NBI-42902

CAT: 0931-T69383-01Size: 25 mgDry Ice: NoHazardous: No
CAT#:0931-T69383-01Size:25 mg
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AVAILABILITY: InStock
24/48H Stock Items & 2 to 6 Weeks non Stock Items.
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CAS Number
352290-60-9
Target
Others|||PERK|||GNRH Receptor
Related Pathways
Others|||GPCR/G Protein|||Apoptosis
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.)
Smiles
CC1=C(C(=O)N(C[C@H](N)C2=CC=CC=C2)C(=O)N1CC3=C(F)C=CC=C3F)C4=C(F)C(OC)=CC=C4
Molecular Formula
C27H24F3N3O3
Molecular Weight
495.49
Shipping Conditions
Cool pack
Storage Temperature
-20°C

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