2. GPCR/G Protein
  3. GnRH Receptor
  4. AG-045572

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.

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AG-045572 Chemical Structure

AG-045572 Chemical Structure

CAS No. : 263847-55-8

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AG-045572 Related Antibodies

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Description

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[1].

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 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 Related Antibodies
In Vivo

AG-045572 (10 mg/kg (i.v.) or 20 mg/kg (p.o.), one time) give to intact male rats, it showed medium T1/2, CL and Vss but oral bioavailability was low, in female rats the bioavailability was much higher (24%), in castrated male rats the pharmacokinetics was similar to that in female rats[1].
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]

大鼠静脉注射10 mg/kg和口服20 mg/kg剂量后AG-045572的药代动力学参数[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.

Animal Model: Male rats were surgically castrated via scrotal approach under halothane anesthesia and allowed 14 days post-operative recovery prior to study[1]
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.
Molecular Weight

491.62

Formula

C30H37NO5
CAS No.
Appearance

Solid

Color

White to off-white

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
Shipping

Room temperature in continental US; may vary elsewhere.
Storage

4°C, protect from light

*In solvent : -80°C, 6 months; -20°C, 1 month (protect from light)

Purity & Documentation
References
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AG-045572 Related Classifications

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Help & FAQs
  • Do most proteins show cross-species activity?

    Species cross-reactivity must be investigated individually for each product. Many human cytokines will produce a nice response in mouse cell lines, and many mouse proteins will show activity on human cells. Other proteins may have a lower specific activity when used in the opposite species.

Keywords:

AG-045572263847-55-8AG045572AG 045572GnRH ReceptorGonadotropin releasing hormone receptorGNRHRGnRH receptor antagonistorallyagonistin-haledliver microsomescastrated ratInhibitorinhibitorinhibit

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