产品
编 号：F298299
分子式：C30H37NO5
分子量：491.62
分子式：C30H37NO5
分子量：491.62
产品类型
规格
价格
是否有货
1mg
询价
询价
5mg
询价
询价
10mg
询价
询价
结构图
CAS No: 263847-55-8
产品详情
生物活性：
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.
体内研究：
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。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。Animal Model:Male rats were surgically castrated via scrotal approach under halothane anesthesia and allowed 14 days post-operative recovery prior to study
Dosage:10 mg/kg, 20 mg/kg; 40 mg/kg
Administration:administered acutely at 10 mg/kg (i.v.) or 20 mg/kg (p.o.), one time; For multiple-dose pretreatment, male rats at 40 mg/kg, i.m. twice a day for 3 days.
Result:Showed medium T1/2, CL and Vss but oral bioavailability was low, in female rats the bioavailability was much higher (24%)Became similar to those in female and castrated male rats.
体外研究：
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。
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.
体内研究：
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。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。Animal Model:Male rats were surgically castrated via scrotal approach under halothane anesthesia and allowed 14 days post-operative recovery prior to study
Dosage:10 mg/kg, 20 mg/kg; 40 mg/kg
Administration:administered acutely at 10 mg/kg (i.v.) or 20 mg/kg (p.o.), one time; For multiple-dose pretreatment, male rats at 40 mg/kg, i.m. twice a day for 3 days.
Result:Showed medium T1/2, CL and Vss but oral bioavailability was low, in female rats the bioavailability was much higher (24%)Became similar to those in female and castrated male rats.
体外研究：
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。
产品资料
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