|
Category:
|
7TM Receptors Peptides (Hypothalamic/Pituitary Hormones)Gonadotropin-releasing Hormone Receptors
|
|
Cat.No.
|
Product Name
|
|
2519 |
T 98475
|
|
|
|
Price and Availability
Click here for full price details of
T 98475
|
|
Chemical Name:
7-[(2,6-Difluorophenyl)methyl]-4,7-dihydro-2-[4-[(2-met
hyl-1-oxopropyl)amino]phenyl]-3-[[methyl(phenylmethyl)a
mino]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:
|
|
|
Resources:
|
|
Certificate of Analysis / MSDS:
|
References:
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. 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. 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.
|
|
View related products by Pharmacological Action
or by Research Area
Keywords: T 98475, Peptides (Hypothalamic / Pituitary Hormones), Gonadotropin-releasing Hormone (GnRH, LHRH) Receptor Antagonist, T98475, Tocris Bioscience
|
|
|
