Chemical Name: 5-[5,6,7,8-Tetrahydro-3,5,5,8,8-pentamethyl-2-naphthalenyl-methyl]-N-(2,4,6-trimethoxyphenyl)-2-furancarboxamide
Purity: ≥97% (HPLC)
Biological Activity
Technical Data
Solubility
Calculators
Datasheets
References
Biological Activity
Selective gonadotropin-releasing hormone (GnRH) receptor antagonist (Ki values are 2.2, 3.8 and 6.0 nM for mouse, rat and human receptors respectively). Suppresses testosterone and luteinising hormone (LH) levels in vivo.
The technical data provided above is for guidance only. For batch specific data refer to the Certificate of Analysis.
All Tocris products are intended for laboratory research use only.
Solubility Data
Solvent
Max Conc. mg/mL
Max Conc. mM
Solubility
DMSO
49.16
100
ethanol
24.58
50
Preparing Stock Solutions
The following data is based on the product molecular weight 491.62. Batch specific molecular weights may vary from batch to batch due to solvent of hydration, which will affect the solvent volumes required to prepare stock solutions.
Concentration / Solvent Volume / Mass
1 mg
5 mg
10 mg
1 mM
2.03 mL
10.17 mL
20.34 mL
5 mM
0.41 mL
2.03 mL
4.07 mL
10 mM
0.2 mL
1.02 mL
2.03 mL
50 mM
0.04 mL
0.2 mL
0.41 mL
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Product Datasheets
Certificate of Analysis / Product Datasheet
Safety Datasheet
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References
References are publications that support the products' biological activity.
Iatsimirskaiaet al (2002) Effect of testosterone suppression on the pharmacokinetics of a potent GnRH receptor antagonist. Pharm.Res. 19 202 PMID: 11883648
Andereset al (2003) Biological characterization of a novel, orally active small molecule gonadotropin-releasing hormone (GnRH) antagonist using castrated and intact rats. J.Pharmacol.Exp.Ther. 305 688 PMID: 12606616