Powder: -20°C for 3 years | In solvent: -80°C for 1 year
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.
パッケージサイズ | 在庫状況 | 単価(税別) | |||
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サンプルについてお問い合わせ | |||||
1 mg | 在庫あり | ¥ 36,000 | |||
5 mg | 在庫あり | ¥ 61,500 | |||
10 mg | 在庫あり | ¥ 80,000 | |||
25 mg | 在庫あり | ¥ 136,500 | |||
50 mg | 在庫あり | ¥ 195,000 | |||
100 mg | 在庫あり | ¥ 268,500 | |||
500 mg | 在庫あり | ¥ 535,000 |
説明 | 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. |
ターゲット&IC50 | GnRH receptor (human):6.0 nM(ki), GnRH receptor (rat):3.8 nM(ki) |
In vitro | 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) is metabolized by CYP3A in both rats and humans. The Km values in male and female human and female rat liver microsomes and expressed CYP3A4 and CYP3A5 were similar (0.39, 0.27, 0.28, 0.25, and 0.26 μM, respectively), while the Km values in male rat liver microsomes were 1.5 μM, indicating that AG-045572 is metabolized by different CYP3A isoenzymes in male and female rats.[1] |
In vivo |
AG 045572 (10 mg/kg (i.v.) or 20 mg/kg (p.o.), one time) in intact male rats showed moderate T1/2, CL and Vss but low oral bioavailability, with The bioavailability is higher in female rats (24%), and the pharmacokinetics in castrated male rats are similar to those in female rats.[1] The pharmacokinetics of AG 045572 (40 mg/kg; i.m.; twice a day for 3 days) in intact male rats changed, and the parameters were similar to those in female and castrated male rats.[1] |
分子量 | 491.62 |
分子式 | C30H37NO5 |
CAS No. | 263847-55-8 |
Powder: -20°C for 3 years | In solvent: -80°C for 1 year
DMSO: 55 mg/mL (111.88 mM)
You can also refer to dose conversion for different animals. 詳細
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AG 045572 263847-55-8 GPCR/G Protein Metabolism P450 GNRH Receptor AG-045572 AG045572 Inhibitor inhibitor inhibit