AG 045572

Research use only, not for human use.

AG 045572 is a potent GnRH receptor antagonist that inhibits the GnRH receptor in humans and rats with Ki values of 6.0 nM and 3.8 nM, respectively.AG 045572 is metabolized by CYP3A and inhibits testosterone.

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.

——

Metabolic Enzyme/Protease

P450

P450 | GNRH Receptor

——

——

263847-55-8

491.62

C30H37NO5

>98% (HPLC)

——

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

——

(-20℃)

With Ice Pack

≥ 2 years