Potent, orally active and non-peptide gonadotropin-releasing hormone (GnRH, LHRH) receptor antagonist (IC50 values are 0.2, 4.0 and 60 nM for human, monkey and rat GnRH receptors respectively). Inhibits LH release in vitro (IC50 = 100 nM) and reduces plasma LH concentration in castrated male cynomolgus monkeys.
|Storage||Desiccate at +4°C|
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.
|Solvent||Max Conc. mg/mL||Max Conc. mM|
Preparing Stock Solutions
The following data is based on the product molecular weight 657.77. 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||1.52 mL||7.6 mL||15.2 mL|
|5 mM||0.3 mL||1.52 mL||3.04 mL|
|10 mM||0.15 mL||0.76 mL||1.52 mL|
|50 mM||0.03 mL||0.15 mL||0.3 mL|
References are publications that support the products' biological activity.
Cho et al (1998) Discovery of a novel, potent, and orally active nonpeptide antagonist of the human luteinizing hormone-releasing hormone (LHRH) receptor. J.Med.Chem. 41 4190 PMID: 9784092
Sasaki et al (2003) Discovery of a thieno[2,3-d]pyrimidine-2,4-dione bearing a p-methoxyureidophenyl moiety at the 6-position: a highly potent and orally bioavailable non-peptide antagonist for the human luteinizing hormone-releasing hormone receptor. J.Med.Chem. 46 113 PMID: 12502365
Imada et al (2006) Design, synthesis, and structure-activity relationships of thieno[2,3-b]pyridin-4-one derivatives as a novel class of potent, orally active, non-peptide luteinizing hormone-releasing hormone receptor antagonists. J.Med.Chem. 49 3809 PMID: 16789738
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