AG-045572
Based on 1 Customer Validation
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.
Para uso exclusivo en investigación. No vendemos a pacientes.
- Pureza: 99.52%
- No. CAS: 263847-55-8
- Fòrmula: C30H37NO5
- Peso molecular:491.62
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Almacenamiento:
4°C, protect from light
* In solvent : -80°C, 6 months; -20°C, 1 month (protect from light)
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Actividad biológica
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 CYP3A4 (HY-P74210) in both rats and humans with the Km values were similar in male and female human, female rat liver microsomes, and expressed CYP3A4 and CYP3A5 (0.39, 0.27, 0.28, 0.25, and 0.26 μM, respectively), and the Km in male rat liver microsomes was 1.5 μM, suggesting that in male and female rats AG-045572 is metabolized by different CYP3A isozymes[1].
MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.
AG-045572 (40 mg/kg, i.m. twice a day for 3 days) pretreated of intact male rats resulted in a change of its pharmacokinetics, the parameters became similar to those in female and castrated male rats[1].
Pharmacokinetic Parameters of AG-045572 in Rats after Administration at 10 mg/kg i.v. and 20 mg/kg p.o.[1]
Pharmacokinetic Analysis[1]
| Animals | t1/2 (h) | CL (L/h/kg) | Vss (L/kg) | Cmax (μM) | Tmax (h) | Fp.o. (%) |
| Male | 1.4 ± 0.1 | 2.2 ± 0.5 | 2.1 ± 0.1 | 0.61 ± 0.21 | 1 | 8 |
| Female | 1.7 ± 0.1 | 1.5 ± 0.1 | 2.7 ± 0.4 | 2.31 ± 0.57 | 1 | 24 |
| Castrated male | 1.7 ± 0.4 | 1.5 ± 0.3 | 3.7 ± 1.5 | 1.98 ± 0.51 | 1 | 23 |
| Pretreated male | 1.9 ± 0.2 | 1.5 ± 0.2 | 2.0 ± 0.6 | 1.89 ± 0.41 | 1 | 27 |
MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.
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Animal Model:Male rats were surgically castrated via scrotal approach under halothane anesthesia and allowed 14 days post-operative recovery prior to study[1]
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Dosage:10 mg/kg, 20 mg/kg; 40 mg/kg
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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.
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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.
Chemical Information
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No. CAS 263847-55-8
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Appearance Solid
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Peso molecular 491.62
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Fòrmula C30H37NO5
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Color White to off-white
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SMILES
CC1(C2=CC(CC3=CC=C(C(NC4=C(C=C(OC)C=C4OC)OC)=O)O3)=C(C)C=C2C(C)(C)CC1)C
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Envío
Room temperature in continental US; may vary elsewhere.
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Almacenamiento
4°C, protect from light
* In solvent : -80°C, 6 months; -20°C, 1 month (protect from light)
Pureza y Documentación
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Ficha de datos (274 KB)
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SDS (252 KB)
- English - EN (252 KB)
- Français - FR (252 KB)
- Deutsch - DE (252 KB)
- Norwegian - NO (252 KB)
- Español - ES (252 KB)
- Swedish - SV (252 KB)
- Italian - IT (252 KB)
- Korean - KR (252 KB)
- Portuguese - PT (252 KB)
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Instrucciones de manejo (2659 KB)
Referencias
Calculators
Concentration (start) × Volume (start) = Concentration (final) × Volume (final)
AG-045572 Related Classifications
HY-107534 Related Classifications
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