生物活性
Mycophenolic acid是一种免疫抑制剂,用于预防器官移植排斥。Mycophenolic acid 也是一种有效的非竞争性肌苷单磷酸脱氢酶 (IMPDH) 抑制剂,EC50 为 0.24 μM,可抑制肝癌类器官的生长。Mycophenolic acid (mycophenolate) is derived from the fungus Penicillium stoloniferum. Mycophenolate mofetil is metabolised in the liver to the active moiety mycophenolic acid. Mycophenolic acid (mycophenolate) inhibits inosine monophosphate dehydrogenase, the enzyme that controls the rate of synthesis of guanine monophosphate in the de novo pathway of purine synthesis used in the proliferation of B and T lymphocytes.Mycophenolic acid (mycophenolate) is potent and can be used in place of the older anti-proliferative azathioprine. Mycophenolic acid (mycophenolate) is usually used as part of a three-compound regimen of immunosuppressants, also including a calcineurin inhibitor (ciclosporin or tacrolimus) and prednisolone.
化学数据
分子量 | 320.34 |
分子式 | C17H20O6 |
CAS号 | 24280-93-1 |
纯度 | 99.28% |
溶解性(25°C) | DMSO ≥ 40 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 | 3.1217 mL | 15.6084 mL | 31.2168 mL |
5 mM | 0.6243 mL | 3.1217 mL | 6.2434 mL |
10 mM | 0.3122 mL | 1.5608 mL | 3.1217 mL |