生物活性
Obeticholic Acid (INT-747) improved the histological features of non-alcoholic steatohepatitis, but its long-term benefits and safety need further clarification. HS diet downregulated tissue DDAH expression while INT-747 protected the loss in DDAH expression and enhanced insulin sensitivity compared to vehicle controls. Intercept's lead drug candidate, the FXR agonist INT-747, is currently being advanced for chronic liver disease indications. Obeticholic acid is undergoing development in phase 2 and 3 studies for specific liver and gastrointestinal disorders.
化学数据
分子量 | 420.63 |
分子式 | C26H44O4 |
CAS号 | 459789-99-2 |
纯度 | 100.00% |
溶解性(25°C) | DMSO 60 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 | 2.3774 mL | 11.8869 mL | 23.7739 mL |
5 mM | 0.4755 mL | 2.3774 mL | 4.7548 mL |
10 mM | 0.2377 mL | 1.1887 mL | 2.3774 mL |