NBI-42902

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].

Product Specifications

CAS Number

[352290-60-9]

UNSPSC

12352005

Hazard Statement

H302, H315, H319, H335

Target

GnRH Receptor; PERK

Type

Reference compound

Related Pathways

Cell Cycle/DNA Damage; GPCR/G Protein

Applications

Cancer-Kinase/protease

Field of Research

Others

Assay Protocol

https://www.medchemexpress.com/nbi-42902.html

Concentration

10mM

Purity

98.65

Solubility

DMSO : 100 mg/mL (ultrasonic)

Smiles

O=C1N(C[C@H](N)C2=CC=CC=C2)C(C(C3=CC=CC(OC)=C3F)=C(C)N1CC4=C(F)C=CC=C4F)=O

Molecular Formula

C27H24F3N3O3

Molecular Weight

495.49

Precautions

H302, H315, H319, H335

References & Citations

[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.