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NBI 42902

Cat. No. M13419

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NBI 42902 Structure

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Quality Control & Documentation
Biological Activity

NBI-42902 is an effective inhibitor of peptide radioligand binding to human GnRH receptor (K(I)=0.56 nm). Tritiated NBI-42902 binds to a single class of binding sites with high affinity (K(d)=0.19 nm) and can be replaced by a range of peptide and non-peptide GnRH receptor ligands.

Chemical Information
Molecular Weight 495.49
Formula C27H24F3N3O3
CAS Number 352290-60-9
Storage Powder          -20°C   3 years ;  4°C   2 years
In solvent       -80°C   6 months ;  -20°C   1 month
References

[1] Susan K Sullivan, et al. Biochemistry. Allosteric and orthosteric binding modes of two nonpeptide human gonadotropin-releasing hormone receptor antagonists

[2] R Scott Struthers, et al. Endocrinology. Pharmacological characterization of a novel nonpeptide antagonist of the human gonadotropin-releasing hormone receptor, NBI-42902

[3] Susan K Sullivan, et al. Biochem Pharmacol. Kinetics of nonpeptide antagonist binding to the human gonadotropin-releasing hormone receptor: Implications for structure-activity relationships and insurmountable antagonism

[4] R Scott Struthers, et al. J Clin Endocrinol Metab. Suppression of serum luteinizing hormone in postmenopausal women by an orally administered nonpeptide antagonist of the gonadotropin-releasing hormone receptor (NBI-42902)

[5] Fabio C Tucci, et al. J Med Chem. 3-[(2R)-Amino-2-phenylethyl]-1-(2,6-difluorobenzyl)-5-(2-fluoro-3-methoxyphenyl)- 6-methylpyrimidin-2,4-dione (NBI 42902) as a potent and orally active antagonist of the human gonadotropin-releasing hormone receptor. Design, synthesis, and in vitro and in䲧璵Ỵ璶㧀璴羹癦

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Keywords: NBI 42902 supplier, inhibitors, activators

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