T 98475

Cat. No. 2519

T 98475 C37H37F2N3O4S [199119-18-1]

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Chemical Name: 7-[(2,6-Difluorophenyl)methyl]-4,7-dihydro-2-[4-[(2-methyl-1-oxopropyl)amino]phenyl]-3-[[methyl(phenylmethyl)amino]methyl]-4-oxo-thieno[2,3-b]pyridine-5-carboxylic acid 1-methylethyl ester

Biological Activity

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.

Technical Data

M.Wt:
657.77
Formula:
C37H37F2N3O4S
Solubility:
Soluble to 50 mM in DMSO
Purity:
>98 %
Storage:
Desiccate at +4°C
CAS No:
199119-18-1

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.

Certificate of Analysis / Product Datasheet / Safety Datasheet

References are publications that support the products' biological activity.

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.

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.

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.

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Keywords: T 98475, supplier, GnRH, receptor, antagonists, Receptors, Gonadotrophin-Releasing, Hormone, T98475, gonadotropin, Tocris Bioscience, Gonadotropin-Releasing Hormone Receptor Antagonist products

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