AG 045572

本公司产品仅用于科研实验，不得用于人体或动物的临床与诊断

AG-045572 是一种 GnRH 受体拮抗剂，对人类和大鼠的 GnRH receptor 的 Ki 值分别为 6.0 nM 和 3.8 nM。AG-045572 通过 CYP3A 代谢并抑制睾酮。

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.

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) .

Animal Model:Male rats were surgically castrated via scrotal approach under halothane anesthesia and allowed 14 days post-operative recovery prior to studyDosage: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.

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Metabolic Enzyme/Protease

P450

P450 | GNRH Receptor

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263847-55-8

491.62

C30H37NO5

>98% (HPLC)

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CC1(C)C=2C(=CC(C)=C(CC=3OC(C(NC4=C(OC)C=C(OC)C=C4OC)=O)=CC3)C2)C(C)(C)CC1

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(-20℃)

With Ice Pack

≥ 2 years