| Identification | Back Directory | [Name]
NBI-42902 | [CAS]
352290-60-9 | [Synonyms]
CS-1113
NBI-42902
NBI-42902;NBI 42902
3-[(2R)-2-Amino-2-phenylethyl]-1-[(2,6-difluorophenyl)methyl]-5-(2-fluoro-3-methoxyphenyl)-6-methyl-2,4(1H,3H)-pyrimidinedione
2,4(1H,3H)-Pyrimidinedione, 3-[(2R)-2-amino-2-phenylethyl]-1-[(2,6-difluorophenyl)methyl]-5-(2-fluoro-3-methoxyphenyl)-6-methyl- | [Molecular Formula]
C27H24F3N3O3 | [MDL Number]
MFCD20275092 | [MOL File]
352290-60-9.mol | [Molecular Weight]
495.49 |
| Hazard Information | Back Directory | [Uses]
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]. | [in vivo]
NBI-42902 (10-100 mg/kg, p.o. or i.v. ) inhibits serum LH levels significantly in castrated macaques[1]. | Animal Model: | Castrated macaques[1] | | Dosage: | 10, 40, 100 mg/kg | | Administration: | Oral administration (p.o.) | | Result: | Inhibited serum LH with dose dependent.
Inhibited serum LH achieved maximum suppression, that was 62-68% of pretreatment baseline, at 4-8 h after administration.
Exhibited no suppression of LH levels after 24 h treated with 10 or 40 mg/kg, but remained suppression at 100 mg/kg.
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| Animal Model: | Castrated macaques[1] | | Dosage: | 10 mg/kg | | Administration: | Intravenous injection (i.v.) | | Result: | Inhibited serum LH achieved maximum suppression was 62-68% of pretreatment baseline between 4-8 h after administration, but exhibited no suppression after 24 h.
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| [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. DOI:10.1210/en.2006-1213 |
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| Company Name: |
Cckinase, Inc.
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+1 (732)236-3202 |
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www.cckinase.com |
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Wuhan Topule
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http://www.topule.com/ |
| Company Name: |
InvivoChem
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13549236410 |
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https://www.invivochem.cn/ |
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