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NBI42902

Names

[ CAS No. ]:
352290-60-9

[ Name ]:
NBI42902

[Synonym ]:
3-[(R)-amino-2-phenylethyl]-5-(2-fluoro-3-methoxyphenyl)-1-[2,6-difluorobenzyl]-6-methyl-pyrimidine-2,4(1H,3H)-dione
2,4(1H,3H)-Pyrimidinedione, 3-[(2R)-2-amino-2-phenylethyl]-1-[(2,6-difluorophenyl)methyl]-5-(2-fluoro-3-methoxyphenyl)-6-methyl-
3-[(2R)-2-Amino-2-phenylethyl]-1-(2,6-difluorobenzyl)-5-(2-fluoro-3-methoxyphenyl)-6-methyl-2,4(1H,3H)-pyrimidinedione
3-[(2R)-2-amino-2-phenylethyl]-1-(2,6-difluorobenzyl)-5-(2-fluoro-3-methoxyphenyl)-6-methylpyrimidine-2,4(1H,3H)-dione
3-[2(R)-amino-2-phenylethyl]-5-(2-fluoro-3-methoxyphenyl)-1-[2,6-difluorobenzyl]-6-methylpyrimidine-2,4(1H,3H)-dione
NBI42902

Biological Activity

[Description]:

NBI-42902 is an orally active, potent functional and competitive antagonist of GnRH receptor with an IC50 value of 0.79 nM, a Ki value of 0.56 nM, respectively. NBI-42902 inhibits GnRH-stimulated inositol phosphate (IP) accumulation, Ca2+ flux, and ERK1/2 activation. NBI-42902 inhibits serum luteinizing hormone (LH) in castrated male macaques. NBI-42902 can be used for research on sex-hormone-related diseases[1].

[Related Catalog]:

Signaling Pathways >> GPCR/G Protein >> GNRH Receptor
Research Areas >> Others
Signaling Pathways >> Cell Cycle/DNA Damage >> PERK

[References]

[1]. Struthers RS, et al. Pharmacological characterization of a novel nonpeptide antagonist of the human gonadotropin-releasing hormone receptor, NBI-42902. Endocrinology. 2007 Feb;148(2):857-67.  

Chemical & Physical Properties

[ Density]:
1.3±0.1 g/cm3

[ Boiling Point ]:
631.0±65.0 °C at 760 mmHg

[ Molecular Formula ]:
C27H24F3N3O3

[ Molecular Weight ]:
495.49

[ Flash Point ]:
335.4±34.3 °C

[ Exact Mass ]:
495.176971

[ PSA ]:
79.25000

[ LogP ]:
6.42

[ Vapour Pressure ]:
0.0±1.8 mmHg at 25°C

[ Index of Refraction ]:
1.602

Synthetic Route

Click to get detail synthetic route

Precursor & DownStream

Precursor

DownStream

Related Compounds