| Bioactivity | AG-045572 is a GnRH receptor antagonist with Kis of 6.0 nM and 3.8 nM for human and rat GnRH receptor, respectively. AG-045572 is metabolized by CYP3A and ressuppresses testosterone[1]. |
| Invitro | AG-045572 (10 μM, 40 min, for human liver microsomes; 10 μM, 10 min, for male rat liver microsomes; 1 μM, 10 min, for female rat liver microsomes) 在大鼠和人体内均通过 CYP3A 代谢，在雄性和雌性人、雌性大鼠肝脏微粒体以及表达的 CYP3A4 和 CYP3A5 中的 Km 值相似 (分别为0.39、0.27、0.28、0.25和0.26 μM)，而在雄性大鼠肝脏微粒体中的 Km 值为 1.5 μM，表明 AG-045572 在雄性和雌性大鼠体内通过不同的 CYP3A 同工酶代谢[1]。 |
| In Vivo | AG-045572 (10 mg/kg (i.v.) or 20 mg/kg (p.o.), one time) 用于完整雄性大鼠，显示出中等的 T1/2、CL 和 Vss，但口服生物利用度较低，用于雌性大鼠的生物利用度较高 (24%)，用于阉割雄性大鼠的药代动力学与雌性大鼠相似[1]。AG-045572 (40 mg/kg, i.m. twice a day for 3 days) 预处理完整雄性大鼠后，其药代动力学发生变化，各项参数与雌性和阉割雄性大鼠相似[1]。 Animal Model: |
| Name | AG-045572 |
| CAS | 263847-55-8 |
| Formula | C30H37NO5 |
| Molar Mass | 491.62 |
| Transport | Room temperature in continental US; may vary elsewhere. |
| Storage | Please store the product under the recommended conditions in the Certificate of Analysis. |
| Reference | [1]. Iatsimirskaia EA, et al. Effect of testosterone suppression on the pharmacokinetics of a potent gnRH receptor antagonist. Pharm Res. 2002 Feb;19(2):202-8. |