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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Based on 1 publication(s) in Google Scholar

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.
Unlabeled CAS

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)

Solvent & Solubility
In Vitro: 

DMSO : 100 mg/mL (203.41 mM; Need ultrasonic; Hygroscopic DMSO has a significant impact on the solubility of product, please use newly opened DMSO)

Preparing
Stock Solutions
Concentration Solvent Mass 1 mg 5 mg 10 mg
1 mM 2.0341 mL 10.1705 mL 20.3409 mL
5 mM 0.4068 mL 2.0341 mL 4.0682 mL
View the Complete Stock Solution Preparation Table

* Please refer to the solubility information to select the appropriate solvent. Once prepared, please aliquot and store the solution to prevent product inactivation from repeated freeze-thaw cycles.
Storage method and period of stock solution: -80°C, 6 months; -20°C, 1 month (protect from light). When stored at -80°C, please use it within 6 months. When stored at -20°C, please use it within 1 month.

  • Molarity Calculator

  • Dilution Calculator

Mass (g) = Concentration (mol/L) × Volume (L) × Molecular Weight (g/mol)

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Concentration (start) × Volume (start) = Concentration (final) × Volume (final)

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In Vivo:

Select the appropriate dissolution method based on your experimental animal and administration route.

For the following dissolution methods, please ensure to first prepare a clear stock solution using an In Vitro approach and then sequentially add co-solvents:
To ensure reliable experimental results, the clarified stock solution can be appropriately stored based on storage conditions. As for the working solution for in vivo experiments, it is recommended to prepare freshly and use it on the same day.
The percentages shown for the solvents indicate their volumetric ratio in the final prepared solution. If precipitation or phase separation occurs during preparation, heat and/or sonication can be used to aid dissolution.

  • Protocol 1

    Add each solvent one by one:  10% DMSO    40% PEG300    5% Tween-80    45% Saline

    Solubility: ≥ 2.5 mg/mL (5.09 mM); Clear solution

    This protocol yields a clear solution of ≥ 2.5 mg/mL (saturation unknown).

    Taking 1 mL working solution as an example, add 100 μL DMSO stock solution (25.0 mg/mL) to 400 μL PEG300, and mix evenly; then add 50 μL Tween-80 and mix evenly; then add 450 μL Saline to adjust the volume to 1 mL.

    Preparation of Saline: Dissolve 0.9 g sodium chloride in ddH₂O and dilute to 100 mL to obtain a clear Saline solution.
  • Protocol 2

    Add each solvent one by one:  10% DMSO    90% Corn Oil

    Solubility: ≥ 2.5 mg/mL (5.09 mM); Clear solution

    This protocol yields a clear solution of ≥ 2.5 mg/mL (saturation unknown). If the continuous dosing period exceeds half a month, please choose this protocol carefully.

    Taking 1 mL working solution as an example, add 100 μL DMSO stock solution (25.0 mg/mL) to 900 μL Corn oil, and mix evenly.

In Vivo Dissolution Calculator
Please enter the basic information of animal experiments:

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mg/kg

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g

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(per animal)

μL

Number of animals

Recommended: Prepare an additional quantity of animals to account for potential losses during experiments.
Please enter your animal formula composition:
%
DMSO +
% 
+
%
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%
Saline
Recommended: Keep the proportion of DMSO in working solution below 2% if your animal is weak.
The co-solvents required include: DMSO, . All of co-solvents are available by MedChemExpress (MCE). , Tween 80. All of co-solvents are available by MedChemExpress (MCE).
Calculation results:
Working solution concentration: mg/mL
Method for preparing stock solution: mg drug dissolved in μL  DMSO (Stock solution concentration: mg/mL).

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

The concentration of the stock solution you require exceeds the measured solubility. The following solution is for reference only. If necessary, please contact MedChemExpress (MCE).
Method for preparing in vivo working solution for animal experiments: Take μL DMSO stock solution, add μL . μL , mix evenly, next add μL Tween 80, mix evenly, then add μL Saline.
 If the continuous dosing period exceeds half a month, please choose this protocol carefully.
Please ensure that the stock solution in the first step is dissolved to a clear state, and add co-solvents in sequence. You can use ultrasonic heating (ultrasonic cleaner, recommended frequency 20-40 kHz), vortexing, etc. to assist dissolution.
Purity & Documentation
References

Complete Stock Solution Preparation Table

* Please refer to the solubility information to select the appropriate solvent. Once prepared, please aliquot and store the solution to prevent product inactivation from repeated freeze-thaw cycles.
Storage method and period of stock solution: -80°C, 6 months; -20°C, 1 month (protect from light). When stored at -80°C, please use it within 6 months. When stored at -20°C, please use it within 1 month.

Optional Solvent Concentration Solvent Mass 1 mg 5 mg 10 mg 25 mg
DMSO 1 mM 2.0341 mL 10.1705 mL 20.3409 mL 50.8523 mL
5 mM 0.4068 mL 2.0341 mL 4.0682 mL 10.1705 mL
10 mM 0.2034 mL 1.0170 mL 2.0341 mL 5.0852 mL
15 mM 0.1356 mL 0.6780 mL 1.3561 mL 3.3902 mL
20 mM 0.1017 mL 0.5085 mL 1.0170 mL 2.5426 mL
25 mM 0.0814 mL 0.4068 mL 0.8136 mL 2.0341 mL
30 mM 0.0678 mL 0.3390 mL 0.6780 mL 1.6951 mL
40 mM 0.0509 mL 0.2543 mL 0.5085 mL 1.2713 mL
50 mM 0.0407 mL 0.2034 mL 0.4068 mL 1.0170 mL
60 mM 0.0339 mL 0.1695 mL 0.3390 mL 0.8475 mL
80 mM 0.0254 mL 0.1271 mL 0.2543 mL 0.6357 mL
100 mM 0.0203 mL 0.1017 mL 0.2034 mL 0.5085 mL
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AG-045572 Related Classifications

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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