NBI-42902

TargetMol
Product Code: TAR-T69383
Supplier: TargetMol
CodeSizePrice
TAR-T69383-5mg5mg£327.00
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TAR-T69383-50mg50mg£1,444.00
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TAR-T69383-100mg100mg£2,079.00
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Overview

Regulatory Status: RUO
Shipping:
cool pack
Storage:
-20°C

Images

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Further Information

Bioactivity:
NBI-42902 is a potent inhibitor of peptide radioligand binding to the human GnRH receptor (K(i) = 0.56 nm). Tritiated NBI-42902 binds with high affinity (K(d) = 0.19 nm) to a single class of binding sites and can be displaced by a range of peptide and nonpeptide GnRH receptor ligands. In vitro experiments demonstrate that NBI-42902 is a potent functional, competitive antagonist of GnRH stimulated IP accumulation, Ca(2+) flux, and ERK1/2 activation. It did not stimulate histamine release from rat peritoneal mast cells. Finally, it is effective in lowering serum LH in castrated male macaques after oral administration. Overall, these data provide a benchmark of pharmacological characteristics required for a nonpeptide GnRH antagonist to effectively suppress gonadotropins in humans and suggest that NBI-42902 may have clinical utility as an oral agent for suppression of the hypothalamic-pituitary-gonadal axis. (source: Endocrinology. 2007 Feb;148(2):857-67. Epub 2006 Nov 9.)
CAS:
352290-60-9
Molecular Weight:
495.49
Purity:
0.98