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AG 045572
🥰Excellent
Catalog No. T22025Cas No. 263847-55-8
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
🥰Excellent
Purity: 98.99%
Catalog No. T22025Cas No. 263847-55-8
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.
| Pack Size | Price | Availability | Quantity |
|---|---|---|---|
| 1 mg | 116 € | In Stock | |
| 5 mg | 234 € | In Stock | |
| 10 mg | 329 € | In Stock | |
| 25 mg | 533 € | In Stock | |
| 50 mg | 747 € | In Stock | |
| 100 mg | 1.016 € | In Stock |
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Purity:98.99%
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All TargetMol products are for research purposes only and cannot be used for human consumption. We do not provide products or services to individuals. Please comply with the intended use and do not use TargetMol products for any other purpose.Product Introduction
Bioactivity
Chemical Properties
| Description | 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. |
| Targets&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] |
| Molecular Weight | 491.62 |
| Formula | C30H37NO5 |
| Cas No. | 263847-55-8 |
| Smiles | 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 |
| Relative Density. | no data available |
Storage & Solubility Information
| Storage | Powder: -20°C for 3 years | In solvent: -80°C for 1 year | Shipping with blue ice. | |||||||||||||||||||||||||||||||||||
| Solubility Information | DMSO: 55 mg/mL (111.88 mM)  | |||||||||||||||||||||||||||||||||||
Solution Preparation Table | ||||||||||||||||||||||||||||||||||||
DMSO
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(mother liquor concentration of 40 mg/mL), if you need to configure a concentration that exceeds the solubility of the product, please contact us first.Preparation method for in vivo formula: Take 50 μL DMSO main solution, add 300 μLPEG300 mix well and clarify, then add 50 more μL Tween 80, mix well and clarify, then add 600 more μLddH2O mix well and clarify
main solution, add 300 μLPEG300 mix well and clarify, then add 50 more μL Tween 80, mix well and clarify, then add 600 more μLddH2O mix well and clarifyFor Reference Only. Please develop an appropriate dissolution method based on your laboratory animals and route of administration.
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