生物活性
Goserelin is an injectable gonadotropin releasing hormone superagonist (GnRH agonist), also known as a luteinizing hormone releasing hormone (LHRH) agonist. Goserelin is a synthetic analogue of a naturally occurring luteinising-hormone releasing hormone (LHRH). Goserelin Acetate is a potent GnRH (LHRH) agonist. After a transient increase, continuous administration of goserelin results in downregulation of LH and FSH levels followed by a suppression of ovarian and testicular steroid biosynthesis. It rapidly binds to the LHRH receptor cells in the pituitary gland thus leading to an initial increase in production of luteinizing hormone and thus leading to an initial increase in the production of corresponding sex hormones.
化学数据
分子量 | 1329.46 |
分子式 | C59H84N18O14.C2H4O2 |
CAS号 | 145781-92-6 |
纯度 | >98% |
溶解性(25°C) | DMSO |
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 | 0.7522 mL | 3.7609 mL | 7.5219 mL |
5 mM | 0.1504 mL | 0.7522 mL | 1.5044 mL |
10 mM | 0.0752 mL | 0.3761 mL | 0.7522 mL |