.47 |
| 分子式 |
C24H24N4O |
| CAS号 |
1533438-83-3 |
| 纯度 |
>98% |
| 溶解性（25°C） |
DMSO: 5 mg/mL
clear (warmed) |
| 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
以下数据基于半岛bd体育手机客户端 分子量，对于特殊半岛bd体育手机客户端 ，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 |
2.601 mL |
13.0049 mL |
26.0098 mL |
| 5 mM |
0.5202 mL |
2.601 mL |
5.202 mL |
| 10 mM |
0.2601 mL |
1.3005 mL |
2.601 mL |
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