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1383719-97-8

1383719-97-8 structure
1383719-97-8 structure
  • Name: PF 04628935
  • Chemical Name: 1-{2-[2-Chloro-4-(2H-1,2,3-triazol-2-yl)benzyl]-2,7-diazaspiro[3.5]non-7-yl}-2-(2-methylimidazo[2,1-b][1,3]thiazol-6-yl)ethanone
  • CAS Number: 1383719-97-8
  • Molecular Formula: C24H26ClN7OS
  • Molecular Weight: 496.03
  • Catalog: Signaling Pathways GPCR/G Protein GHSR
  • Create Date: 2021-01-10 17:59:41
  • Modify Date: 2024-01-17 10:32:48
  • PF-04628935 (compound 10n) is a potent ghrelin receptor inverse agonist, with an IC50 of 4.6 nM. PF-04628935 exhibits oral bioavailability of 43% in rats and shows reasonable penetration into the brain. PF-04628935 can be used for stress and anxiety research[1][2].

Name 1-{2-[2-Chloro-4-(2H-1,2,3-triazol-2-yl)benzyl]-2,7-diazaspiro[3.5]non-7-yl}-2-(2-methylimidazo[2,1-b][1,3]thiazol-6-yl)ethanone
Synonyms 1-{2-[2-Chloro-4-(2H-1,2,3-triazol-2-yl)benzyl]-2,7-diazaspiro[3.5]non-7-yl}-2-(2-methylimidazo[2,1-b][1,3]thiazol-6-yl)ethanone
Ethanone, 1-[2-[[2-chloro-4-(2H-1,2,3-triazol-2-yl)phenyl]methyl]-2,7-diazaspiro[3.5]non-7-yl]-2-(2-methylimidazo[2,1-b]thiazol-6-yl)-
Description PF-04628935 (compound 10n) is a potent ghrelin receptor inverse agonist, with an IC50 of 4.6 nM. PF-04628935 exhibits oral bioavailability of 43% in rats and shows reasonable penetration into the brain. PF-04628935 can be used for stress and anxiety research[1][2].
Related Catalog
Target

GHSR1a:4.6 nM (IC50)

References

[1]. Kung DW, et, al. Identification of spirocyclic piperidine-azetidine inverse agonists of the ghrelin receptor. Bioorg Med Chem Lett. 2012 Jul 1;22(13):4281-7.  

[2]. Cavalcante DP, et, al. Role of dorsal raphe nucleus GHS-R1a receptors in the regulation of inhibitory avoidance and escape behaviors in rats. Behav Brain Res. 2019 Jun 3;365:178-184.  

Density 1.5±0.1 g/cm3
Molecular Formula C24H26ClN7OS
Molecular Weight 496.03
Exact Mass 495.160797
LogP 4.14
Index of Refraction 1.764
RIDADR NONH for all modes of transport